|University of Toledo Health Science Campus
|Pharmaceutical Sciences (Pharmacology/Toxicology)
|Full text PDF:
Drug abuse and addiction is a major problem in the United States. Studies have shown that M5 muscarinic receptors may be a target for the treatment of drug addiction because of their unique locations and functions in the brain reward system. Selective antagonists for M5 muscarinic receptors might be useful in the treatment of drug abuse. GZ-002-05 was identified previously as a novel, M5-selective muscarinic antagonist. Muscarinic receptor selectivity was characterized by measuring the effects of acetylcholine in the presence or absence of the compound using CHO cells expressing human M1, M3, or M5 muscarinic receptors. A [3H] arachidonic acid release assay measured receptor activity and helped delineate the nature of the interaction(s) between the compound and muscarinic receptor subtypes. The results suggest that GZ-002-05 may be very useful as a lead compound in the development of new therapeutic agents for the treatment of drug abuse.