Discovery, Synthesis and Characterization of a Highly Muscarinic Acetylcholine Receptor (mAChR)-Selective M5-Orthosteric Antagonist, VU0488130 (ML381): A Novel Molecular Probe

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

(2013) Patrick R. Gentry et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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)

(2013) Cody J. Wenthur et al.   JOURNAL OF MEDICINAL CHEMISTRY

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)

(2013) Patrick R. Gentry et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structural Modifications to Tetrahydropyridine-3-carboxylate Esters en Route to the Discovery of M5-Preferring Muscarinic Receptor Orthosteric Antagonists

(2013) Guangrong Zheng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Muscarinic Acetylcholine Receptor Subtypes as Potential Drug Targets for the Treatment of Schizophrenia, Drug Abuse, and Parkinson’s Disease

(2011) Ditte Dencker et al.   ACS Chemical Neuroscience

Allosteric Modulation of Seven Transmembrane Spanning Receptors: Theory, Practice, and Opportunities for Central Nervous System Drug Discovery

(2011) Bruce J. Melancon et al.   JOURNAL OF MEDICINAL CHEMISTRY

Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M5 PAM

(2009) Thomas M. Bridges et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of the First Highly M5-Preferring Muscarinic Acetylcholine Receptor Ligand, an M5 Positive Allosteric Modulator Derived from a Series of 5-TrifluoromethoxyN-Benzyl Isatins

(2009) Thomas M. Bridges et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Novel Selective Muscarinic Acetylcholine Receptor Subtype 1 Antagonist Reduces Seizures without Impairing Hippocampus-Dependent Learning

(2009) D. J. Sheffler et al.   MOLECULAR PHARMACOLOGY

Muscarinic receptor blockade in the ventral tegmental area attenuates cocaine enhancement of laterodorsal tegmentum stimulation-evoked accumbens dopamine efflux in the mouse

(2009) Deranda B. Lester et al.   SYNAPSE

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

(2009) P. Jeffrey Conn et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Muscarinic acetylcholine receptors as CNS drug targets

(2007) Christopher J. Langmead et al.   PHARMACOLOGY & THERAPEUTICS