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List of works by Craig W. Lindsley

"Molecular switches" on mGluR allosteric ligands that modulate modes of pharmacology

scientific article published on 04 March 2011

(3-Cyano-5-fluorophenyl)biaryl negative allosteric modulators of mGlu(5): Discovery of a new tool compound with activity in the OSS mouse model of addiction

scientific article

(S)-(+)-Mecamylamine (TC-5214): A Neuronal Nicotinic Receptor Modulator Enters Phase III Trials as an Adjunct Treatment for Major Depressive Disorder (MDD) ⬇️

scientific article published on August 18, 2010

2012 trends and statistics for prescription medications in the United States: CNS therapeutics continue to hold leading positions

scientific article published on August 2013

2013 Philip S. Portoghese Medicinal Chemistry Lectureship: drug discovery targeting allosteric sites

scientific article

2013 Statistics for global prescription medications: CNS therapeutics maintain a leading position among small molecule therapeutics

scientific article published on April 2014

2013 trends and statistics for prescription medications in the United States: CNS highest ranked and record number of prescriptions dispensed

scientific article published in March 2015

2015: A New Impact Factor for ACS Chemical Neuroscience and New Topline Data for Global Pharmaceutical Products

scientific article

2016: Onward and Upward

scientific article published in January 2016

2018: A New Impact Factor and an Expanded Cast of Associate Editors

scientific article published on 01 July 2018

2020-A Year of Growth for ACS Chemical Neuroscience

scientific article published on 01 February 2020

2021: A New Year and New Directions for the <i>Journal of Medicinal Chemistry</i>

scientific article published on 04 January 2021

3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds with CNS exposure in rats

scientific article

43.1 GENETIC INSIGHTS LEAD TO DISCOVERY OF SELECTIVE ACTIVATORS OF MGLU1 AND MGLU3 METABOTROPIC GLUTAMATE RECEPTORS AS POTENTIAL TREATMENTS FOR SCHIZOPHRENIA.

scientific article

A Call to Action on Mental Illness from the World Health Organization.

scientific article

A Duplexed High-Throughput Screen to Identify Allosteric Modulators of the Glucagon-Like Peptide 1 and Glucagon Receptors

scientific article published on 13 February 2014

A General, Enantioselective Synthesis of 1-Azabicyclo[m.n.0]alkane Ring Systems

scientific article published in March 2013

A General, Enantioselective Synthesis of Protected Morpholines and Piperazines ⬇️

scientific article published on May 22, 2012

A New Bromo Trienyne: Synthesis of all-E, Conjugated Tetra-, Penta-, and Hexaenes Common to Oxo Polyene Macrolide Antibiotics ⬇️

scientific article published on September 4, 1998

A New Impact Factor and New Directions for ACS Chemical Neuroscience ⬇️

scientific article published on July 17, 2013

A New Impact Factor: the Upward Momentum Continues.

scientific article

A Possible Repeal of the Orphan Drug Tax Credit?

scientific article published in December 2017

A Screen of Approved Drugs Identifies the Androgen Receptor Antagonist Flutamide and Its Pharmacologically Active Metabolite 2-Hydroxy-Flutamide as Heterotropic Activators of Cytochrome P450 3A In Vitro and In Vivo

scientific article published on 11 August 2015

A Special “Reviews” Issue on the Chemical Senses.

scientific article published on 19 January 2011

A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5.

scientific article

A general, enantioselective synthesis of N-alkyl terminal aziridines and C2-functionalized azetidines via organocatalysis

scientific article published on March 2015

A general, enantioselective synthesis of β- and γ-fluoroamines

scientific article published on July 2013

A new catalytic Cu(II)/sparteine oxidant system for beta,beta-phenolic couplings of styrenyl phenols: synthesis of carpanone and unnatural analogs

scientific article published on 27 August 2008

A new multi-gram synthetic route to labeling precursors for the D(2/3) PET agent 18F-fallypride

scientific article published on 20 July 2008

A new, non-SSRI mechanism of action for Prozac

scientific article

A novel M1 PAM VU0486846 exerts efficacy in cognition models without displaying agonist activity or cholinergic toxicity

scientific article published on 27 April 2018

A novel class of H3 antagonists derived from the natural product guided synthesis of unnatural analogs of the marine bromopyrrole alkaloid dispyrin

scientific article published on 3 May 2009

A novel class of succinimide-derived negative allosteric modulators of metabotropic glutamate receptor subtype 1 provides insight into a disconnect in activity between the rat and human receptors

scientific article

A novel radioligand for glycine transporter 1: characterization and use in autoradiographic and in vivo brain occupancy studies

scientific article

A novel selective allosteric modulator potentiates the activity of native metabotropic glutamate receptor subtype 5 in rat forebrain

scientific article

A novel selective muscarinic acetylcholine receptor subtype 1 antagonist reduces seizures without impairing hippocampus-dependent learning

scientific article

A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral models

scientific article

A rodent model of traumatic stress induces lasting sleep and quantitative electroencephalographic disturbances

scientific article

A selective allosteric potentiator of the M1 muscarinic acetylcholine receptor increases activity of medial prefrontal cortical neurons and restores impairments in reversal learning

scientific article

A unique industrial-academic collaboration towards the next generation of schizophrenia therapeutics

scientific article published on January 2014

A versatile enantioselective synthesis of azabicyclic ring systems: a concise total synthesis of (+)-grandisine D and unnatural analogues

scientific article published on 30 March 2012

ACS Chemical Neuroscience and Neuroscience Drug Discovery as 2012 Comes to a Close ⬇️

scientific article published on December 19, 2012

ACS Chemical Neuroscience in 2012:Opportunities and Challenges.

scientific article published on 18 January 2012

ACS Chemical Neuroscience in 2014.

scientific article published on 19 February 2014

ACS Chemical Neuroscience: Most Cited Papers from 2015.

scientific article published on August 2017

ACS Chemical Neuroscience: Most Cited Papers from 2016.

scientific article

ACS Editors' Choice: Providing Recognition to Authors and Open Access to the Community

scientific article

Accelerating Precision Drug Development and Drug Repurposing by Leveraging Human Genetics

scientific article published on 5 April 2017

Activation of Metabotropic Glutamate Receptor 7 Is Required for Induction of Long-Term Potentiation at SC-CA1 Synapses in the Hippocampus

scientific article published on May 2015

Activation of metabotropic glutamate receptors as a novel approach for the treatment of schizophrenia

scientific article published on 06 December 2008

Acute Negative Allosteric Modulation of M5 Muscarinic Acetylcholine Receptors Inhibits Oxycodone Self-Administration and Cue-Induced Reactivity with No Effect on Antinociception

scientific article published on 24 July 2019

Acyl dihydropyrazolo[1,5-a]pyrimidinones as metabotropic glutamate receptor 5 positive allosteric modulators

scientific article published on 9 October 2015

Akt-dependent and isoform-specific regulation of dopamine transporter cell surface expression.

scientific article

Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors

scientific article

Allosteric activation of M4 muscarinic receptors improve behavioral and physiological alterations in early symptomatic YAC128 mice.

scientific article

Allosteric modulation of Class C GPCRs: a novel approach for the treatment of CNS disorders

scientific article

Allosteric modulation of kinases and GPCRs: design principles and structural diversity

scientific article published on 18 April 2008

Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery

scientific article

Allosteric modulation of the M1 muscarinic acetylcholine receptor: improving cognition and a potential treatment for schizophrenia and Alzheimer's disease

scientific article (publication date: December 2013)

Allosteric modulators for the treatment of schizophrenia: targeting glutamatergic networks

scientific article published on January 2013

Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders

scientific article published on January 2009

Alzheimer's disease: development of disease-modifying treatments is the challenge for our generation

scientific article published on November 2012

An mGlu5-Positive Allosteric Modulator Rescues the Neuroplasticity Deficits in a Genetic Model of NMDA Receptor Hypofunction in Schizophrenia

scientific article published on 7 January 2016

Analgesic Effects of the GIRK Activator, VU0466551, Alone and in Combination with Morphine in Acute and Persistent Pain Models

scientific article published on 11 December 2018

Antipsychotic drug-like effects of the selective M4 muscarinic acetylcholine receptor positive allosteric modulator VU0152100

scientific article

Antipsychotic-like Effects of M4 Positive Allosteric Modulators Are Mediated by CB2 Receptor-Dependent Inhibition of Dopamine Release

scientific article published on 3 September 2016

Application of Parallel Multiparametric Cell-Based FLIPR Detection Assays for the Identification of Modulators of the Muscarinic Acetylcholine Receptor 4 (M4)

scientific article published on 15 April 2015

Application of combinatorial chemistry science on modern drug discovery

scientific article published on 26 January 2008

Applications of microwave-assisted organic synthesis on the multigram scale

scientific article

Asymmetric Synthesis of Natural and Unnatural Dibenzylbutane Lignans from a Common Intermediate

scientific article published on 24 April 2019

Attenuation of cocaine's reinforcing and discriminative stimulus effects via muscarinic M1 acetylcholine receptor stimulation.

scientific article

Autoregulation of phospholipase D activity is coupled to selective induction of phospholipase D1 expression to promote invasion of breast cancer cells

scientific article published in February 2011

Biased M1 receptor-positive allosteric modulators reveal role of phospholipase D in M1-dependent rodent cortical plasticity

scientific article published on 03 December 2019

Biased mGlu5-Positive Allosteric Modulators Provide In Vivo Efficacy without Potentiating mGlu5 Modulation of NMDAR Currents

scientific article

Biomimetic Synthesis and Biological Evaluation of Aplidiopsamine A ⬇️

scientific article published on October 29, 2012

Biotransformation of a novel positive allosteric modulator of metabotropic glutamate receptor subtype 5 contributes to seizure-like adverse events in rats involving a receptor agonism-dependent mechanism

scientific article published on 02 July 2013

CNS Pathogens: A Special Issue of ACS Chemical Neuroscience

scientific article published on 01 August 2020

Call for Papers! A SpecialThematic Compilation/Special Issue Crossover with the Journal of Medicinal Chemistry and ACS Medicinal Chemistry Letters Focused on Alzheimer’s Disease.

scientific article published on 21 March 2012

Call for Papers: Allosteric Modulators of Drug Targets-Special Issue for 2019

scientific article published on 01 March 2018

Call for Papers: DARK Classics in Chemical Neuroscience

scientific article published in September 2017

Call for Papers: Strategies and Tactics in CNS Drug Synthesis

scientific article published on 01 March 2019

Centrally active allosteric potentiators of the M4 muscarinic acetylcholine receptor reverse amphetamine-induced hyperlocomotor activity in rats

scientific article

Challenges in the development of an M4 PAM in vivo tool compound: The discovery of VU0467154 and unexpected DMPK profiles of close analogs

scientific article

Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and in vivo characterization of a series of 3-aminoazetidine-derived amides

scientific article published on 6 May 2017

Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA.

scientific article

Chemical Modification of the M1 Agonist VU0364572 Reveals Molecular Switches in Pharmacology and a Bitopic Binding Mode ⬇️

scientific article published on September 9, 2012

Chemical inhibition of fatty acid absorption and cellular uptake limits lipotoxic cell death

scientific article published on 19 September 2015

Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM.

scientific article

Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part II: development of a potent and highly selective M1 PAM

scientific article

Chemical modulation of glycerolipid signaling and metabolic pathways

scientific article published on 15 January 2014

Chemical modulation of mutant mGlu1 receptors derived from deleterious GRM1 mutations found in schizophrenics

scientific article

Cholinergic Projections to the Substantia Nigra Pars Reticulata Inhibit Dopamine Modulation of Basal Ganglia through the M4 Muscarinic Receptor

scientific article published in December 2017

Chronic Traumatic Encephalopathy (CTE): A Brief Historical Overview and Recent Focus on NFL Players

scientific article published in August 2017

Chronic Traumatic Encephalopathy (CTE): A Virtual Issue Dedicated to Advances in Understanding, Diagnosing, and Potentially Treating Tauopathies

scientific article published on 12 March 2020

Classics in Chemical Neuroscience: Memantine

scientific article

Classics in Chemical Neuroscience: Risperidone

scientific article

Classics in Chemical Neuroscience: Xanomeline

scientific article published on 31 January 2017

Classics in chemical neuroscience: clozapine

scientific article published on July 2013

Co-Activation of Metabotropic Glutamate Receptor 3 and Beta-Adrenergic Receptors Modulates Cyclic-AMP, Long-Term Potentiation, and Disrupts Memory Reconsolidation

scientific article

Competition and allostery govern substrate selectivity of cyclooxygenase-2.

scientific article

Confronting Racism in Chemistry Journals

scientific article published on 19 June 2020

Contextual Fear Extinction Induces Hippocampal Metaplasticity Mediated by Metabotropic Glutamate Receptor 5.

scientific article published on 9 November 2017

Continued optimization of the M5 NAM ML375: Discovery of VU6008667, an M5 NAM with high CNS penetration and a desired short half-life in rat for addiction studies

scientific article published on 13 February 2017

Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor ⬇️

scientific article published on March 29, 2012

Contribution of both M1 and M4 receptors to muscarinic agonist-mediated attenuation of the cocaine discriminative stimulus in mice ⬇️

scientific article published on October 1, 2011

Contributions of Protease-Activated Receptors PAR1 and PAR4 to Thrombin-Induced GPIIbIIIa Activation in Human Platelets

scientific article published on 26 October 2016

Cooperative signaling between Slit2 and Ephrin-A1 regulates a balance between angiogenesis and angiostasis.

scientific article

Correction to Analgesic Effects of the GIRK Activator, VU0466551, Alone and in Combination with Morphine in Acute and Persistent Pain Models

scientific article published on 26 March 2019

Corrigendum: Metabotropic Glutamate Receptor 7: A New Therapeutic Target in Neurodevelopmental Disorders

scholarly article published in Frontiers in molecular neuroscience

Crystal structure of the M5 muscarinic acetylcholine receptor

scientific article published on 26 November 2019

DARK Classics in Chemical Neuroscience: Gamma-Hydroxybutyrate (GHB)

scientific article published on 23 July 2019

DARK Classics in Chemical Neuroscience: Opium, a Historical Perspective

scientific article published on 08 October 2018

DARK Classics in Chemical Neuroscience: Phencyclidine (PCP)

Design and Synthesis of N-Aryl Phenoxyethoxy Pyridinones as Highly Selective and CNS Penetrant mGlu3 NAMs

scientific article

Design and Synthesis of mGlu2 NAMs with Improved Potency and CNS Penetration Based on a Truncated Picolinamide Core

scientific article

Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part I: Impact of alternative halogenated privileged structures for PLD1 specificity

scientific article (publication date: April 2009)

Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part II. Identification of the 1,3,8-triazaspiro[4,5]decan-4-one privileged structure that engenders PLD2 selectivity

scientific article published on 6 March 2009

Design of 4-Oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as Selective Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 2.

scientific article published on 2 November 2015

Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness

scientific article

Design of potent GlyT1 inhibitors: in vitro and in vivo profiles

scientific article published on December 2008

Design, Synthesis, and Biological Evaluation of Halogenated N-(2-(4-Oxo-1-phenyl-1,3,8-triazaspiro[4.5]decan-8-yl)ethyl)benzamides: Discovery of an Isoform-Selective Small Molecule Phospholipase D2 Inhibitor ⬇️

scientific article published on September 23, 2010

Design, synthesis, and evaluation of a novel 4-aminomethyl-4-fluoropiperidine as a T-type Ca2+ channel antagonist

scientific article published on 10 June 2008

Design, synthesis, and evaluation of novel 3,6-diaryl-4-aminoalkoxyquinolines as selective agonists of somatostatin receptor subtype 2.

scientific article

Design, synthesis, and in vivo efficacy of glycine transporter-1 (GlyT1) inhibitors derived from a series of [4-phenyl-1-(propylsulfonyl)piperidin-4-yl]methyl benzamides

scientific article published on 01 August 2006

Development and Antiparkinsonian Activity of VU0418506, a Selective Positive Allosteric Modulator of Metabotropic Glutamate Receptor 4 Homomers without Activity at mGlu2/4 Heteromers

scientific article

Development of Novel, CNS Penetrant Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 1 (mGlu1), Based on an N-(3-Chloro-4-(1,3-dioxoisoindolin-2-yl)phenyl)-3-methylfuran-2-carboxamide Scaffold, That Potentiate Wild Type

scientific article published in October 2015

Development of a Series of (1-Benzyl-3-(6-methoxypyrimidin-3-yl)-5-(trifluoromethoxy)-1H-indol-2-yl)methanols as Selective Protease Activated Receptor 4 (PAR4) Antagonists with in Vivo Utility and Activity Against γ-Thrombin

scientific article published on 2 August 2016

Development of a custom high-throughput preparative liquid chromatography/mass spectrometer platform for the preparative purification and analytical analysis of compound libraries

scientific article

Development of a highly potent, novel M5 positive allosteric modulator (PAM) demonstrating CNS exposure: 1-((1H-indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide (ML380)

scientific article (publication date: 25 September 2014)

Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071.

scientific article

Development of a more highly selective M1 antagonist from the continued optimization of the MLPCN Probe ML012 ⬇️

scientific article published on December 6, 2011

Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM.

scientific article published on 30 April 2012

Development of a selective small-molecule inhibitor of Kir1.1, the renal outer medullary potassium channel

scientific article

Development of an in vivo active, dual EP1 and EP3 selective antagonist based on a novel acyl sulfonamide bioisostere ⬇️

scientific article published on November 24, 2012

Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells.

scientific article published on 13 March 2013

Development of novel M1 antagonist scaffolds through the continued optimization of the MLPCN probe ML012 ⬇️

scientific article published on June 15, 2012

Development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved physical properties and cell activity

scientific article published on 13 November 2007

Difference in mGluR5 interaction between positive allosteric modulators from two structural classes

scientific article published in November 2003

Differential Pharmacology and Binding of mGlu2 Receptor Allosteric Modulators

scientific article published on 15 March 2018

Differential effects of allosteric M(1) muscarinic acetylcholine receptor agonists on receptor activation, arrestin 3 recruitment, and receptor downregulation

scientific article published on August 2010

Dihydrothiazolopyridone derivatives as a novel family of positive allosteric modulators of the metabotropic glutamate 5 (mGlu5) receptor

scientific article published on 04 September 2013

Discoidin domain receptor 1 kinase activity is required for regulating collagen IV synthesis

scientific article published on 30 November 2016

Discovery and Characterization of ML398, a Potent and Selective Antagonist of the D4 Receptor with in Vivo Activity

scientific article

Discovery and Optimization of Potent and CNS Penetrant M5-Preferring Positive Allosteric Modulators Derived from a Novel, Chiral N-(Indanyl)piperidine Amide Scaffold

scientific article published on 26 April 2018

Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5.

scientific article published on 9 October 2009

Discovery and SAR of a novel series of GIRK1/2 and GIRK1/4 activators ⬇️

scientific article published on July 18, 2013

Discovery and SAR of a novel series of metabotropic glutamate receptor 5 positive allosteric modulators with high ligand efficiency

scientific article

Discovery and SAR of a novel series of non-MPEP site mGlu5 PAMs based on an aryl glycine sulfonamide scaffold ⬇️

scientific article published on October 23, 2012

Discovery and SAR of a novel series of potent, CNS penetrant M4 PAMs based on a non-enolizable ketone core: Challenges in disposition

scientific article published on 21 July 2016

Discovery and SAR of muscarinic receptor subtype 1 (M1) allosteric activators from a molecular libraries high throughput screen. Part 1: 2,5-dibenzyl-2H-pyrazolo[4,3-c]quinolin-3(5H)-ones as positive allosteric modulators

scientific article

Discovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype

scientific article published on 03 May 2009

Discovery and SAR of novel series of imidazopyrimidinones and dihydroimidazopyrimidinones as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5).

scientific article

Discovery and characterization of 2-(cyclopropanesulfonamido)-N-(2-ethoxyphenyl)benzamide, ML382: a potent and selective positive allosteric modulator of MrgX1.

scientific article

Discovery and characterization of a novel series of N-phenylsulfonyl-1H-pyrrole picolinamides as positive allosteric modulators of the metabotropic glutamate receptor 4 (mGlu4).

scientific article published on 11 May 2016

Discovery and characterization of novel allosteric potentiators of M1 muscarinic receptors reveals multiple modes of activity

scientific article

Discovery and characterization of novel subtype-selective allosteric agonists for the investigation of M(1) receptor function in the central nervous system

scientific article published on January 2010

Discovery and development of a potent and highly selective small molecule muscarinic acetylcholine receptor subtype I (mAChR 1 or M1) antagonist in vitro and in vivo probe

scientific article published on January 2009

Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core

scientific article published on 05 May 2016

Discovery and optimization of a novel, selective and brain penetrant M1 positive allosteric modulator (PAM): The development of ML169, an MLPCN probe ⬇️

scientific article published on December 9, 2010

Discovery of (R)-(2-fluoro-4-((-4-methoxyphenyl)ethynyl)phenyl) (3-hydroxypiperidin-1-yl)methanone (ML337), an mGlu3 selective and CNS penetrant negative allosteric modulator (NAM)

scientific article

Discovery of (S)-2-cyclopentyl-N-((1-isopropylpyrrolidin2-yl)-9-methyl-1-oxo-2,9-dihydro-1H-pyrrido[3,4-b]indole-4-carboxamide (VU0453379): a novel, CNS penetrant glucagon-like peptide 1 receptor (GLP-1R) positive allosteric modulator (PAM).

scientific article published on 2 December 2014

Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels

scientific article published on 26 September 2008

Discovery of 2,3,5-trisubstituted pyridine derivatives as potent Akt1 and Akt2 dual inhibitors

scientific article

Discovery of 2-(2-benzoxazoyl amino)-4-aryl-5-cyanopyrimidine as negative allosteric modulators (NAMs) of metabotropic glutamate receptor 5 (mGlu₅): from an artificial neural network virtual screen to an in vivo tool compound

scientific article

Discovery of 3-aminopicolinamides as metabotropic glutamate receptor subtype 4 (mGlu4) positive allosteric modulator warheads engendering CNS exposure and in vivo efficacy

scientific article published on 19 April 2016

Discovery of GlyT1 inhibitors with improved pharmacokinetic properties

scientific article published on 10 January 2009

Discovery of MK-1832, a Kv1.5 inhibitor with improved selectivity and pharmacokinetics

scientific article published on 16 January 2017

Discovery of ML326: The first sub-micromolar, selective M5 PAM

scientific article

Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor

scientific article published on 6 June 2012

Discovery of N-(5-Fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide (VU0424238): A Novel Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Selected for Clinical Evaluation

scientific article

Discovery of N-Aryl Piperazines as Selective mGlu(5) Potentiators with Efficacy in a Rodent Model Predictive of Anti-Psychotic Activity

scientific article published on 13 August 2010

Discovery of N-{[1-(propylsulfonyl)-4-pyridin-2-ylpiperidin-4-yl]methyl}benzamides as novel, selective and potent GlyT1 inhibitors

scientific article

Discovery of Small-Molecule Nonfluorescent Inhibitors of Fluorogen-Fluorogen Activating Protein Binding Pair

scientific article

Discovery of Tricyclic Triazolo- and Imidazopyridine Lactams as M1 Positive Allosteric Modulators

scientific article published on 09 August 2018

Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety

scientific article published on 10 September 2013

Discovery of VU0409551/JNJ-46778212: An mGlu5 Positive Allosteric Modulator Clinical Candidate Targeting Schizophrenia

scientific article published on 20 May 2015

Discovery of VU0431316: a negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety

scientific article published on 11 June 2014

Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia

scientific article

Discovery of VU6005649, a CNS Penetrant mGlu7/8 Receptor PAM Derived from a Series of Pyrazolo[1,5-a]pyrimidines

scientific article published in September 2017

Discovery of a Novel Chemical Class of mGlu(5) Allosteric Ligands with Distinct Modes of Pharmacology

scientific article

Discovery of a Novel Series of Orally Bioavailable and CNS Penetrant Glucagon-like Peptide-1 Receptor (GLP-1R) Noncompetitive Antagonists Based on a 1,3-Disubstituted-7-aryl-5,5-bis(trifluoromethyl)-5,8-dihydropyrimido[4,5-d]pyrimidine-2,4(1H,3H)-di

scientific article published on 19 January 2017

Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents

scientific article published on 3 September 2015

Discovery of a highly selective PLD2 inhibitor (ML395): a new probe with improved physiochemical properties and broad-spectrum antiviral activity against influenza strains

scientific article

Discovery of a new molecular probe ML228: An activator of the hypoxia inducible factor (HIF) pathway ⬇️

scientific article published on November 28, 2011

Discovery of a novel 2,4-dimethylquinoline-6-carboxamide M4 positive allosteric modulator (PAM) chemotype via scaffold hopping

scientific article published on 9 October 2017

Discovery of a novel, CNS penetrant M4 PAM chemotype based on a 6-fluoro-4-(piperidin-1-yl)quinoline-3-carbonitrile core

scientific article published on 20 August 2017

Discovery of a selective M4 positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: Development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia ⬇️

scientific article published on January 1, 2013

Discovery of an Orally Bioavailable and Central Nervous System (CNS) Penetrant mGlu7 Negative Allosteric Modulator (NAM) in Vivo Tool Compound: N-(2-(1 H-1,2,4-triazol-1-yl)-5-(trifluoromethoxy)phenyl)-4-(cyclopropylmethoxy)-3-methoxybenzamide (VU60

scientific article published on 17 January 2019

Discovery of desketoraloxifene analogues as inhibitors of mammalian, Pseudomonas aeruginosa, and NAPE phospholipase D enzymes

scientific article

Discovery of imidazo[1,2-a]-, [1,2,4]triazolo[4,3-a]-, and [1,2,4]triazolo[1,5-a]pyridine-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.

scientific article published on 20 September 2017

Discovery of molecular switches that modulate modes of metabotropic glutamate receptor subtype 5 (mGlu5) pharmacology in vitro and in vivo within a series of functionalized, regioisomeric 2- and 5-(phenylethynyl)pyrimidines

scientific article

Discovery of molecular switches within the ADX-47273 mGlu5 PAM scaffold that modulate modes of pharmacology to afford potent mGlu5 NAMs, PAMs and partial antagonists ⬇️

scientific article published on 03 December 2010

Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral models of anxiolytic and antipsychotic activity

scientific article

Discovery of novel central nervous system penetrant metabotropic glutamate receptor subtype 2 (mGlu) Negative Allosteric Modulators (NAMs) based on functionalized pyrazolo[1,5- a]pyrimidine-5-carboxamide and thieno[3,2- b]pyridine-5-carboxamide cores

article

Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo

scientific article

Discovery of positive allosteric modulators of metabotropic glutamate receptor subtype 5 (mGluR5).

scientific article published in January 2005

Discovery of the first M5-selective and CNS penetrant negative allosteric modulator (NAM) of a muscarinic acetylcholine receptor: (S)-9b-(4-chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-one (ML375)

scientific article

Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins

scientific article (publication date: 11 June 2009)

Discovery of ‘molecular switches’ within a GIRK activator scaffold that afford selective GIRK inhibitors ⬇️

scientific article published on June 20, 2013

Discovery, Structure-Activity Relationship, and Biological Characterization of a Novel Series of 6-((1 H-Pyrazolo[4,3- b]pyridin-3-yl)amino)-benzo[ d]isothiazole-3-carboxamides as Positive Allosteric Modulators of the Metabotropic Glutamate Receptor

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Discovery, synthesis, and structure-based optimization of a series of N-(tert-butyl)-2-(N-arylamido)-2-(pyridin-3-yl) acetamides (ML188) as potent noncovalent small molecule inhibitors of the severe acute respiratory syndrome coronavirus [...]

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Disease-Modifying Effects of M1 Muscarinic Acetylcholine Receptor Activation in an Alzheimer's Disease Mouse Model

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Dynamic subunit stoichiometry confers a progressive continuum of pharmacological sensitivity by KCNQ potassium channels ⬇️

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Dysregulation of the norepinephrine transporter sustains cortical hypodopaminergia and schizophrenia-like behaviors in neuronal rictor null mice

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Effects of VU0410120, a novel GlyT1 inhibitor, on measures of sociability, cognition and stereotypic behaviors in a mouse model of autism

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Elevating standards for discoveries reported in ACS Chemical Neuroscience: new criteria to enhance reproducibility, experimental transparency, reliability, and the value of negative data

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Enantioselective synthesis of C2-functionalized, N-protected morpholines and orthogonally N,N′-protected piperazines via organocatalysis ⬇️

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Evaluation of the biosynthetic proposal for the synthesis of marineosins A and B

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Exploration of allosteric agonism structure-activity relationships within an acetylene series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs): discovery of 5-((3-fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolin

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Further optimization of the M1 PAM VU0453595: Discovery of novel heterobicyclic core motifs with improved CNS penetration

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Further optimization of the M5 NAM MLPCN probe ML375: tactics and challenges

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High-throughput screening reveals a small-molecule inhibitor of the renal outer medullary potassium channel and Kir7.1.

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Human phospholipase D activity transiently regulates pyrimidine biosynthesis in malignant gliomas

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Identification of the minimum PAR4 inhibitor pharmacophore and optimization of a series of 2-methoxy-6-arylimidazo[2,1-b][1,3,4]thiadiazoles

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Impaired striatal Akt signaling disrupts dopamine homeostasis and increases feeding

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In vivo structure-activity relationship study of dorsomorphin analogues identifies selective VEGF and BMP inhibitors.

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Is the Microbiome the Fifth Horseman of the Apocalypse in Drug Discovery? Implications for the Gut-Brain Axis.

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Isatin replacements applied to the highly selective, muscarinic M1 PAM ML137: continued optimization of an MLPCN probe molecule

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Isoxazole compound ML327 blocks MYC expression and tumor formation in neuroblastoma

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Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 3. Engineering plasma stability by discovery and optimization of isoindolinone analogs

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M5 receptor activation produces opposing physiological outcomes in dopamine neurons depending on the receptor's location

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ML297 (VU0456810), the First Potent and Selective Activator of the GIRK Potassium Channel, Displays Antiepileptic Properties in Mice ⬇️

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ML327 induces apoptosis and sensitizes Ewing sarcoma cells to TNF-related apoptosis-inducing ligand

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ML418: The First Selective, Sub-Micromolar Pore Blocker of Kir7.1 Potassium Channels

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Metabotropic glutamate receptor 3 activation is required for long-term depression in medial prefrontal cortex and fear extinction

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Metabotropic glutamate receptor 4 (mGlu4)-positive allosteric modulators for the treatment of Parkinson's disease: historical perspective and review of the patent literature

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Metabotropic glutamate receptor 5-positive allosteric modulators for the treatment of schizophrenia (2004-2012).

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Metabotropic glutamate receptor subtype 3 gates acute stress-induced dysregulation of amygdalo-cortical function

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Modulation of pyramidal cell output in the medial prefrontal cortex by mGluR5 interacting with CB1 ⬇️

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Muscarinic M5 receptors modulate ethanol seeking in rats

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N-Acyl-N'-arylpiperazines as negative allosteric modulators of mGlu1: identification of VU0469650, a potent and selective tool compound with CNS exposure in rats

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N-Alkylpyrido[1',2':1,5]pyrazolo-[4,3-d]pyrimidin-4-amines: A new series of negative allosteric modulators of mGlu1/5 with CNS exposure in rodents

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Neuronal ablation of p-Akt at Ser473 leads to altered 5-HT1A/2A receptor function

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Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 1: development of a potent and CNS penetrant [3.1.0]-based lead

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Novel allosteric agonists of M1 muscarinic acetylcholine receptors induce brain region-specific responses that correspond with behavioral effects in animal models

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Novel indole-3-sulfonamides as potent HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs)

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Novel selective allosteric activator of the M1 muscarinic acetylcholine receptor regulates amyloid processing and produces antipsychotic-like activity in rats.

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Octahydropyrrolo[3,4-c]pyrrole negative allosteric modulators of mGlu1.

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Opportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders

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Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of MPEP-site interaction crossover

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Optimization of the choline transporter (CHT) inhibitor ML352: Development of VU6001221, an improved in vivo tool compound

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Orthosteric- and allosteric-induced ligand-directed trafficking at GPCRs ⬇️

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PF-06827443 Displays Robust Allosteric Agonist and Positive Allosteric Modulator Activity in High Receptor Reserve and Native Systems

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PLD1 rather than PLD2 regulates phorbol-ester-, adhesion-dependent and Fc{gamma}-receptor-stimulated ROS production in neutrophils

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Parallel synthesis of N-biaryl quinolone carboxylic acids as selective M(1) positive allosteric modulators

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Partial mGlu₅ Negative Allosteric Modulators Attenuate Cocaine-Mediated Behaviors and Lack Psychotomimetic-Like Effects

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Pharmacokinetics, Tissue Localization, Toxicity, and Treatment Efficacy in the First Small Animal (Rabbit) Model of Intra-Arterial Chemotherapy for Retinoblastoma

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Pharmacological stimulation of metabotropic glutamate receptor type 4 in a rat model of Parkinson's disease and L-DOPA-induced dyskinesia: Comparison between a positive allosteric modulator and an orthosteric agonist

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Phospholipase D as a Therapeutic Target in Brain Disorders ⬇️

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Phospholipase D facilitates efficient entry of influenza virus, allowing escape from innate immune inhibition

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Phospholipase D1 Couples CD4+ T Cell Activation to c-Myc-Dependent Deoxyribonucleotide Pool Expansion and HIV-1 Replication

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Phospholipase D2 mediates survival signaling through direct regulation of Akt in glioblastoma cells

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Phospholipase D: enzymology, functionality, and chemical modulation

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Platelet Lipidomic Profiling: Novel Insight into Cytosolic Phospholipase A2α Activity and Its Role in Human Platelet Activation

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Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4). Part II: Challenges in hit-to-lead

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Potent antagonists of the Kv1.5 potassium channel: synthesis and evaluation of analogous N,N-diisopropyl-2-(pyridine-3-yl)acetamides

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Potentiating mGluR5 function with a positive allosteric modulator enhances adaptive learning

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Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate Receptors

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Prefrontal Cortex-Mediated Impairments in a Genetic Model of NMDA Receptor Hypofunction Are Reversed by the Novel M1 PAM VU6004256.

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Preliminary investigation of 6,7-dihydropyrazolo[1,5-a]pyrazin-4-one derivatives as a novel series of mGlu5 receptor positive allosteric modulators with efficacy in preclinical models of schizophrenia

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Preparation of 1,5-Dihydropyrazolo[3',4':5,6]pyrano[3,4- b]pyridines via a Microwave-Assisted, Palladium-Catalyzed Regioselective C-H Heteroarylation of Electron-Rich Pyrazoles

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Preparation of Unsymmetrical 1,2,4,5-Tetrazines via a Mild Suzuki Cross-Coupling Reaction

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Probing the metabotropic glutamate receptor 5 (mGlu₅) positive allosteric modulator (PAM) binding pocket: discovery of point mutations that engender a "molecular switch" in PAM pharmacology

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Progress in the preparation and testing of glycine transporter type-1 (GlyT1) inhibitors

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Progress toward the total synthesis of lucentamycin A: total synthesis and biological evaluation of 8-epi-lucentamycin A.

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Progress towards small molecule menin-mixed lineage leukemia (MLL) interaction inhibitors with in vivo utility

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Progress towards validating the NMDA receptor hypofunction hypothesis of schizophrenia

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ROMK inhibitor actions in the nephron probed with diuretics

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Rapid, general access to chiral beta-fluoroamines and beta,beta-difluoroamines via organocatalysis

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Re-exploration of the PHCCC Scaffold: Discovery of Improved Positive Allosteric Modulators of mGluR4

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Re-exploration of the mGlu₁ PAM Ro 07-11401 scaffold: Discovery of analogs with improved CNS penetration despite steep SAR.

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Recent progress in the development of mGluR4 positive allosteric modulators for the treatment of Parkinson's disease.

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Recent progress in the discovery and development of negative allosteric modulators of mGluR5.

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Regulation of Phospholipase D Activity and Phosphatidic Acid Production after Purinergic (P2Y6) Receptor Stimulation ⬇️

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Relationship between in vivo receptor occupancy and efficacy of metabotropic glutamate receptor subtype 5 allosteric modulators with different in vitro binding profiles

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Restoring Agonist Function at a Chemogenetically Modified M1 Muscarinic Acetylcholine Receptor

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Return of D4 Dopamine Receptor Antagonists in Drug Discovery

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Reversible inhibitors of regulators of G-protein signaling identified in a high-throughput cell-based calcium signaling assay

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Role of mGlu5 Receptors and Inhibitory Neurotransmission in M1 Dependent Muscarinic LTD in the Prefrontal Cortex: Implications in Schizophrenia

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Roles of the M1 muscarinic acetylcholine receptor subtype in the regulation of basal ganglia function and implications for the treatment of Parkinson's disease.

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Schizophrenia: moving beyond monoamine antagonists

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Screening and Beyond: New Opportunities to Advance Neuroscience Discovery ⬇️

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Selective Inhibition of the Kir2 Family of Inward Rectifier Potassium Channels by a Small Molecule Probe: The Discovery, SAR, and Pharmacological Characterization of ML133 ⬇️

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Selective activation of M4 muscarinic acetylcholine receptors reverses MK-801-induced behavioral impairments and enhances associative learning in rodents

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Selective activation of the M1 muscarinic acetylcholine receptor achieved by allosteric potentiation

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Selective inhibition of M5 muscarinic acetylcholine receptors attenuates cocaine self-administration in rats

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Small molecule/ML327 mediated transcriptional de-repression of E-cadherin and inhibition of epithelial-to-mesenchymal transition

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Small-molecule screen identifies inhibitors of the neuronal K-Cl cotransporter KCC2

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Solution-phase parallel synthesis and SAR of homopiperazinyl analogs as positive allosteric modulators of mGlu₄.

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Species-Specific Involvement of Aldehyde Oxidase and Xanthine Oxidase in the Metabolism of the Pyrimidine-Containing mGlu5-Negative Allosteric Modulator VU0424238 (Auglurant).

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Specific activin receptor-like kinase 3 inhibitors enhance liver regeneration

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Spiroaminal model systems of the marineosins with final step pyrrole incorporation ⬇️

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Spirocyclic replacements for the isatin in the highly selective, muscarinic M1 PAM ML137: the continued optimization of an MLPCN probe molecule

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State-dependent alterations in sleep/wake architecture elicited by the M4 PAM VU0467154 - Relation to antipsychotic-like drug effects

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Sterol 14α-Demethylase Structure-Based Design of VNI (( R)- N-(1-(2,4-Dichlorophenyl)-2-(1 H-imidazol-1-yl)ethyl)-4-(5-phenyl-1,3,4-oxadiazol-2-yl)benzamide)) Derivatives To Target Fungal Infections: Synthesis, Biological Evaluation, and Crystallogr

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Sterol 14α-Demethylase Structure-Based Optimization of Drug Candidates for Human Infections with the Protozoan Trypanosomatidae

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Substituted indoles as selective protease activated receptor 4 (PAR-4) antagonists: Discovery and SAR of ML354.

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Subtype-selective allosteric modulators of muscarinic receptors for the treatment of CNS disorders

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Synthesis and Biological Evaluation of Cremastrine and an Unnatural Analogue

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Synthesis and SAR of GlyT1 inhibitors derived from a series of N-((4-(morpholine-4-carbonyl)-1-(propylsulfonyl)piperidin-4-yl)methyl)benzamides

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Synthesis and SAR of N-(4-(4-alklylpiperazin-1-yl)phenyl)benzamides as muscarinic acetylcholine receptor subtype 1 (M1) anatgonists

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Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold

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Synthesis and SAR of a novel metabotropic glutamate receptor 4 (mGlu4) antagonist: Unexpected ‘molecular switch’ from a closely related mGlu4 positive allosteric modulator ⬇️

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Synthesis and SAR of a novel positive allosteric modulator (PAM) of the metabotropic glutamate receptor 4 (mGluR4).

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Synthesis and SAR of analogs of the M1 allosteric agonist TBPB. Part II: Amides, sulfonamides and ureas--the effect of capping the distal basic piperidine nitrogen

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Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties

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Synthesis and SAR of centrally active mGlu5 positive allosteric modulators based on an aryl acetylenic bicyclic lactam scaffold ⬇️

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Synthesis and SAR of novel histamine H3 receptor antagonists

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Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS).

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Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS

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Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists

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Synthesis and SAR of substituted pyrazolo[1,5-a]quinazolines as dual mGlu(2)/mGlu(3) NAMs

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Synthesis and biological characterization of a series of novel diaryl amide M1 antagonists ⬇️

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Synthesis and characterization of a series of chiral alkoxymethyl morpholine analogs as dopamine receptor 4 (D4R) antagonists

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Synthesis and evaluation of 4,6-disubstituted pyrimidines as CNS penetrant pan-muscarinic antagonists with a novel chemotype

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Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs)

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Synthesis and structure-activity relationships of a series of 4-methoxy-3-(piperidin-4-yl)oxy benzamides as novel inhibitors of the presynaptic choline transporter

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Synthesis and structure-activity relationships of allosteric potentiators of the m(4) muscarinic acetylcholine receptor

scientific article published on October 2009

Synthesis of 2,3-diarylsubstituted indazoles utilizing a Suzuki cross-coupling/deprotection/N-arylation sequence

scientific article published on July 2010

Synthesis of Indole Derived Protease-Activated Receptor 4 Antagonists and Characterization in Human Platelets ⬇️

scientific article published on June 11, 2013

Synthesis of Substituted 6,7-Dihydro-5H-pyrrolo[2,3-c]pyridazines/pyrazines via Catalyst-Free Tandem Hydroamination-Aromatic Substitution

scientific article published on 09 April 2020

Synthesis, SAR and unanticipated pharmacological profiles of analogues of the mGluR5 ago-potentiator ADX-47273

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T227. THE METABOTROPIC GLUTAMATE RECEPTOR SUBTYPE 1 REGULATES STRIATAL DOPAMINE RELEASE VIA AN ENDOCANNABINOID-DEPENDENT MECHANISM: IMPLICATIONS FOR THE TREATMENT OF SCHIZOPHRENIA.

scientific article published in April 2018

T39. NEURAL MECHANISMS OF METABOTROPIC GLUTAMATE RECEPTOR 3 MEDIATED ENHANCEMENT OF SYNAPTIC PLASTICITY AND COGNITION.

scientific article published in April 2018

Targeting phospholipase D in cancer, infection and neurodegenerative disorders

scientific article published on 17 February 2017

Targeting selective activation of M(1) for the treatment of Alzheimer's disease: further chemical optimization and pharmacological characterization of the M(1) positive allosteric modulator ML169.

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Targeting the phosphatidylinositol-3 kinase/Akt pathway for the treatment of cancer

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Tetrahydronaphthyridine and dihydronaphthyridinone ethers as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu₅).

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The Akt/PKB family of protein kinases: a review of small molecule inhibitors and progress towards target validation

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The Akt/PKB family of protein kinases: a review of small molecule inhibitors and progress towards target validation: a 2009 update

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The Akt/PKB pathway: molecular target for cancer drug discovery

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The Discovery and Characterization of ML218: A Novel, Centrally Active T-Type Calcium Channel Inhibitor with Robust Effects in STN Neurons and in a Rodent Model of Parkinson's Disease.

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The Ecstasy and Agony of Assay Interference Compounds

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The Ecstasy and Agony of Assay Interference Compounds

The Ecstasy and Agony of Assay Interference Compounds

The Ecstasy and Agony of Assay Interference Compounds

scientific article published on 28 February 2017

The Ecstasy and Agony of Assay Interference Compounds

The Ecstasy and Agony of Assay Interference Compounds

scientific article published in 2017

The Ecstasy and Agony of Assay Interference Compounds

The Ecstasy and Agony of Assay Interference Compounds.

scientific article published on 28 February 2017

The Evolution of Histamine H3 Antagonists/Inverse Agonists ⬇️

scientific article published on January 1, 2011

The Last Issue of Our Inaugural Year: Reflections and a View to the Future.

scientific article published on 15 December 2010

The Muscarinic Acetylcholine Receptor M5: Therapeutic Implications and Allosteric Modulation

scientific article published on 17 October 2018

The NIH's role in accelerating translational sciences ⬇️

scientific article published on January 9, 2012

The PI3K/Akt pathway: recent progress in the development of ATP-competitive and allosteric Akt kinase inhibitors

scientific article published on February 2008

The Top Prescription Drugs of 2010 in the United States: Antipsychotics Show Strong Growth ⬇️

scientific article published on June 15, 2011

The antipsychotic potential of muscarinic allosteric modulation

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The end of an era and new beginnings for the editorial leadership of ACS Chemical Neuroscience

scientific article published on November 2013

The future of neurodegenerative diseases: emerging targets, treatments and technologies

scientific article published in September 2012

The metabotropic glutamate receptor 4-positive allosteric modulator VU0364770 produces efficacy alone and in combination with L-DOPA or an adenosine 2A antagonist in preclinical rodent models of Parkinson's disease.

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The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.

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The synthesis and preclinical evaluation in rhesus monkey of [18F]MK‐6577 and [11C]CMPyPB glycine transporter 1 positron emission tomography radiotracers ⬇️

scientific article published on April 1, 2011

The top prescription drugs of 2009 in the US: CNS therapeutics rank among highest grossing

scientific article published in June 2010

The top prescription drugs of 2011 in the United States: antipsychotics and antidepressants once again lead CNS therapeutics

scientific article published on August 2012

The top prescription drugs of 2012 globally: biologics dominate, but small molecule CNS drugs hold on to top spots

scientific article published in June 2013

Torn from the Headlines: Angiostrongylus cantonensis (Rat Lungworm) Is Established in Florida

scientific article published in August 2017

Torn from the Headlines: Surviving the "Brain Eating Amoeba".

scientific article published in October 2016

Torn from the headlines: AstraZeneca fined for illegal marketing of SEROQUEL.

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Total RNA Sequencing of Rett Syndrome Autopsy Samples Identifies the M4 Muscarinic Receptor as a Novel Therapeutic Target

scientific article published on 9 March 2018

Total Synthesis and Biological Evaluation of Hybrubin A.

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Total Synthesis and Biological Evaluation of Phidianidines A and B Uncovers Unique Pharmacological Profiles at CNS Targets ⬇️

scientific article published on June 27, 2012

Total Synthesis of (+)-7-Bromotrypargine and Unnatural Analogues: Biological Evaluation Uncovers Activity at CNS Targets of Therapeutic Relevance ⬇️

scientific article published on November 16, 2011

Total Synthesis of Hinduchelins A-D, Stereochemical Revision of Hinduchelin A, and Biological Evaluation of Natural and Unnatural Analogues

scientific article published on 08 May 2019

Total Synthesis of Stemaphylline N‐Oxide and Related C9a‐Epimeric Analogues ⬇️

scientific article published on August 16, 2013

Total synthesis and biological evaluation of tambjamine K and a library of unnatural analogs

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Total synthesis and biological evaluation of the marine bromopyrrole alkaloid dispyrin: elucidation of discrete molecular targets with therapeutic potential

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Total synthesis of Ciliatamides A-C: stereochemical revision and the natural product-guided synthesis of unnatural analogs

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Total synthesis of brevisamide

scientific article published on September 2009

Towards the Total Synthesis of Marineosin A: Construction of the Macrocyclic Pyrrole and an Advanced, Functionalized Spiroaminal Model

scientific article published on July 2013

Towards the treatment of Alzheimer's disease: Discovery and development of novel subtype-specific M1 allosteric agonists

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Tumor cell sensitization to apoptotic stimuli by selective inhibition of specific Akt/PKB family members

scientific article published in February 2005

Tumor necrosis factor (TNF) blockers ignite FDA inquiry over cancer concerns

scientific article published on 01 January 2008

Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity

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Update to Our Reader, Reviewer, and Author Communities-April 2020

scientific article published on 22 April 2020

Update to Our Reader, Reviewer, and Author Communities-April 2020

scientific article published on 23 April 2020

Use of chemical probes to explore the toxicological potential of the K/Cl cotransporter (KCC) as a novel insecticide target to control the primary vector of dengue and Zika virus, Aedes aegypti

scientific article published on 06 April 2018

VU0477573: Partial Negative Allosteric Modulator of the Subtype 5 Metabotropic Glutamate Receptor with In Vivo Efficacy

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Web enabling technology for the design, enumeration, optimization and tracking of compound libraries

scientific article published in January 2005

Welcome to Professor Hsin-Yi Lai, the Newest Associate Editor for ACS Chemical Neuroscience

scientific article published on 01 June 2020

Welcome to the DARK Side: DARK Classics in Chemical Neuroscience

scientific article published on 01 October 2018

What Papers Are People Citing and What Are People Reading?

scientific article published on 01 September 2018

Yohimbine Depresses Excitatory Transmission in BNST and Impairs Extinction of Cocaine Place Preference Through Orexin-Dependent, Norepinephrine-Independent Processes.

scientific article published on 15 April 2013

Yohimbine depresses excitatory transmission in BNST and impairs extinction of cocaine place preference through orexin-dependent, norepinephrine-independent processes ⬇️

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cFLIP critically modulates apoptotic resistance in epithelial-to-mesenchymal transition

scientific article published on 25 July 2017

mGlu1 and mGlu5 modulate distinct excitatory inputs to the nucleus accumbens shell

scientific article published on 27 March 2018

mGlu5 positive allosteric modulation normalizes synaptic plasticity defects and motor phenotypes in a mouse model of Rett syndrome

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mGlu7 potentiation rescues cognitive, social, and respiratory phenotypes in a mouse model of Rett syndrome.

scientific article published in August 2017

mGluR4-positive allosteric modulation as potential treatment for Parkinson's disease.

scientific article published on June 2009

mGluR5 positive allosteric modulators facilitate both hippocampal LTP and LTD and enhance spatial learning

scientific article

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