ACS chemical neuroscience
Discovery of VU6025733 (AG06827): A Highly Selective, Orally Bioavailable, and Structurally Distinct M4 Muscarinic Acetylcholine Receptor Positive Allosteric Modulator (PAM) with Robust In Vivo Efficacy.
Alison R Gregro, Charlotte Park, Madeline F Long, Logan A Baker, Katrina A Bollinger, Anna E Ringuette, Li Peng, Vincent B Luscombe, Natasha B Billard, Alice L Rodriguez, Colleen M Niswender, Weimin Peng, Jonathan W Dickerson, Jerri M Rook, Jordan O'Neill
Published: 202610.1021/acschemneuro.5c00963
Abstract
This work describes progress toward an M4 PAM preclinical candidate. The SAR to address potency, clearance, subtype selectivity, CNS exposure, and P-gp efflux are detailed within. A novel 1-(7,8-dimethyl-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin…
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