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List of works by Kenneth A. Jacobson

"Reversine" and its 2-substituted adenine derivatives as potent and selective A3 adenosine receptor antagonists

scientific article

(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists.

scientific article

2-Chloro-N(6)-cyclopentyladenosine, adenosine A(1) receptor agonist, antagonizes the adenosine A(3) receptor

scientific article published in May 2002

2-Phenylimidazo[2,1-i]purin-5-ones: structure-activity relationships and characterization of potent and selective inverse agonists at Human A3 adenosine receptors.

scientific article

2-[2-[4-[2-[2-[ 1,3-Dihydro- 1,1-bis (4-hydroxyphenyl)-3-oxo-5-isobenzofuranthioureidyl]ethylaminocarbonyl]ethyl]phenyl] ethylamino]-5'-N-ethylcarboxamidoadenosine (FITC-APEC): A Fluorescent Ligand For A2a-Adenosine Receptors.

scientific article published on December 1992

2-triazole-substituted adenosines: a new class of selective A3 adenosine receptor agonists, partial agonists, and antagonists

scientific article published on December 2006

4-Alkyloxyimino derivatives of uridine-5'-triphosphate: distal modification of potent agonists as a strategy for molecular probes of P2Y2, P2Y4, and P2Y6 receptors

scientific article

4-Alkyloxyimino-cytosine nucleotides: tethering approaches to molecular probes for the P2Y6 receptor.

scientific article published in May 2013

5′-Phosphate and 5′-Phosphonate Ester Derivatives of (N)-Methanocarba Adenosine with in Vivo Cardioprotective Activity ⬇️

scientific article published on January 22, 2013

6-phenyl-1,4-dihydropyridine derivatives as potent and selective A3 adenosine receptor antagonists

scientific article published on November 1996

8-Substituted xanthines as antagonists at A1- and A2-adenosine receptors.

scientific article

8-cyclopentyl-1,3-dipropylxanthine and other xanthines differentially bind to the wild-type and delta F508 first nucleotide binding fold (NBF-1) domains of the cystic fibrosis transmembrane conductance regulator

scientific article published on 01 May 1997

A Key Opinion Leader interview: insight into the research and career of Dr KA Jacobson.

scientific article published on 12 December 2014

A PROSTHETIC GROUP FOR THE RAPID INTRODUCTION OF FLUORINE INTO PEPTIDES AND FUNCTIONALIZED DRUGS.

scientific article

A binding kinetics study of human adenosine A3 receptor agonists.

scientific article

A conformationally locked analogue of the anti-HIV agent stavudine. An important correlation between pseudorotation and maximum amplitude

scientific article

A missense mutation in the seven-transmembrane domain of the human Ca2+ receptor converts a negative allosteric modulator into a positive allosteric modulator

scientific article published on 30 May 2006

A neoceptor approach to unraveling microscopic interactions between the human A2A adenosine receptor and its agonists

scientific article

A new synthetic route to (North)-methanocarba nucleosides designed as A3 adenosine receptor agonists.

scientific article published on January 2005

A physiological role of the adenosine A 3 receptor: Sustained cardioprotection ⬇️

scientific article published on June 9, 1998

A pyridoxine cyclic phosphate and its 6-azoaryl derivative selectively potentiate and antagonize activation of P2X1 receptors

scientific article published on June 1998

A region in the seven-transmembrane domain of the human Ca2+ receptor critical for response to Ca2+.

scientific article

A role for central A3-adenosine receptors. Mediation of behavioral depressant effects

scientific article

A selective high-affinity antagonist of the P2Y14 receptor inhibits UDP-glucose-stimulated chemotaxis of human neutrophils.

scientific article published on 16 April 2013

A2A adenosine receptor antagonists: From caffeine to selective non-xanthines

scientific article published on 18 May 2020

A2B Adenosine Receptor and Cancer

scientific article published on 17 October 2019

A2B adenosine receptor blockade inhibits growth of prostate cancer cells.

scientific article

A3 Adenosine Receptors as Modulators of Inflammation: From Medicinal Chemistry to Therapy

scientific article

A3 adenosine receptor activation mechanisms: molecular dynamics analysis of inactive, active, and fully active states

scientific article published on 22 November 2019

A3 adenosine receptor agonist prevents the development of paclitaxel-induced neuropathic pain by modulating spinal glial-restricted redox-dependent signaling pathways.

scientific article published on 19 September 2014

AMP-activated protein kinase as regulator of P2Y6 receptor-induced insulin secretion in mouse pancreatic β-cells ⬇️

scientific article published on January 17, 2013

Accelerating the Throughput of Affinity Mass Spectrometry-Based Ligand Screening toward a G Protein-Coupled Receptor

scientific article published on 12 June 2019

Action of nucleosides and nucleotides at 7 transmembrane-spanning receptors

scientific article published on January 2006

Actions of a Series of PPADS Analogs at P2X1 and P2X3 Receptors

scientific article published on August 2001

Activation and Desensitization of Rat A3-Adenosine Receptors by Selective Adenosine Derivatives and Xanthine-7-Ribosides

scientific article published on June 1998

Activation of A(3) adenosine receptor induces calcium entry and chloride secretion in A(6) cells.

scientific article

Activation of A(3)adenosine receptor protects against doxorubicin-induced cardiotoxicity

scientific article published in June 2001

Activation of Phosphoinositide Breakdown and Elevation of Intracellular Calcium in a Rat RBL-2H3 Mast Cell Line by Adenosine Analogs: Involvement of A(3)-Adenosine Receptors?

scientific article

Activation of adenosine A2A or A2B receptors causes hypothermia in mice

scientific article published on 13 March 2018

Activation of basal forebrain purinergic P2 receptors promotes wakefulness in mice

scientific article published on 16 July 2018

Activation of distinct P2Y receptor subtypes stimulates insulin secretion in MIN6 mouse pancreatic beta cells.

scientific article

Activation of neuronal adenosine A1 receptors causes hypothermia through central and peripheral mechanisms

scientific article published on 16 December 2020

Activation of the A2A adenosine receptor inhibits nitric oxide production in glial cells ⬇️

scientific article published on June 12, 1998

Activation of the A3 adenosine receptor affects cell cycle progression and cell growth

scientific article

Activation of the P2Y1 receptor induces apoptosis and inhibits proliferation of prostate cancer cells.

scientific article

Activity of Novel Adenine Nucleotide Derivatives as Agonists and Antagonists at Recombinant Rat P2X Receptors

scientific article

Acyclic analogues of adenosine bisphosphates as P2Y receptor antagonists: phosphate substitution leads to multiple pathways of inhibition of platelet aggregation.

scientific article published on December 2002

Acyclic analogues of deoxyadenosine 3',5'-bisphosphates as P2Y(1) receptor antagonists

scientific article published on 01 February 2000

Acyclic and cyclopropyl analogues of adenosine bisphosphate antagonists of the P2Y1 receptor: structure-activity relationships and receptor docking

scientific article published in September 2001

Adenine nucleotide analogues locked in a Northern methanocarba conformation: enhanced stability and potency as P2Y(1) receptor agonists

scientific article published on May 2002

Adenine nucleotide control of coronary blood flow during exercise ⬇️

scientific article published on September 17, 2010

Adenosine A(2A) receptor dynamics studied with the novel fluorescent agonist Alexa488-APEC.

scientific article published on 04 July 2008

Adenosine A1-A2A Receptor-Receptor Interaction: Contribution to Guanosine-Mediated Effects

scientific article published on 13 December 2019

Adenosine A3 receptor agonists protect HL-60 and U-937 cells from apoptosis induced by A3 antagonists

scientific article published on March 1997

Adenosine A3 receptor stimulation and cerebral ischemia

scientific article

Adenosine A3 receptors: novel ligands and paradoxical effects ⬇️

scientific article published on May 1, 1998

Adenosine Receptors: The Contributions by John W. Daly.

scientific article

Adenosine protects against angiotensin II-induced apoptosis in rat cardiocyte cultures

scientific article

Adenosine receptors as therapeutic targets

scientific article

Adenosine-induced cell death: evidence for receptor-mediated signalling.

scientific article published on June 1999

Adenosine: a prototherapeutic concept in neurodegeneration.

scientific article

Affinity chromatography of the bovine cerebral cortex A1 adenosine receptor

scientific article published on November 1989

Agonist-bound structure of the human P2Y12 receptor

scientific article

Allosteric Coupling of Drug Binding and Intracellular Signaling in the A2A Adenosine Receptor

scientific article published on 27 December 2017

Allosteric modulation and functional selectivity of G protein-coupled receptors.

scientific article published on January 2013

Allosteric modulation of purine and pyrimidine receptors

scientific article

Allosteric modulation of the adenosine family of receptors

scientific article

Amphiphilic pyridinium salts block TNF alpha/NF kappa B signaling and constitutive hypersecretion of interleukin-8 (IL-8) from cystic fibrosis lung epithelial cells

scientific article published in August 2005

Angiotensin II-induced apoptosis in rat cardiomyocyte culture: a possible role of AT1 and AT2 receptors.

scientific article

Antiaggregatory activity in human platelets of potent antagonists of the P2Y 1 receptor.

scientific article

Apoptosis by 2-chloro-2'-deoxy-adenosine and 2-chloro-adenosine in human peripheral blood mononuclear cells.

scientific article

Apparent heterogeneity of cardiac A1 adenosine receptors as revealed by radioligand binding experiments on N-ethylmaleimide-treated membranes

scientific article published in December 1991

Application of the functionalized congener approach to dendrimer-based signaling agents acting through A(2A) adenosine receptors.

scientific article published on 04 July 2008

Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.

scientific article

Assessment of biased agonism at the A3 adenosine receptor using β-arrestin and miniGαi recruitment assays

scientific article published on 26 March 2020

Attenuation of apoptosis in vitro and ischemia/reperfusion injury in vivo in mouse skeletal muscle by P2Y6 receptor activation

scientific article

Author Correction: Salvianolic acids from antithrombotic Traditional Chinese Medicine Danshen are antagonists of human P2Y and P2Y receptors

scientific article published in Scientific Reports

Autoradiographic localization of adenosine A1 receptors in rat brain using [3H]XCC, a functionalized congener of 1,3-dipropylxanthine

scientific article published in October 1987

Autoradiographic localization of mouse brain adenosine receptors with an antagonist ([3H]xanthine amine congener) ligand probe.

scientific article

A₃ adenosine receptor allosteric modulator induces an anti-inflammatory effect: in vivo studies and molecular mechanism of action

scientific article

Barrier qualities of the mouse eye to topically applied drugs.

scientific article

Bitopic fluorescent antagonists of the A2A adenosine receptor based on pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine functionalized congeners

scientific article

Breakthrough in GPCR Crystallography and Its Impact on Computer-Aided Drug Design

scientific article published in January 2018

CF102 an A3 adenosine receptor agonist mediates anti‐tumor and anti‐inflammatory effects in the liver ⬇️

scientific article published on September 1, 2011

Caged agonist of P2Y1 and P2Y12 receptors for light-directed facilitation of platelet aggregation.

scientific article published on 4 December 2007

Cardioprotective effects of adenosine A1 and A3 receptor activation during hypoxia in isolated rat cardiac myocytes

scientific article published on January 2001

Characterization by flow cytometry of fluorescent, selective agonist probes of the A(3) adenosine receptor.

scientific article published on 31 January 2013

Characterization of Polyamidoamino (PAMAM) Dendrimers Using In-Line Reversed Phase LC Electrospray Ionization Mass Spectrometry

scientific article published on 7 December 2015

Characterization of adenosine receptors in intact cultured heart cells

scientific article published on August 1994

Characterization of the UDP-glucose receptor (re-named here the P2Y14 receptor) adds diversity to the P2Y receptor family

scientific article (publication date: February 2003)

Characterization of “Mini-Nucleotides” as P2X Receptor Agonists in Rat Cardiomyocyte Cultures. An Integrated Synthetic, Biochemical, and Theoretical Study

article

Chiral resolution and stereospecificity of 6-phenyl-4-phenylethynyl- 1,4-dihydropyridines as selective A(3) adenosine receptor antagonists

scientific article published on August 1999

Chronic NMDA receptor stimulation: therapeutic implications of its effect on adenosine A1 receptors

scientific article published on September 1995

Chronic adenosine A1 receptor agonist and antagonist: effect on receptor density and N-methyl-D-aspartate induced seizures in mice

scientific article published on February 1994

Chronic administration of adenosine A3 receptor agonist and cerebral ischemia: neuronal and glial effects

scientific article

Chronic administration of selective adenosine A1 receptor agonist or antagonist in cerebral ischemia

scientific article published on April 1994

Click modification in the N6 region of A3 adenosine receptor-selective carbocyclic nucleosides for dendrimeric tethering that preserves pharmacophore recognition.

scientific article published on 11 January 2012

Comparative molecular field analysis of selective A3 adenosine receptor agonists

scientific article published on October 1995

Comparison of three GPCR structural templates for modeling of the P2Y12 nucleotide receptor ⬇️

scientific article published on April 3, 2011

Competitive and selective antagonism of P2Y1 receptors by N6-methyl 2'-deoxyadenosine 3',5'-bisphosphate

scientific article published on May 1998

Computational prediction of homodimerization of the A3 adenosine receptor.

scientific article published on 24 March 2006

Computational studies to predict or explain G protein coupled receptor polypharmacology

scientific article

Conformational changes involved in G-protein-coupled-receptor activation

scientific article

Conjugable A3 adenosine receptor antagonists for the development of functionalized ligands and their use in fluorescent probes

scientific article published on 22 November 2019

Controlling murine and rat chronic pain through A3 adenosine receptor activation

scientific article published on 17 February 2012

Conversion of A3 adenosine receptor agonists into selective antagonists by modification of the 5'-ribofuran-uronamide moiety

scientific article

Coordinated adenine nucleotide phosphohydrolysis and nucleoside signaling in posthypoxic endothelium: role of ectonucleotidases and adenosine A2B receptors

scientific article

Coronary artery reperfusion: The ADP receptor P2Y(1) mediates early reactive hyperemia in vivo in pigs

scientific article published on December 2004

Correction to Accelerating the Throughput of Affinity Mass Spectrometry-Based Ligand Screening toward a G Protein-Coupled Receptor

scientific article published on 03 March 2020

CysLT1 leukotriene receptor antagonists inhibit the effects of nucleotides acting at P2Y receptors

scientific article

D-4'-thioadenosine derivatives as highly potent and selective agonists at the human A3 adenosine receptor

scientific article

Deficiency of adenosine deaminase 2 triggers adenosine-mediated NETosis and TNF production in patients with DADA2

scientific article published on 23 April 2019

Defining the nucleotide binding sites of P2Y receptors using rhodopsin-based homology modeling

scientific article published on 01 July 2006

Demystifying P2Y1 Receptor Ligand Recognition through Docking and Molecular Dynamics Analyses

scientific article

Deoxyadenosine bisphosphate derivatives as potent antagonists at P2Y1 receptors

scientific article published on 01 January 1998

Derivatives of the triazoloquinazoline adenosine antagonist (CGS 15943) having high potency at the human A2B and A3 receptor subtypes.

scientific article published in July 1998

Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype

scientific article published on October 1996

Design and in Vivo Characterization of A1 Adenosine Receptor Agonists in the Native Ribose and Conformationally Constrained (N)-Methanocarba Series

scientific article published on 03 January 2019

Design and in vivo activity of A3 adenosine receptor agonist prodrugs

scientific article published on 27 July 2020

Design and synthesis of 3'-ureidoadenosine-5'-uronamides: effects of the 3'-ureido group on binding to the A3 adenosine receptor

scientific article published in October 2004

Design and synthesis of A3 adenosine receptor ligands, 2'-fluoro analogues of Cl-IB-MECA.

scientific article published on May 2003

Design and synthesis of A3 adenosine receptor ligands, 3'-fluoro analogues of Cl-IB-MECA.

scientific article published on May 2003

Design and synthesis of N(6)-substituted-4'-thioadenosine-5'-uronamides as potent and selective human A(3) adenosine receptor agonists

scientific article

Design and synthesis of new bicyclic diketopiperazines as scaffolds for receptor probes of structurally diverse functionality.

scientific article

Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists.

scientific article published on 4 April 2008

Design, synthesis and binding affinity of 3'-fluoro analogues of Cl-IB-MECA as adenosine A3 receptor ligands

scientific article published on March 2003

Design, synthesis, and anti-tumor activity of 4'-thionucleosides as potent and selective agonists at the human A3 adenosine receptor

scientific article published on January 2007

Design, synthesis, and biological activity of N6-substituted-4'-thioadenosines at the human A3 adenosine receptor

scientific article published on 05 April 2006

Design, synthesis, pharmacological characterization of a fluorescent agonist of the P2Y₁₄ receptor

scientific article

Development of selective agonists and antagonists of P2Y receptors

scientific article

Development of selective high affinity antagonists, agonists, and radioligands for the P2Y1 receptor.

scientific article

Dexamethasone enhances ATP-induced inflammatory responses in endothelial cells

scientific article

Differential allosteric modulation by amiloride analogues of agonist and antagonist binding at A(1) and A(3) adenosine receptors

scientific article

Differential effects of flavonoids on testosterone-metabolizing cytochrome P450s

scientific article published on 01 January 1997

Digitoxin mimics gene therapy with CFTR and suppresses hypersecretion of IL-8 from cystic fibrosis lung epithelial cells

scientific article

Diisothiocyanate derivatives as potent, insurmountable antagonists of P2Y6 nucleotide receptors.

scientific article

Direct activation of cystic fibrosis transmembrane conductance regulator channels by 8-cyclopentyl-1,3-dipropylxanthine (CPX) and 1,3-diallyl-8-cyclohexylxanthine (DAX).

scientific article

Discovery and Structure-Activity Relationships of Novel Template, Truncated 1'-Homologated Adenosine Derivatives as Pure Dual PPARγ/δ Modulators

scientific article published on 16 December 2020

Discovery of New Human A(2A) Adenosine Receptor Agonists: Design, Synthesis, and Binding Mode of Truncated 2-Hexynyl-4'-thioadenosine.

scientific article

Discovery of a new nucleoside template for human A3 adenosine receptor ligands: D-4'-thioadenosine derivatives without 4'-hydroxymethyl group as highly potent and selective antagonists

scientific article published on 08 June 2007

Distinct Signaling Patterns of Allosteric Antagonism at the P2Y1 Receptor

scientific article

Distinct structural changes in a G protein-coupled receptor caused by different classes of agonist ligands

scientific article

Dopamine D(2) receptor-mediated modulation of adenosine A(2A) receptor agonist binding within the A(2A)R/D(2)R oligomer framework.

scientific article published on 23 April 2013

Effect of adenosine on Na+ and Cl- currents in A6 monolayers. Receptor localization and messenger involvement

scientific article published on June 1996

Effects of N6-cyclopentyl adenosine and 8-cyclopentyl-1,3-dipropylxanthine on N-methyl-D-aspartate induced seizures in mice

scientific article published on November 1993

Effects of chronic administration of adenosine A1 receptor agonist and antagonist on spatial learning and memory

scientific article published on November 1993

Effects of the allosteric modulator SCH-202676 on adenosine and P2Y receptors

scientific article

Electrochemical detection of biogenic amines following acylation by N-hydroxysuccinimide esters.

scientific article published in September 1985

Emerging adenosine receptor agonists

scientific article

Emerging adenosine receptor agonists – an update ⬇️

scientific article published on December 7, 2011

Endogenous adenosine A3 receptor activation selectively alleviates persistent pain states

scientific article

Engagement of the GABA to KCC2 signaling pathway contributes to the analgesic effects of A3AR agonists in neuropathic pain

scientific article

Enhanced A3 adenosine receptor selectivity of multivalent nucleoside-dendrimer conjugates.

scientific article published on 23 October 2008

Enhancement of glucose uptake in mouse skeletal muscle cells and adipocytes by P2Y6 receptor agonists

scientific article

Evaluation of homology modeling of G-protein-coupled receptors in light of the A(2A) adenosine receptor crystallographic structure.

scientific article

Evaluation of molecular modeling of agonist binding in light of the crystallographic structure of an agonist-bound A₂A adenosine receptor

scientific article published on 12 December 2011

Evidence for the Recognition of Non-Nucleotide Antagonists Within the Transmembrane Domains of the Human P2Y(1) Receptor

scientific article

Exploration of Alternative Scaffolds for P2Y14 Receptor Antagonists Containing a Biaryl Core

scientific article published on 06 August 2020

Exploring a 2-naphthoic acid template for the structure-based design of P2Y14 receptor antagonist molecular probes

scientific article

Exploring distal regions of the A3 adenosine receptor binding site: sterically constrained N6-(2-phenylethyl)adenosine derivatives as potent ligands.

scientific article

Exploring human adenosine A3 receptor complementarity and activity for adenosine analogues modified in the ribose and purine moiety

scientific article

Exploring the Role of N6-Substituents in Potent Dual Acting 5'-C-Ethyltetrazolyladenosine Derivatives: Synthesis, Binding, Functional Assays, and Antinociceptive Effects in Mice ∇.

scientific article published on 27 April 2017

Extended N(6) substitution of rigid C2-arylethynyl nucleosides for exploring the role of extracellular loops in ligand recognition at the A3 adenosine receptor.

scientific article

Extracellular adenine nucleotides regulate Na+/H+ exchanger NHE3 activity in A6-NHE3 transfectants by a cAMP/PKA-dependent mechanism.

scientific article published on August 2002

Extracellular nucleotides induce vasodilatation in human arteries via prostaglandins, nitric oxide and endothelium‐derived hyperpolarising factor ⬇️

scientific article published on April 1, 2003

Extrinsic Tryptophans as NMR Probes of Allosteric Coupling in Membrane Proteins: Application to the A2A Adenosine Receptor

scientific article published on 20 June 2018

Farnesyl pyrophosphate is an endogenous antagonist to ADP-stimulated P2Y₁₂ receptor-mediated platelet aggregation.

scientific article published on 25 May 2012

Flavonoid Derivatives as Adenosine Receptor Antagonists: A Comparison of the Hypothetical Receptor Binding Site Based on a Comparative Molecular Field Analysis Model

article

Flexible modulation of agonist efficacy at the human A3 adenosine receptor by the imidazoquinoline allosteric enhancer LUF6000

scientific article

Fluorescent ligands for adenosine receptors

scientific article published on 5 November 2012

Fluorosulfonyl- and bis-(beta-chloroethyl)amino-phenylamino functionalized pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine derivatives: irreversible antagonists at the human A3 adenosine receptor and molecular modeling studies

scientific article

Fragment optimization for GPCRs by molecular dynamics free energy calculations: Probing druggable subpockets of the A 2A adenosine receptor binding site

scientific article

Functionalized congeners of A3 adenosine receptor-selective nucleosides containing a bicyclo[3.1.0]hexane ring system.

scientific article

Functionalized congeners of P2Y1 receptor antagonists: 2-alkynyl (N)-methanocarba 2'-deoxyadenosine 3',5'-bisphosphate analogues and conjugation to a polyamidoamine (PAMAM) dendrimer carrier

scientific article

Functionalized congeners of tyrosine-based P2X(7) receptor antagonists: probing multiple sites for linking and dimerization

scientific article published on September 2002

Functionally biased modulation of A(3) adenosine receptor agonist efficacy and potency by imidazoquinolinamine allosteric enhancers

scientific article

G protein-coupled adenosine (P1) and P2Y receptors: ligand design and receptor interactions ⬇️

scientific article published on February 29, 2012

GPCR ligand dendrimer (GLiDe) conjugates: adenosine receptor interactions of a series of multivalent xanthine antagonists

scientific article

GPCR ligand–dendrimer (GLiDe) conjugates: future smart drugs? ⬇️

scientific article published on October 18, 2010

Heteromultimeric P2X(1/2) receptors show a novel sensitivity to extracellular pH

scientific article published on February 2002

Highly selective A3 adenosine receptor agonists relieve chronic neuropathic pain

scientific article

History of Chemistry in the National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK).

scientific article

Human P2Y(14) receptor agonists: truncation of the hexose moiety of uridine-5'-diphosphoglucose and its replacement with alkyl and aryl groups

scientific article

Human P2Y(6) receptor: molecular modeling leads to the rational design of a novel agonist based on a unique conformational preference.

scientific article published on December 2005

Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites.

scientific article

Hypothermia in mouse is caused by adenosine A1 and A3 receptor agonists and AMP via three distinct mechanisms

scientific article published on 30 November 2016

Identification by site-directed mutagenesis of residues involved in ligand recognition and activation of the human A3 adenosine receptor

scientific article

Identification of A3 adenosine receptor agonists as novel non-narcotic analgesics.

scientific article published on 25 January 2016

Identification of Essential Residues Involved in the Allosteric Modulation of the Human A3Adenosine Receptor ⬇️

scientific article published on May 1, 2003

Identification of a New Heterocyclic Scaffold for Inhibitors of the Polo-Box Domain of Polo-like Kinase 1

scientific article published on 11 November 2020

Identification of a new dysfunctional platelet P2Y12 receptor variant associated with bleeding diathesis

scientific article

Identification of an agonist-induced conformational change occurring adjacent to the ligand-binding pocket of the M(3) muscarinic acetylcholine receptor

scientific article published on 10 August 2005

Imidazo[2,1-i]purin-5-ones and related tricyclic water-soluble purine derivatives: potent A(2A)- and A(3)-adenosine receptor antagonists

scientific article published on August 2002

Improvement of cold tolerance by selective A1 adenosine receptor antagonists in rats

scientific article published on September 1990

In vivo phenotypic screening for treating chronic neuropathic pain: modification of C2-arylethynyl group of conformationally constrained A3 adenosine receptor agonists

scientific article

Increased Signaling via Adenosine A1 Receptors, Sleep Deprivation, Imipramine, and Ketamine Inhibit Depressive-like Behavior via Induction of Homer1a

scientific article

Induction of apoptosis in HL-60 human promyelocytic leukemia cells by adenosine A(3) receptor agonists.

scientific article

Induction of apoptosis in cardiac myocytes by an A3 adenosine receptor agonist

scientific article published on September 1998

Induction of novel agonist selectivity for the ADP-activated P2Y1 receptor versus the ADP-activated P2Y12 and P2Y13 receptors by conformational constraint of an ADP analog.

scientific article

Inherited dysfunctional platelet P2Y12 receptor mutations associated with bleeding disorders.

scientific article

Inhibition of Ecto-Apyrase and Ecto-ATPase by Pyridoxal Phosphate-Related Compounds

scientific article published on November 2000

Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: selectivity for A3 receptors

scientific article published on July 1996

Interactions of flavones and other phytochemicals with adenosine receptors

scientific article (publication date: 2002)

Interactions of flavonoids and other phytochemicals with adenosine receptors

scientific article published on February 1996

International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and classification of adenosine receptors--an update

scientific article

International Union of Pharmacology LVIII: update on the P2Y G protein-coupled nucleotide receptors: from molecular mechanisms and pathophysiology to therapy

scientific article

Involvement of UTP in protection of cardiomyocytes from hypoxic stress.

scientific article

Involvement of uracil nucleotides in protection of cardiomyocytes from hypoxic stress

scientific article published on April 2005

John Daly Lecture: Structure-guided Drug Design for Adenosine and P2Y Receptors

scientific article published on 16 October 2014

John W. Daly - An Appreciation

scientific article published in January 2009

Lack of adipocyte purinergic P2Y6 receptor greatly improves whole body glucose homeostasis

scientific article published on 16 November 2020

Ligand and structure-based methodologies for the prediction of the activity of G protein-coupled receptor ligands

scientific article published on 16 May 2008

Ligand-specific changes in M3 muscarinic acetylcholine receptor structure detected by a disulfide scanning strategy

scientific article

Lighting up G protein-coupled purinergic receptors with engineered fluorescent ligands.

scientific article

Limits of ligand selectivity from docking to models: in silico screening for A(1) adenosine receptor antagonists

scientific article

Liquid chromatographic assay for cerebrospinal fluid normetanephrine.

scientific article published in April 1987

Liquid chromatographic assay for cerebrospinal fluid serotonin.

scientific article published in February 1986

Locomotor activity in mice during chronic treatment with caffeine and withdrawal.

scientific article published on January 1993

MRS2500 [2-iodo-N6-methyl-(N)-methanocarba-2'-deoxyadenosine-3',5'-bisphosphate], a potent, selective, and stable antagonist of the platelet P2Y1 receptor with strong antithrombotic activity in mice

scientific article published on 19 October 2005

Medicinal chemistry of adenosine, P2Y and P2X receptors

scientific article published on 11 December 2015

Medicinal chemistry of the A3 adenosine receptor: agonists, antagonists, and receptor engineering

scientific article

Metabolic mapping of A3 adenosine receptor agonist MRS5980

scientific article

Methanocarba analogues of purine nucleosides as potent and selective adenosine receptor agonists.

scientific article

Methanocarba modification of uracil and adenine nucleotides: high potency of Northern ring conformation at P2Y1, P2Y2, P2Y4, and P2Y11 but not P2Y6 receptors

scientific article

Methanocarba ring as a ribose modification in ligands of G protein-coupled purine and pyrimidine receptors: synthetic approaches.

scientific article published in December 2013

Modeling ligand recognition at the P2Y12 receptor in light of X-ray structural information

scientific article

Modulation of G protein-coupled adenosine receptors by strategically functionalized agonists and antagonists immobilized on gold nanoparticles.

scientific article published on 20 November 2012

Modulation of adenosine receptor affinity and intrinsic efficacy in adenine nucleosides substituted at the 2-position

scientific article

Molecular Architecture of G Protein-Coupled Receptors.

scientific article

Molecular Modeling and Reengineering of A3 Adenosine Receptors

article

Molecular determinants of A2AR-D2R allosterism: role of the intracellular loop 3 of the D2R.

scientific article

Molecular docking screening using agonist-bound GPCR structures: probing the A2A adenosine receptor.

scientific article published on 13 February 2015

Molecular modeling as a tool to investigate molecular recognition in P2Y receptors

scientific article

Molecular modeling of a PAMAM-CGS21680 dendrimer bound to an A2A adenosine receptor homodimer.

scientific article published on 28 June 2008

Molecular modeling of adenosine receptors. The ligand binding site on the rat adenosine A2A receptor

scientific article published on 01 June 1994

Molecular modeling of the human P2Y14 receptor: A template for structure-based design of selective agonist ligands.

scientific article

Molecular modeling of the human P2Y2 receptor and design of a selective agonist, 2'-amino-2'-deoxy-2-thiouridine 5'-triphosphate

scientific article

Molecular probes for the A2A adenosine receptor based on a pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine scaffold

scientific article

Molecular recognition at adenine nucleotide (P2) receptors in platelets.

scientific article published on April 2005

Molecular recognition at purine and pyrimidine nucleotide (P2) receptors.

scientific article published in January 2004

Molecular recognition in the P2Y(14) receptor: Probing the structurally permissive terminal sugar moiety of uridine-5'-diphosphoglucose

scientific article published on 15 May 2009

Molecular structure of P2Y receptors: mutagenesis, modeling, and chemical probes ⬇️

scientific article published on September 12, 2012

Mutagenesis Reveals Structure−Activity Parallels between Human A2AAdenosine Receptors and Biogenic Amine G Protein-Coupled Receptors ⬇️

scientific article published on August 1, 1997

N6-Substituted 5'-N-Methylcarbamoyl-4'-selenoadenosines as Potent and Selective A3 Adenosine Receptor Agonists with Unusual Sugar Puckering and Nucleobase Orientation

scientific article published on 5 April 2017

N6-Substituted adenosine derivatives: selectivity, efficacy, and species differences at A3 adenosine receptors ⬇️

scientific article published on May 15, 2003

N6-functionalized congeners of adenosine with high potency at A2-adenosine receptors: potential ligands for affinity chromatography.

scientific article

N6-substituted D-4'-thioadenosine-5'-methyluronamides: potent and selective agonists at the human A3 adenosine receptor

scientific article published on August 2003

NEW BASE-ALTERED ADENOSINE ANALOGUES: SYNTHESIS AND AFFINITY AT ADENOSINE A1 and A2A RECEPTORS.

scientific article

Neoceptors: reengineering GPCRs to recognize tailored ligands

scientific article published on 5 February 2007

New 8-substituted xanthiene derivatives as potent bronchodilators

scientific article published on 21 October 2005

New Insights for Drug Design from the X-Ray Crystallographic Structures of G-Protein-Coupled Receptors ⬇️

scientific article published on June 13, 2012

New high-performance liquid chromatographic procedure for the detection and quantification of beta-phenylethylamine

scientific article published on 01 March 1987

New paradigms in GPCR drug discovery.

scientific article published on 08 August 2015

Non-xanthine heterocycles: activity as antagonists of A1- and A2-adenosine receptors

scientific article

Northern Ring Conformation of Methanocarba-Adenosine 5'-Triphosphate Required for Activation of P2X Receptors.

scientific article

Novel 2- and 4-substituted 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric modulators of the A3 adenosine receptor

scientific article published on April 2009

Novel fluorescent antagonist as a molecular probe in A(3) adenosine receptor binding assays using flow cytometry

scientific article published in March 2012

Novel protective role of endogenous cardiac myocyte P2X4 receptors in heart failure

scientific article

Nucleoside conjugates of quantum dots for characterization of G protein-coupled receptors: strategies for immobilizing A2A adenosine receptor agonists

scientific article

Nucleoside modification and concerted mutagenesis of the human A3 adenosine receptor to probe interactions between the 2-position of adenosine analogs and Gln167 in the second extracellular loop.

scientific article published on January 2005

Nucleoside-derived antagonists to A3 adenosine receptors lower mouse intraocular pressure and act across species.

scientific article published on 28 October 2009

Nucleotide analogues containing 2-oxa-bicyclo[2.2.1]heptane and l-alpha-threofuranosyl ring systems: interactions with P2Y receptors ⬇️

scientific article

Nucleotides Acting at P2Y Receptors: Connecting Structure and Function

scientific article published on 2 April 2015

Ocular Purine Receptors as Drug Targets in the Eye.

scientific article published on 30 August 2016

On the selectivity of the Gαq inhibitor UBO-QIC: A comparison with the Gαi inhibitor pertussis toxin.

scientific article published on 5 March 2016

Optimization of adenosine 5'-carboxamide derivatives as adenosine receptor agonists using structure-based ligand design and fragment screening

scientific article

Orthogonal activation of the reengineered A3 adenosine receptor (neoceptor) using tailored nucleoside agonists

scientific article

P2-Purinoceptors: Advances and therapeutic opportunities

scientific article published on 01 October 1995

P2X purinergic receptor-mediated ionic current in cardiac myocytes of calsequestrin model of cardiomyopathy: implications for the treatment of heart failure

scientific article published on 13 October 2006

P2X4 receptor-eNOS signaling pathway in cardiac myocytes as a novel protective mechanism in heart failure.

scientific article

P2Y(13) receptor is responsible for ADP-mediated degranulation in RBL-2H3 rat mast cells.

scientific article

P2Y1 antagonists: combining receptor-based modeling and QSAR for a quantitative prediction of the biological activity based on consensus scoring

scientific article published on 12 June 2007

P2Y14 Receptor Antagonists Reverse Chronic Neuropathic Pain in a Mouse Model

scientific article published on 30 April 2020

P2Y2 receptor agonist with enhanced stability protects the heart from ischemic damage in vitro and in vivo

scientific article published on 05 July 2013

P2Y6 nucleotide receptor activates PKC to protect 1321N1 astrocytoma cells against tumor necrosis factor-induced apoptosis ⬇️

scientific article

PEGylated dendritic unimolecular micelles as versatile carriers for ligands of G protein-coupled receptors

scientific article published on 28 September 2009

PHOTOLABILE A1-ADENOSINE RECEPTOR AGONISTS AS "CAGED" ELECTROPHYSIOLOGICAL PROBES

scientific article

Partial agonists for A(3) adenosine receptors.

scientific article published on January 2004

Penetration of adenosine antagonists into mouse brain as determined by ex vivo binding

scientific article published on February 1992

Peptide-Liganded G Protein-Coupled Receptors as Neurotherapeutics

scientific article published on 18 March 2020

Peripheral Adenosine A3 Receptor Activation Causes Regulated Hypothermia in Mice That Is Dependent on Central Histamine H1 Receptors.

scientific article

Pharmacochemistry of the platelet purinergic receptors.

scientific article

Pharmacological and therapeutic effects of A3 adenosine receptor agonists ⬇️

scientific article published on October 19, 2011

Pharmacological characterization of novel A3 adenosine receptor-selective antagonists ⬇️

scientific article published on September 1, 1997

Pharmacology of purine and pyrimidine receptors. Preface

scientific article published on 01 January 2011

Photomodulation of G protein-coupled adenosine receptors by a novel light-switchable ligand

scientific article

Physiology and effects of nucleosides in mice lacking all four adenosine receptors

scientific article published on 01 March 2019

Polyamidoamine (PAMAM) dendrimer conjugate specifically activates the A3 adenosine receptor to improve post-ischemic/reperfusion function in isolated mouse hearts

scientific article

Polypharmacology of N6-(3-Iodobenzyl)adenosine-5'-N-methyluronamide (IB-MECA) and Related A3 Adenosine Receptor Ligands: Peroxisome Proliferator Activated Receptor (PPAR) γ Partial Agonist and PPARδ Antagonist Activity Suggests Their Antidiabetic Po

scientific article published on 11 August 2017

Polypharmacology of conformationally locked methanocarba nucleosides

scientific article

Portraying G protein-coupled receptors with fluorescent ligands

scientific article

Positive inotropic effects by uridine triphosphate (UTP) and uridine diphosphate (UDP) via P2Y2 and P2Y6 receptors on cardiomyocytes and release of UTP in man during myocardial infarction

scientific article

Potent P2X7 Receptor Antagonists: Tyrosyl Derivatives Synthesized Using a Sequential Parallel Synthetic Approach

scientific article published on October 2001

Potent convulsant actions of the adenosine receptor antagonist, xanthine amine congener (XAC)

scientific article

Potential for developing purinergic drugs for gastrointestinal diseases

scientific article

Preclinical evaluation of the first adenosine A receptor partial agonist radioligand for positron emission tomography (PET) imaging

article

Predicted structures of agonist and antagonist bound complexes of adenosine A3 receptor

scientific article

Preface: special issue on medicinal chemistry of purines

scientific article published on March 2009

Presence of both A1 and A2a adenosine receptors in human cells and their interaction

scientific article published on March 1995

Probing Structure-Activity Relationship in β-Arrestin2 Recruitment of Diversely Substituted Adenosine Derivatives

article

Probing adenosine receptors using biotinylated purine derivatives.

scientific article

Probing biased/partial agonism at the G protein-coupled A(2B) adenosine receptor

scientific article

Probing distal regions of the A2B adenosine receptor by quantitative structure-activity relationship modeling of known and novel agonists.

scientific article published on 6 March 2008

Probing the binding site of the A1 adenosine receptor reengineered for orthogonal recognition by tailored nucleosides.

scientific article

Programmable nanoscaffolds that control ligand display to a G-protein-coupled receptor in membranes to allow dissection of multivalent effects.

scientific article

Progress in the pursuit of therapeutic adenosine receptor antagonists

scientific article

Pronounced conformational changes following agonist activation of the M(3) muscarinic acetylcholine receptor

scientific article published on 2 May 2005

Protection from myocardial ischemia/reperfusion injury by a positive allosteric modulator of the A₃ adenosine receptor

scientific article published on 19 October 2011

Protective roles of adenosine A1, A2A, and A3 receptors in skeletal muscle ischemia and reperfusion injury

scientific article published on 5 October 2007

Purification and characterization of bovine cerebral cortex A1 adenosine receptor.

scientific article

Purification and recognition of recombinant mouse P2X1 receptors expressed in a baculovirus system ⬇️

scientific article published on September 1, 2000

Purine (N)-Methanocarba Nucleoside Derivatives Lacking an Exocyclic Amine as Selective A3 Adenosine Receptor Agonists.

scientific article

Purine derivatives as ligands for A3 adenosine receptors.

scientific article

Purinergic Signaling in Mast Cell Degranulation and Asthma

scientific article published on 22 December 2017

Purinergic drug targets for gastrointestinal disorders.

scientific article published on 14 November 2017

Pyran Template Approach to the Design of Novel A3 Adenosine Receptor Antagonists

scientific article (publication date: December 1999)

Pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidines to develop functionalized ligands to target adenosine receptors: fluorescent ligands as an example

scientific article published on 18 February 2019

Pyrimidine Nucleotides Containing a (S)-Methanocarba Ring as P2Y6 Receptor Agonists.

scientific article published on 6 September 2017

Pyrimidine nucleotides with 4-alkyloxyimino and terminal tetraphosphate δ-ester modifications as selective agonists of the P2Y(4) receptor

scientific article

Quantification of Gi-mediated inhibition of adenylyl cyclase activity reveals that UDP is a potent agonist of the human P2Y14 receptor

scientific article published on 16 September 2009

Quantification of recombinant and platelet P2Y(1) receptors utilizing a [(125)I]-labeled high-affinity antagonist 2-iodo-N(6)-methyl-(N)-methanocarba-2'-deoxyadenosine-3',5'-bisphosphate ([(125)I]MRS2500)

scientific article published on 4 June 2010

Quinazolines as adenosine receptor antagonists: SAR and selectivity for A2B receptors.

scientific article

Random mutagenesis of the M3 muscarinic acetylcholine receptor expressed in yeast: identification of second-site mutations that restore function to a coupling-deficient mutant M3 receptor.

scientific article

Rapid identification of functionally critical amino acids in a G protein-coupled receptor.

scientific article

Rapid synthesis of alkoxyamine hydrochloride derivatives from alkyl bromide and N,N'-di-tert-butoxycarbonylhydroxylamine ((Boc)2NOH).

scientific article

Rational design of sulfonated A3 adenosine receptor-selective nucleosides as pharmacological tools to study chronic neuropathic pain

scientific article published on 03 July 2013

Recent developments in adenosine receptor ligands and their potential as novel drugs ⬇️

scientific article published on December 23, 2010

Regio- and stereoselective synthesis of truncated 3′-aminocarbanucleosides and their binding affinity at the A3 adenosine receptor ⬇️

scientific article published on August 23, 2011

Regulation of A1 adenosine receptors by amiodarone and electrical stimulation in rat myocardial cells in vitro

scientific article published on September 1997

Regulation of death and survival in astrocytes by ADP activating P2Y1 and P2Y12 receptors.

scientific article

Remote control of movement disorders using a photoactive adenosine A2A receptor antagonist

scientific article published on 31 May 2018

Renal intercalated cells sense and mediate inflammation via the P2Y14 receptor

scientific article

Reply to: 'the discovery of a new class of synaptic transmitters in smooth muscle fifty years ago and amelioration of coronary artery thrombosis'.

scientific article published on 17 April 2013

Rhodopsin and the others: a historical perspective on structural studies of G protein-coupled receptors

scientific article

Riboflavin: Inhibitory Effects on Receptors, G-Proteins, and Adenylate Cyclase.

scientific article

Ribose modified nucleosides and nucleotides as ligands for purine receptors

scientific article

Rigid Adenine Nucleoside Derivatives as Novel Modulators of the Human Sodium Symporters for Dopamine and Norepinephrine.

scientific article published on 26 January 2016

Rigidified A3 Adenosine Receptor Agonists: 1-Deazaadenine Modification Maintains High in Vivo Efficacy

scientific article published on 20 May 2015

Role of the extracellular loops of G protein-coupled receptors in ligand recognition: a molecular modeling study of the human P2Y1 receptor.

scientific article published on March 1999

Roles of BCL-2 and caspase 3 in the adenosine A3 receptor-induced apoptosis

scientific article published on December 2001

Salvianolic acids from antithrombotic Traditional Chinese Medicine Danshen are antagonists of human P2Y1 and P2Y12 receptors.

scientific article

Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters

scientific article

Selective A(3) adenosine receptor antagonists derived from nucleosides containing a bicyclo[3.1.0]hexane ring system

scientific article published on 07 August 2008

Selective A(3) adenosine receptor antagonists: water-soluble 3, 5-diacyl-1,2,4-trialkylpyridinium salts and their oxidative generation from dihydropyridine precursors

scientific article

Selective allosteric enhancement of agonist binding and function at human A3 adenosine receptors by a series of imidazoquinoline derivatives

scientific article published on July 2002

Shift in purine/pyrimidine base recognition upon exchanging extracellular domains in P2Y 1/6 chimeric receptors.

scientific article

Signaling of the Human P2Y(1) Receptor Measured by a Yeast Growth Assay with Comparisons to Assays of Phospholipase C and Calcium Mobilization in 1321N1 Human Astrocytoma Cells

scientific article

Simultaneous determination of histamine and N tau-methylhistamine with high-performance liquid chromatography using electrochemical detection

scientific article published in January 1986

Site-directed mutagenesis of the human adenosine A2A receptor. Critical involvement of Glu13 in agonist recognition

scientific article published on August 1996

Site-directed mutagenesis studies of human A(2A) adenosine receptors: involvement of glu(13) and his(278) in ligand binding and sodium modulation

scientific article

Small molecule positive allosteric modulation of TRPV1 activation by vanilloids and acidic pH.

scientific article published on 17 October 2011

Solubilized rabbit striatal A2a-adenosine receptors: stability and antagonist binding

scientific article published on September 1993

South (S)- and North (N)-Methanocarba-7-Deazaadenosine Analogues as Inhibitors of Human Adenosine Kinase.

scientific article published on 13 July 2016

Species differences and mechanism of action of A3 adenosine receptor allosteric modulators

scientific article

Spinal neuroimmune activation is independent of T-cell infiltration and attenuated by A3 adenosine receptor agonists in a model of oxaliplatin-induced peripheral neuropathy

scientific article

Stereoselective synthesis of 1'-functionalized-4'-thionucleosides

scientific article published on January 2007

Stimulation of Xenopus P2Y1 receptor activates CFTR in A6 cells.

scientific article published on October 2004

Stimulation of the P2X7 receptor kills rat retinal ganglion cells in vivo.

scientific article

Structural Connection between Activation Microswitch and Allosteric Sodium Site in GPCR Signaling

scientific article published on 26 January 2018

Structural Probing and Molecular Modeling of the A₃ Adenosine Receptor: A Focus on Agonist Binding

scientific article

Structural determinants of A(3) adenosine receptor activation: nucleoside ligands at the agonist/antagonist boundary

scientific article published in September 2002

Structural determinants of efficacy at A3 adenosine receptors: modification of the ribose moiety.

scientific article

Structural probing of off-target G protein-coupled receptor activities within a series of adenosine/adenine congeners

scientific article (publication date: 2014)

Structural sweet spot for A1 adenosine receptor activation by truncated (N)-methanocarba nucleosides: receptor docking and potent anticonvulsant activity

scientific article

Structurally related nucleotides as selective agonists and antagonists at P2Y1 receptors

scientific article

Structure activity relationship of 2-arylalkynyl-adenine derivatives as human A3 adenosine receptor antagonists

scientific article published on 18 October 2018

Structure activity relationships for derivatives of adenosine‐5′‐triphosphate as agonists at P2 purinoceptors: Heterogeneity within P2x and P2y subtypes ⬇️

scientific article published on October 5, 2004

Structure of an agonist-bound human A2A adenosine receptor

scientific article

Structure of the human P2Y12 receptor in complex with an antithrombotic drug

scientific article

Structure-Activity Relationship of Purine and Pyrimidine Nucleotides as Ecto-5'-Nucleotidase (CD73) Inhibitors

scientific article published on 21 March 2019

Structure-Based Design of 3-(4-Aryl-1H-1,2,3-triazol-1-yl)-Biphenyl Derivatives as P2Y14 Receptor Antagonists.

scientific article

Structure-Based Design of Reactive Nucleosides for Site-Specific Modification of the A2A Adenosine Receptor

scientific article

Structure-Based Scaffold Repurposing for G Protein-Coupled Receptors: Transformation of Adenosine Derivatives into 5HT2B/5HT2C Serotonin Receptor Antagonists

scientific article

Structure-Based Screening of Uncharted Chemical Space for Atypical Adenosine Receptor Agonists.

scientific article

Structure-Guided Modification of Heterocyclic Antagonists of the P2Y14 Receptor

scientific article published on 16 May 2018

Structure-activity relationship of (N)-Methanocarba phosphonate analogues of 5'-AMP as cardioprotective agents acting through a cardiac P2X receptor.

scientific article

Structure-activity relationships and molecular modeling of 1,2,4-triazoles as adenosine receptor antagonists

scientific article published on 30 July 2012

Structure-activity relationships and molecular modeling of 3, 5-diacyl-2,4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists

scientific article

Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions.

scientific article

Structure-activity relationships of 1,4-dihydropyridines that act as enhancers of the vanilloid receptor 1 (TRPV1)

scientific article published on 26 August 2008

Structure-activity relationships of 2,N(6),5'-substituted adenosine derivatives with potent activity at the A2B adenosine receptor.

scientific article

Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-uronamides as highly potent and selective agonists at the human A3 adenosine receptor

scientific article published on January 2006

Structure-activity relationships of 4-(phenylethynyl)-6-phenyl-1,4-dihydropyridines as highly selective A3 adenosine receptor antagonists

scientific article published in August 1997

Structure-activity relationships of bisphosphate nucleotide derivatives as P2Y1 receptor antagonists and partial agonists.

scientific article published on May 1999

Structure-activity relationships of new 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric enhancers of the A3 adenosine receptor

scientific article published on June 2006

Structure-activity relationships of pyridoxal phosphate derivatives as potent and selective antagonists of P2X1 receptors

scientific article

Structure-activity relationships of thiazole and thiadiazole derivatives as potent and selective human adenosine A3 receptor antagonists

scientific article

Structure-activity relationships of truncated C2- or C8-substituted adenosine derivatives as dual acting A₂A and A₃ adenosine receptor ligands.

scientific article published on 28 December 2011

Structure-activity relationships of truncated D- and l-4'-thioadenosine derivatives as species-independent A3 adenosine receptor antagonists

scientific article published on 24 September 2008

Structure-based approaches to ligands for G-protein-coupled adenosine and P2Y receptors, from small molecules to nanoconjugates.

scientific article

Structure-based discovery of A2A adenosine receptor ligands

scientific article

Structure-guided design of A(3) adenosine receptor-selective nucleosides: combination of 2-arylethynyl and bicyclo[3.1.0]hexane substitutions.

scientific article

Survey of ribose ring pucker of signaling nucleosides and nucleotides

scientific article published on 28 August 2019

Synthesis and Binding Affinity of Homologated Adenosine Analogues as A3 Adenosine Receptor Ligands.

scientific article published on January 2011

Synthesis and P2Y receptor activity of nucleoside 5'-phosphonate derivatives

scientific article published on 14 April 2009

Synthesis and P2Y₂ receptor agonist activities of uridine 5'-phosphonate analogues

scientific article published on 15 February 2012

Synthesis and anti-renal fibrosis activity of conformationally locked truncated 2-hexynyl-N(6)-substituted-(N)-methanocarba-nucleosides as A3 adenosine receptor antagonists and partial agonists.

scientific article published on 05 February 2014

Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists

scientific article published on June 1996

Synthesis and biological activity of a new series of N6-arylcarbamoyl, 2-(Ar)alkynyl-N6-arylcarbamoyl, and N6-carboxamido derivatives of adenosine-5'-N-ethyluronamide as A1 and A3 adenosine receptor agonists

scientific article published on August 1998

Synthesis and biological evaluation of a new series of 1,2,4-triazolo[1,5-a]-1,3,5-triazines as human A(2A) adenosine receptor antagonists with improved water solubility

scientific article published on 7 January 2011

Synthesis and characterization of [76Br]-labeled high-affinity A3 adenosine receptor ligands for positron emission tomography

scientific article published on January 2009

Synthesis and evaluation of 1,2,4-triazolo[1,5-c]pyrimidine derivatives as A2A receptor-selective antagonists

scientific article

Synthesis and evaluation of N⁶-substituted apioadenosines as potential adenosine A₃ receptor modulators

scientific article

Synthesis and pharmacological characterization of [(125)I]MRS1898, a high-affinity, selective radioligand for the rat A(3) adenosine receptor.

scientific article published on 05 June 2008

Synthesis and pharmacological characterization of [(125)I]MRS5127, a high affinity, selective agonist radioligand for the A3 adenosine receptor

scientific article

Synthesis and pharmacological characterization of a new series of 5,7-disubstituted-[1,2,4]triazolo[1,5-a][1,3,5]triazine derivatives as adenosine receptor antagonists: A preliminary inspection of ligand-receptor recognition process

scientific article

Synthesis and potency of novel uracil nucleotides and derivatives as P2Y2 and P2Y6 receptor agonists

scientific article published on 9 May 2008

Synthesis and structure-activity relationship studies of tyrosine-based antagonists at the human P2X7 receptor

scientific article

Synthesis of 3'-acetamidoadenosine derivatives as potential A3 adenosine receptor agonists

scientific article published on April 2008

Synthesis of 3'-ureidoadenosine analogues and their binding affinity to the A3 adenosine receptor

scientific article

Synthesis of N6-substituted 3'-ureidoadenosine derivatives as highly potent agonists at the mutant A3 adenosine receptor

scientific article published on January 2007

Synthesis of enantiomerically pure (S)-methanocarbaribo uracil nucleoside derivatives for use as antiviral agents and P2Y receptor ligands.

scientific article published on 24 September 2008

Synthesis of ethyl (1S,2R,3S,4S,5S)-2,3-O-(isopropylidene)-4-hydroxy-bicyclo[3.1.0]hexane-carboxylate from L-ribose: a versatile chiral synthon for preparation of adenosine and P2 receptor ligands.

scientific article published in March 2008

Synthesis of hypermodified adenosine derivatives as selective adenosine A3 receptor ligands

scientific article published on 2 November 2005

Synthesis of novel apio carbocyclic nucleoside analogues as selective a(3) adenosine receptor agonists

scientific article published on June 2005

Synthesis of pyridoxal phosphate derivatives with antagonist activity at the P2Y13 receptor

scientific article

Synthesis using ring closure metathesis and effect on nucleoside transport of a (N)-methanocarba S-(4-nitrobenzyl)thioinosine derivative.

scientific article

Synthesis, Biological Activity, and Molecular Modeling of Ribose-Modified Deoxyadenosine Bisphosphate Analogues as P2Y1Receptor Ligands

article

Synthesis, CoMFA analysis, and receptor docking of 3,5-diacyl-2, 4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists

scientific article published on February 1999

Synthesis, biological properties, and molecular modeling investigation of the first potent, selective, and water-soluble human A(3) adenosine receptor antagonist

scientific article published on August 2002

Systematic investigation of polyamidoamine dendrimers surface-modified with poly(ethylene glycol) for drug delivery applications: synthesis, characterization, and evaluation of cytotoxicity.

scientific article

Techniques: Recent developments in computer-aided engineering of GPCR ligands using the human adenosine A3 receptor as an example

scientific article

Tetrahydrobenzothiophenone derivatives as a novel class of adenosine receptor antagonists

scientific article published in January 1996

The A3 adenosine receptor attenuates the calcium rise triggered by NMDA receptors in retinal ganglion cells

scientific article

The A3 adenosine receptor mediates cell spreading, reorganization of actin cytoskeleton, and distribution of Bcl-XL: studies in human astroglioma cells.

scientific article published in December 1997

The effects of adenosine A3 receptor stimulation on seizures in mice

scientific article published on February 1995

The recently deorphanized GPR80 (GPR99) proposed to be the P2Y15 receptor is not a genuine P2Y receptor

scientific article

The role of P2Y(14) and other P2Y receptors in degranulation of human LAD2 mast cells

scientific article published on 24 July 2012

The role of activated adenosine receptors in degranulation of human LAD2 mast cells.

scientific article

The role of amino acids in extracellular loops of the human P2Y1 receptor in surface expression and activation processes.

scientific article

The therapeutic effect of 2-cyclohexylthio-AMP in heart failure

scientific article published on June 2013

The utilization of a unified pharmacophore query in the discovery of new antagonists of the adenosine receptor family

scientific article published on January 2000

Thermostabilization and purification of the human dopamine transporter (hDAT) in an inhibitor and allosteric ligand bound conformation

scientific article published on 02 July 2018

Three-dimensional quantitative structure-activity relationship of nucleosides acting at the A3 adenosine receptor: analysis of binding and relative efficacy

scientific article published on 06 March 2007

Toward multivalent signaling across G protein-coupled receptors from poly(amidoamine) dendrimers

scientific article published on 5 January 2008

Translocation of arrestin induced by human A(3) adenosine receptor ligands in an engineered cell line: comparison with G protein-dependent pathways

scientific article

Treatment of dry eye syndrome with orally administered CF101: data from a phase 2 clinical trial

scientific article

Treatment of heart failure by a methanocarba derivative of adenosine monophosphate: implication for a role of cardiac purinergic P2X receptors.

scientific article

Tribute to Prof. Geoffrey Burnstock: transition of purinergicsignaling to drug discovery

scientific article published on 14 August 2020

Truncated (N)-Methanocarba Nucleosides as A(1) Adenosine Receptor Agonists and Partial Agonists: Overcoming Lack of a Recognition Element

scientific article

Truncated (N)-Methanocarba Nucleosides as Partial Agonists at Mouse and Human A3 Adenosine Receptors: Affinity Enhancement by N6-(2-Phenylethyl) Substitution

scientific article published on 09 April 2020

Truncated Nucleosides as A(3) Adenosine Receptor Ligands: Combined 2-Arylethynyl and Bicyclohexane Substitutions

scientific article

Tumor necrosis factor alpha-induced apoptosis in astrocytes is prevented by the activation of P2Y6, but not P2Y4 nucleotide receptors

scientific article

Two disparate ligand-binding sites in the human P2Y1 receptor

scientific article

UDP is a competitive antagonist at the human P2Y14 receptor

scientific article

UDP-glucose acting at P2Y14 receptors is a mediator of mast cell degranulation

scientific article

UDP-glucose promotes neutrophil recruitment in the lung

scientific article published on 15 July 2016

Uncovering caffeine's adenosine A2A receptor inverse agonism in experimental parkinsonism

scientific article

Update of P2X receptor properties and their pharmacology: IUPHAR Review 30

scientific article published on 30 October 2020

Update of P2Y Receptor Pharmacology: IUPHAR Review:27

scientific article published on 09 February 2020

Uridine-5'-triphosphate (UTP) reduces infarct size and improves rat heart function after myocardial infarct.

scientific article published on 30 August 2006

Virtual screening leads to the discovery of novel non-nucleotide P2Y₁ receptor antagonists.

scientific article

Visual methods for the nanomolar detection of electrophilic reagents

scientific article published on 01 November 1983

Xanthines as Adenosine Receptor Antagonists ⬇️

scientific article published on January 1, 2011

[3H]MRS 1754, a selective antagonist radioligand for A(2B) adenosine receptors

scientific article published on March 2001

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