List of works - Patrick R Gentry

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

scientific article

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

Crystal structure of the M5 muscarinic acetylcholine receptor

scientific article published on 26 November 2019

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)

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 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 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 ML326: The first sub-micromolar, selective M5 PAM

scientific article

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, Optimization, and Characterization of Novel Subtype-Selective M5 Muscarinic Acetylcholine Receptor Ligands ⬇️

doctoral dissertation

Discovery, synthesis and characterization of a highly muscarinic acetylcholine receptor (mAChR)-selective M5-orthosteric antagonist, VU0488130 (ML381): a novel molecular probe

scientific article (publication date: August 2014)

Drugs for allosteric sites on receptors

scientific article

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

scientific article published on 13 December 2014

Identification of a novel scaffold for a small molecule GPR139 receptor agonist

scientific article published on 07 March 2019

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

scientific article published on February 2010

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

scientific article

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

scientific article published on February 2014

Molecular Mechanisms of Action of M5 Muscarinic Acetylcholine Receptor Allosteric Modulators

scientific article published on 26 July 2016

Novel Allosteric Modulators of G Protein-coupled Receptors

scientific article

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

scientific article

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

scientific article published on 18 July 2009

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

scientific article

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

scientific article

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

scientific article published on October 2009

List of works by Patrick R Gentry

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

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.

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

Crystal structure of the M5 muscarinic acetylcholine receptor

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)

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

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).

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

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

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)

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

Discovery, Optimization, and Characterization of Novel Subtype-Selective M5 Muscarinic Acetylcholine Receptor Ligands ⬇️

Discovery, synthesis and characterization of a highly muscarinic acetylcholine receptor (mAChR)-selective M5-orthosteric antagonist, VU0488130 (ML381): a novel molecular probe

Drugs for allosteric sites on receptors

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

Identification of a novel scaffold for a small molecule GPR139 receptor agonist

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

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

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

Molecular Mechanisms of Action of M5 Muscarinic Acetylcholine Receptor Allosteric Modulators

Novel Allosteric Modulators of G Protein-coupled Receptors

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

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

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

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

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