RGNCY-0019 (VUO467154 - M4 Receptor Agonist)

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Allosteric activators of the M4 muscarinic acetylcholine receptor represent a novel approach for the treatment of psychotic symptoms associated with schizophrenia and other neuropsychiatric disorders.  VU0467154 produced a robust dose-dependent reversal of MK-801-induced hyperlocomotion and deficits in preclinical models of associative learning and memory functions in wild-type mice, but failed to reverse these stimulant-induced deficits in M4 KO mice. VU0467154 also enhanced the acquisition of both contextual and cue-mediated fear conditioning when administered alone in wild-type mice.

Systematic Name: 5-amino-3,4-dimethyl-N-(4-((trifluoromethyl)sulfonyl)benzyl)thieno[2,3-c]pyridazine-6-carboxamide

SMILES: O=S(C1=CC=C(C=C1)CNC(C2=C(N)C3=C(C)C(C)=NN=C3S2)=O)(C(F)(F)F)=O

Molecular Weight: 444.45

Formula: C17H15F3N4O3S2

PMID: 25137629

Reference: Bubser, Michael et. al. "Selective Activation of M4 Muscarinic Acetylcholine Receptors Reverses MK-801-Induced Behavioral Impairments and Enhances Associative Learning in Rodents" ACS Clinical Neuroscience 5 (2014): 920 - 942

Data Sheet


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Tags: M4, RGNCY-0019, VUO467154, Receptor, Muscarinic, Psychosis, MK-801, Learning, Memory