List of works - Jose Brea

1,3-Dialkyl-8-(hetero)aryl-9-OH-9-deazaxanthines as potent A2B adenosine receptor antagonists: design, synthesis, structure-affinity and structure-selectivity relationships

scientific article

1,3-dialkyl-8-N-substituted benzyloxycarbonylamino-9-deazaxanthines as potent adenosine receptor ligands: Design, synthesis, structure-affinity and structure-selectivity relationships.

scientific article published on 5 April 2009

1-, 3- and 8-substituted-9-deazaxanthines as potent and selective antagonists at the human A2B adenosine receptor

scientific article

2-Aryladenine derivatives as a potent scaffold for A1, A3 and dual A1/A3 adenosine receptor antagonists: Synthesis and structure-activity relationships

scientific article published on 20 June 2019

2-Phenylquinazolinones as dual-activity tankyrase-kinase inhibitors

scientific article

3,4-Dihydropyrimidin-2(1<i>H</i>)-ones as Antagonists of the Human A<sub>2B</sub> Adenosine Receptor: Optimization, Structure-Activity Relationship Studies, and Enantiospecific Recognition

scientific article published on 29 December 2020

5-HT2 receptor binding, functional activity and selectivity in N-benzyltryptamines

scientific article published in PLoS ONE

A New Model of Sensorial Neuron-Like Cells for HTS of Novel Analgesics for Neuropathic Pain

scientific article published on 01 November 2018

A Positive Allosteric Modulator of the Serotonin 5-HT2C Receptor for Obesity

scientific article published on 8 November 2017

A Potential Nanomedicine Consisting of Heparin-Loaded Polysaccharide Nanocarriers for the Treatment of Asthma

scholarly article by Felipe A. Oyarzun-Ampuero et al published 23 November 2011 in Macromolecular Bioscience

A new chemical tool (C0036E08) supports the role of adenosine A(2B) receptors in mediating human mast cell activation

scientific article

A novel mechanism of neuroprotection: Blood glutamate grabber

scientific article published on 02 October 2015

Association of community-acquired pneumonia with antipsychotic drug use in elderly patients: a nested case-control study

scientific article

Butyrophenone analogues in the carbazole series as potential atypical antipsychotics: synthesis and determination of affinities at D2, 5-HT2A, 5-HT2B and 5-HT2C receptors

scientific article published on 01 January 2000

Chemoenzymatic synthesis and binding affinity of novel (R)- and (S)-3-aminomethyl-1-tetralones, potential atypical antipsychotics

scientific article published in February 2004

Chitosan-hyaluronic acid nanoparticles loaded with heparin for the treatment of asthma.

scientific article published on 15 April 2009

Clinical validation of blood/brain glutamate grabbing in acute ischemic stroke

scientific article published on 22 August 2018

Computer-aided design of multi-target ligands at A1R, A2AR and PDE10A, key proteins in neurodegenerative diseases

scientific article published on 30 December 2017

Computer-aided structure-based design of multitarget leads for Alzheimer's disease

scientific article

Concise asymmetric syntheses of novel phenanthroquinolizidines

scientific article published on 21 January 2016

Conformationally constrained butyrophenones as new pharmacological tools to study 5-HT 2A and 5-HT 2C receptor behaviours

scientific article published in April 2003

Cytocompatibility and P-glycoprotein inhibition of block copolymers: structure-activity relationship.

scientific article published on 25 June 2013

Detection of new biased agonists for the serotonin 5-HT2A receptor: modeling and experimental validation.

scientific article published on 6 February 2015

Development of Fluorescent Probes that Target Serotonin 5-HT2B Receptors

scientific article published on 7 September 2017

Development of a Multiplex Assay for Studying Functional Selectivity of Human Serotonin 5-HT2A Receptors and Identification of Active Compounds by High-Throughput Screening.

scientific article

Different pharmacological properties of two equipotent antagonists (clozapine and rauwolscine) for 5-HT2B receptors in rat stomach fundus

scientific article published in September 2003

Differential regulation of rat peripheral 5-HT(2A) and 5-HT(2B) receptor systems: influence of drug treatment

scientific article

Discovery of 3,4-Dihydropyrimidin-2(1H)-ones As a Novel Class of Potent and Selective A2B Adenosine Receptor Antagonists

scientific article

Discovery of potent p38α MAPK inhibitors through a funnel like workflow combining in silico screening and in vitro validation

scientific article published on 16 August 2019

Divergent solution-phase synthesis of diarylpyrimidine libraries as selective A3 adenosine receptor antagonists

scientific article

Docking Screens for Dual Inhibitors of Disparate Drug Targets for Parkinson's Disease

scientific article published on 15 June 2018

Doxorubicin-loaded micelles of reverse poly(butylene oxide)-poly(ethylene oxide)-poly(butylene oxide) block copolymers as efficient "active" chemotherapeutic agents

scientific article published on February 2013

EU-OPENSCREEN: A Novel Collaborative Approach to Facilitate Chemical Biology

scientific article published on 07 January 2019

Effect of Nitrogen Atom Substitution in A3 Adenosine Receptor Binding: N-(4,6-Diarylpyridin-2-yl)acetamides as Potent and Selective Antagonists

scientific article published on 9 August 2017

Effect of phosphodiesterase 7 (PDE7) inhibitors in experimental autoimmune encephalomyelitis mice. Discovery of a new chemically diverse family of compounds

scientific article published on 16 March 2012

Emerging opportunities and concerns for drug discovery at serotonin 5-HT2B receptors

scientific article published on January 2010

Enantiospecific Recognition at the A2B Adenosine Receptor by Alkyl 2-Cyanoimino-4-substituted-6-methyl-1,2,3,4-tetrahydropyrimidine-5-carboxylates

scientific article published on 3 April 2017

Evidence for distinct antagonist-revealed functional states of 5-hydroxytryptamine(2A) receptor homodimers.

scientific article published on 11 March 2009

Exploring the size of the lipophilic unit of the soluble epoxide hydrolase inhibitors

scientific article published on 26 August 2019

Fingerprint-Based Machine Learning Approach to Identify Potent and Selective 5-HT2BR Ligands.

scientific article published on 10 May 2018

Genetic enhancement of Ras-ERK pathway does not aggravate L-DOPA-induced dyskinesia in mice but prevents the decrease induced by lovastatin

scientific article published in Scientific Reports

High-affinity sequence-selective DNA binding by iridium(iii) polypyridyl organometallopeptides

scholarly article by Ilaria Gamba et al published 2016 in Chemical Communications

Identification in silico and experimental validation of novel phosphodiesterase 7 inhibitors with efficacy in experimental autoimmune encephalomyelitis mice

scientific article

Identification of New Activators of Mitochondrial Fusion Reveals a Link between Mitochondrial Morphology and Pyrimidine Metabolism

scientific article published on 23 December 2017

Identification of novel species-selective agonists of the G-protein-coupled receptor GPR35 that promote recruitment of β-arrestin-2 and activate Gα13.

scientific article

In silico directed chemical probing of the adenosine receptor family

scientific article

Inhibition of P-glycoprotein pumps by PEO-PPO amphiphiles: branched versus linear derivatives

scientific article published on November 2010

Intracellular delivery of docetaxel using freeze-dried polysaccharide nanocapsules.

scientific article

Membrane-disrupting iridium(iii) oligocationic organometallopeptides

scientific article published on 19 August 2016

Modulation of cAMP-specific PDE without emetogenic activity: new sulfide-like PDE7 inhibitors

scientific article published on 8 October 2014

Multiple conformations of native and recombinant human 5-hydroxytryptamine(2a) receptors are labeled by agonists and discriminated by antagonists.

scientific article published in October 2001

Multistructure 3D-QSAR Studies on a Series of Conformationally Constrained Butyrophenones Docked into a New Homology Model of the 5-HT2AReceptor

article

Multitarget-directed tricyclic pyridazinones as G protein-coupled receptor ligands and cholinesterase inhibitors

scientific article published on 29 April 2015

Natural tetraponerines: a general synthesis and antiproliferative activity

scientific article published on 14 April 2014

Neuroprotective efficacy of quinazoline type phosphodiesterase 7 inhibitors in cellular cultures and experimental stroke model

scientific article

New Serotoninergic Ligands Containing Indolic and Methyl Indolic Nuclei: Synthesis and in Vitro Pharmacological Evaluation

scientific article published on 13 June 2019

New chromene scaffolds for adenosine A(2A) receptors: synthesis, pharmacology and structure-activity relationships.

scientific article

New serotonin 5-HT(2A), 5-HT(2B), and 5-HT(2C) receptor antagonists: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo and heterocycloalkanones

scientific article published in January 2002

Novel insights on the structural determinants of clozapine and olanzapine multi-target binding profiles

scholarly article by Jana Selent et al published April 2014 in European Journal of Medicinal Chemistry

Open PHACTS computational protocols for in silico target validation of cellular phenotypic screens: knowing the knowns.

scientific article

Open Source Drug Discovery with the Malaria Box Compound Collection for Neglected Diseases and Beyond

scientific article (publication date: July 2016)

Parallel regulation by olanzapine of the patterns of expression of 5-HT2A and D3 receptors in rat central nervous system and blood cells

scientific article published on 14 August 2006

Perturbation Theory/Machine Learning Model of ChEMBL Data for Dopamine Targets: Docking, Synthesis, and Assay of New l-Prolyl-l-leucyl-glycinamide Peptidomimetics

scientific article published on 25 June 2018

Pharmacological tools based on imidazole scaffold proved the utility of PDE10A inhibitors for Parkinson's disease

scientific article published on 09 May 2017

Phe369(7.38) at human 5-HT(7) receptors confers interspecies selectivity to antagonists and partial agonists.

scientific article published on 18 November 2009

Poly(styrene oxide)-poly(ethylene oxide) block copolymers: From "classical" chemotherapeutic nanocarriers to active cell-response inducers.

scientific article published on 23 January 2013

Pyridazines. Part 28: 5-alkylidene-6-phenyl-3(2H)-pyridazinones, a new family of platelet aggregation inhibitors

scientific article

Pyrimidine derivatives as potent and selective A3 adenosine receptor antagonists

scientific article published on 27 December 2010

QF2004B, a potential antipsychotic butyrophenone derivative with similar pharmacological properties to clozapine.

scientific article published on 11 May 2006

Reelin influences the expression and function of dopamine D2 and serotonin 5-HT2A receptors: a comparative study

scientific article published on 28 January 2015

Selective and potent adenosine A3 receptor antagonists by methoxyaryl substitution on the N-(2,6-diarylpyrimidin-4-yl)acetamide scaffold

scientific article

Sensitization to MDMA locomotor effects and changes in the functionality of 5-HT(2A) and D₂ receptors in mice

scientific article published in August 2011

Serotonin 2A receptor disulfide bridge integrity is crucial for ligand binding to different signalling states but not for its homodimerization.

scientific article published on 9 September 2017

Serotonin-2A homodimers are needed for signalling via both phospholipase A2 and phospholipase C in transfected CHO cells

scientific article

Stapling Amantadine to Melanostatin Neuropeptide: Discovery of Potent Positive Allosteric Modulators of the D2 Receptors

Structure-Based Discovery of Selective Serotonin 5-HT 1B Receptor Ligands

scholarly article by David Rodríguez published in August 2014

Syntheses and cytotoxicity of (R)- and (S)-7-methoxycryptopleurine

scientific article

Synthesis and Evaluation of Adenosine Antagonist Activity of a Series of [1,2,4]Triazolo[1,5-c]quinazolines

scientific article published on 01 March 2007

Synthesis and allosteric modulation of the dopamine receptor by peptide analogs of L-prolyl-L-leucyl-glycinamide (PLG) modified in the L-proline or L-proline and L-leucine scaffolds.

scientific article

Synthesis and binding affinity of new 1,4-disubstituted triazoles as potential dopamine D(3) receptor ligands

scientific article published on 16 August 2013

Synthesis and binding affinity of new pyrazole and isoxazole derivatives as potential atypical antipsychotics

article published in 2007

Synthesis and binding affinity of novel 3-aminoethyl-1-tetralones, potential atypical antipsychotics

scientific article published in June 2005

Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif

scientific article published on 17 September 2009

Synthesis and biological activity of new potential agonists for the human adenosine A2A receptor

scientific article

Synthesis and biological evaluation of a series of aminoalkyl-tetralones and tetralols as dual dopamine/serotonin ligands

scientific article

Synthesis and pharmacological evaluation of novel 1,3,8- and 1,3,7,8-substituted xanthines as adenosine receptor antagonists

scientific article

Synthesis and pharmacological evaluation of novel 1- and 8-substituted-3-furfuryl xanthines as adenosine receptor antagonists

scientific article

Synthesis and pharmacological evaluation of novel substituted 9-deazaxanthines as A2B receptor antagonists

scientific article published on 12 March 2010

Synthesis by microwave-assisted 1,3-dipolar cycloaddition of 1,2,3-triazole 1'-homo-3'-isoazanucleosides and evaluation of their anticancer activity

scientific article published on 21 May 2015

Synthesis of new mannosyl, galactosyl and glucosyl theophylline nucleosides with potential activity as antagonists of adenosine receptors. DEMA-induced cyclization of glycosylideneiminouracils

scientific article published on 18 January 2008

Synthesis of novel 1-alkyl-8-substituted-3-(3-methoxypropyl) xanthines as putative A(2B) receptor antagonists.

scientific article

Synthesis of novel chromene scaffolds for adenosine receptors

Synthesis of theophylline derivatives and study of their activity as antagonists at adenosine receptors

scientific article published on 15 February 2010

Synthesis, 3D-QSAR, and structural modeling of benzolactam derivatives with binding affinity for the D(2) and D(3) receptors

scientific article published in August 2010

Synthesis, Pharmacological, and Biological Evaluation of MIF-1 Picolinoyl Peptidomimetics as Positive Allosteric Modulators of D2R

scientific article published on 07 August 2019

Synthesis, adenosine receptor binding and 3D-QSAR of 4-substituted 2-(2'-furyl)-1,2,4-triazolo[1,5-a]quinoxalines

scientific article published on 24 January 2008

Synthesis, binding affinity and SAR of new benzolactam derivatives as dopamine D3 receptor ligands

scientific article published on 27 January 2009

Synthesis, binding affinity, and molecular docking analysis of new benzofuranone derivatives as potential antipsychotics

scientific article published on 11 September 2008

Synthesis, pharmacological evaluation and molecular docking of pyranopyrazole-linked 1,4-dihydropyridines as potent positive inotropes

scientific article published on 25 April 2017

Targeting PDE10A GAF Domain with Small Molecules: A Way for Allosteric Modulation with Anti-Inflammatory Effects.

scientific article published on 4 September 2017

The Pyrazolobenzothiazine Core as a New Chemotype of p38 Alpha Mitogen-Activated Protein Kinase Inhibitors.

scientific article published on 14 January 2015

The application of the open pharmacological concepts triple store (Open PHACTS) to support drug discovery research

scientific article published in 2014

The arylpiperazine derivatives N-(4-cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide and N-benzyl-4-(2-diphenyl)-1-piperazinehexanamide exert a long-lasting inhibition of human serotonin 5-HT7 receptor binding and cAMP signaling.

scientific article published on 5 December 2013

Trifluorinated Pyrimidine-Based A2B Antagonists: Optimization and Evidence of Stereospecific Recognition

scientific article published on 04 October 2019

Unraveling phosphodiesterase surfaces. Identification of phosphodiesterase 7 allosteric modulation cavities

scientific article published on 22 October 2013

cis-Platinum Complex Encapsulated in Self-Assembling Cyclic Peptide Dimers

scientific article published on 4 May 2017

List of works by Jose Brea

1,3-Dialkyl-8-(hetero)aryl-9-OH-9-deazaxanthines as potent A2B adenosine receptor antagonists: design, synthesis, structure-affinity and structure-selectivity relationships

1,3-dialkyl-8-N-substituted benzyloxycarbonylamino-9-deazaxanthines as potent adenosine receptor ligands: Design, synthesis, structure-affinity and structure-selectivity relationships.

1-, 3- and 8-substituted-9-deazaxanthines as potent and selective antagonists at the human A2B adenosine receptor

2-Aryladenine derivatives as a potent scaffold for A1, A3 and dual A1/A3 adenosine receptor antagonists: Synthesis and structure-activity relationships

2-Phenylquinazolinones as dual-activity tankyrase-kinase inhibitors

3,4-Dihydropyrimidin-2(1<i>H</i>)-ones as Antagonists of the Human A<sub>2B</sub> Adenosine Receptor: Optimization, Structure-Activity Relationship Studies, and Enantiospecific Recognition

5-HT2 receptor binding, functional activity and selectivity in N-benzyltryptamines

A New Model of Sensorial Neuron-Like Cells for HTS of Novel Analgesics for Neuropathic Pain

A Positive Allosteric Modulator of the Serotonin 5-HT2C Receptor for Obesity

A Potential Nanomedicine Consisting of Heparin-Loaded Polysaccharide Nanocarriers for the Treatment of Asthma

A new chemical tool (C0036E08) supports the role of adenosine A(2B) receptors in mediating human mast cell activation

A novel mechanism of neuroprotection: Blood glutamate grabber

Association of community-acquired pneumonia with antipsychotic drug use in elderly patients: a nested case-control study

Butyrophenone analogues in the carbazole series as potential atypical antipsychotics: synthesis and determination of affinities at D2, 5-HT2A, 5-HT2B and 5-HT2C receptors

Chemoenzymatic synthesis and binding affinity of novel (R)- and (S)-3-aminomethyl-1-tetralones, potential atypical antipsychotics

Chitosan-hyaluronic acid nanoparticles loaded with heparin for the treatment of asthma.

Clinical validation of blood/brain glutamate grabbing in acute ischemic stroke

Computer-aided design of multi-target ligands at A1R, A2AR and PDE10A, key proteins in neurodegenerative diseases

Computer-aided structure-based design of multitarget leads for Alzheimer's disease

Concise asymmetric syntheses of novel phenanthroquinolizidines

Conformationally constrained butyrophenones as new pharmacological tools to study 5-HT 2A and 5-HT 2C receptor behaviours

Cytocompatibility and P-glycoprotein inhibition of block copolymers: structure-activity relationship.

Detection of new biased agonists for the serotonin 5-HT2A receptor: modeling and experimental validation.

Development of Fluorescent Probes that Target Serotonin 5-HT2B Receptors

Development of a Multiplex Assay for Studying Functional Selectivity of Human Serotonin 5-HT2A Receptors and Identification of Active Compounds by High-Throughput Screening.

Different pharmacological properties of two equipotent antagonists (clozapine and rauwolscine) for 5-HT2B receptors in rat stomach fundus

Differential regulation of rat peripheral 5-HT(2A) and 5-HT(2B) receptor systems: influence of drug treatment

Discovery of 3,4-Dihydropyrimidin-2(1H)-ones As a Novel Class of Potent and Selective A2B Adenosine Receptor Antagonists

Discovery of potent p38α MAPK inhibitors through a funnel like workflow combining in silico screening and in vitro validation

Divergent solution-phase synthesis of diarylpyrimidine libraries as selective A3 adenosine receptor antagonists

Docking Screens for Dual Inhibitors of Disparate Drug Targets for Parkinson's Disease

Doxorubicin-loaded micelles of reverse poly(butylene oxide)-poly(ethylene oxide)-poly(butylene oxide) block copolymers as efficient "active" chemotherapeutic agents

EU-OPENSCREEN: A Novel Collaborative Approach to Facilitate Chemical Biology

Effect of Nitrogen Atom Substitution in A3 Adenosine Receptor Binding: N-(4,6-Diarylpyridin-2-yl)acetamides as Potent and Selective Antagonists

Effect of phosphodiesterase 7 (PDE7) inhibitors in experimental autoimmune encephalomyelitis mice. Discovery of a new chemically diverse family of compounds

Emerging opportunities and concerns for drug discovery at serotonin 5-HT2B receptors

Enantiospecific Recognition at the A2B Adenosine Receptor by Alkyl 2-Cyanoimino-4-substituted-6-methyl-1,2,3,4-tetrahydropyrimidine-5-carboxylates

Evidence for distinct antagonist-revealed functional states of 5-hydroxytryptamine(2A) receptor homodimers.

Exploring the size of the lipophilic unit of the soluble epoxide hydrolase inhibitors

Fingerprint-Based Machine Learning Approach to Identify Potent and Selective 5-HT2BR Ligands.

Genetic enhancement of Ras-ERK pathway does not aggravate L-DOPA-induced dyskinesia in mice but prevents the decrease induced by lovastatin

High-affinity sequence-selective DNA binding by iridium(iii) polypyridyl organometallopeptides

Identification in silico and experimental validation of novel phosphodiesterase 7 inhibitors with efficacy in experimental autoimmune encephalomyelitis mice

Identification of New Activators of Mitochondrial Fusion Reveals a Link between Mitochondrial Morphology and Pyrimidine Metabolism

Identification of novel species-selective agonists of the G-protein-coupled receptor GPR35 that promote recruitment of β-arrestin-2 and activate Gα13.

In silico directed chemical probing of the adenosine receptor family

Inhibition of P-glycoprotein pumps by PEO-PPO amphiphiles: branched versus linear derivatives

Intracellular delivery of docetaxel using freeze-dried polysaccharide nanocapsules.

Membrane-disrupting iridium(iii) oligocationic organometallopeptides

Modulation of cAMP-specific PDE without emetogenic activity: new sulfide-like PDE7 inhibitors

Multiple conformations of native and recombinant human 5-hydroxytryptamine(2a) receptors are labeled by agonists and discriminated by antagonists.

Multistructure 3D-QSAR Studies on a Series of Conformationally Constrained Butyrophenones Docked into a New Homology Model of the 5-HT2AReceptor

Multitarget-directed tricyclic pyridazinones as G protein-coupled receptor ligands and cholinesterase inhibitors

Natural tetraponerines: a general synthesis and antiproliferative activity

Neuroprotective efficacy of quinazoline type phosphodiesterase 7 inhibitors in cellular cultures and experimental stroke model

New Serotoninergic Ligands Containing Indolic and Methyl Indolic Nuclei: Synthesis and in Vitro Pharmacological Evaluation

New chromene scaffolds for adenosine A(2A) receptors: synthesis, pharmacology and structure-activity relationships.

New serotonin 5-HT(2A), 5-HT(2B), and 5-HT(2C) receptor antagonists: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo and heterocycloalkanones

Novel insights on the structural determinants of clozapine and olanzapine multi-target binding profiles

Open PHACTS computational protocols for in silico target validation of cellular phenotypic screens: knowing the knowns.

Open Source Drug Discovery with the Malaria Box Compound Collection for Neglected Diseases and Beyond

Parallel regulation by olanzapine of the patterns of expression of 5-HT2A and D3 receptors in rat central nervous system and blood cells

Perturbation Theory/Machine Learning Model of ChEMBL Data for Dopamine Targets: Docking, Synthesis, and Assay of New l-Prolyl-l-leucyl-glycinamide Peptidomimetics

Pharmacological tools based on imidazole scaffold proved the utility of PDE10A inhibitors for Parkinson's disease

Phe369(7.38) at human 5-HT(7) receptors confers interspecies selectivity to antagonists and partial agonists.

Poly(styrene oxide)-poly(ethylene oxide) block copolymers: From "classical" chemotherapeutic nanocarriers to active cell-response inducers.

Pyridazines. Part 28: 5-alkylidene-6-phenyl-3(2H)-pyridazinones, a new family of platelet aggregation inhibitors

Pyrimidine derivatives as potent and selective A3 adenosine receptor antagonists

QF2004B, a potential antipsychotic butyrophenone derivative with similar pharmacological properties to clozapine.

Reelin influences the expression and function of dopamine D2 and serotonin 5-HT2A receptors: a comparative study

Selective and potent adenosine A3 receptor antagonists by methoxyaryl substitution on the N-(2,6-diarylpyrimidin-4-yl)acetamide scaffold

Sensitization to MDMA locomotor effects and changes in the functionality of 5-HT(2A) and D₂ receptors in mice

Serotonin 2A receptor disulfide bridge integrity is crucial for ligand binding to different signalling states but not for its homodimerization.

Serotonin-2A homodimers are needed for signalling via both phospholipase A2 and phospholipase C in transfected CHO cells

Stapling Amantadine to Melanostatin Neuropeptide: Discovery of Potent Positive Allosteric Modulators of the D2 Receptors

Structure-Based Discovery of Selective Serotonin 5-HT 1B Receptor Ligands

Syntheses and cytotoxicity of (R)- and (S)-7-methoxycryptopleurine

Synthesis and Evaluation of Adenosine Antagonist Activity of a Series of [1,2,4]Triazolo[1,5-c]quinazolines

Synthesis and allosteric modulation of the dopamine receptor by peptide analogs of L-prolyl-L-leucyl-glycinamide (PLG) modified in the L-proline or L-proline and L-leucine scaffolds.