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M5 negative allosteric modulator

Development stage
Preclinical
Lead developer
Vanderbilt University
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

The M5 negative allosteric modulator (M5 NAM) is a preclinical small molecule program being developed by the Warren Center for Neuroscience Drug Discovery (WCNDD) at Vanderbilt University, in collaboration with the University of Glasgow. The program focuses on the discovery and optimization of compounds that selectively target the M5 muscarinic acetylcholine receptor to treat substance use disorders, particularly opioid use disorder. By inhibiting M5 receptor signaling through negative allosteric modulation or antagonism, these compounds aim to decrease the reinforcing and addictive properties of opioids without affecting their analgesic efficacy. The program has identified several CNS-penetrant lead compounds, such as the tool compound ML375, and is currently in the lead optimization phase with support from the Wellcome Trust.

Other names
M5 muscarinic receptor negative allosteric modulatorM-5 muscarinic receptor negative allosteric modulatorM 5 muscarinic receptor negative allosteric modulatorM5 NAMM-5 NAMM 5 NAM
02

Targets

CHRM5 (M5)

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