Drug intelligence / Profile preview

VU0255035

Development stage
Preclinical
Lead developer
Vanderbilt University
Modality
Small Molecules
Administration
Intraperitoneal (in Research Studies)
01

Overview

VU0255035 is a highly selective, competitive muscarinic acetylcholine receptor subtype 1 (M1) antagonist with a Ki of approximately 14.87 nM and more than 75-fold selectivity over other muscarinic receptor subtypes. It acts at the orthosteric binding site of the M1 receptor, effectively blocking M1-mediated signaling. VU0255035 displays excellent brain penetration and reduces pilocarpine-induced seizures in animal models without the severe cognitive side effects typically seen with non-selective muscarinic antagonists. This compound has been used primarily as a research tool for studying the role of M1 receptors in central nervous system disorders, particularly seizures and epilepsy[1][3][5][7][9][10].

Other names
N-[3-Oxo-3-[4-(4-pyridinyl)-1-piperazinyl]propyl]-2,1,3-benzothiadiazole-4-sulfonamide
02

Targets

M1 (Muscarinic acetylcholine receptor M1)

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