1314801-63-2

AT-1001 is a novel potent and selective partial agonist of human and rat α3β4 nicotinic cholinergic receptors.

AT 1001 is a high-affinity and selective antagonist of the α3β4 nicotinic acetylcholine receptor (α3β4 nAChR) (Ki=2.64 nM). AT 1001 reversibly blocks inward currents induced by Epibatidine (HY-101078) in HEK cells transfected with α3β4 nAChR. AT-1001 dose-dependently inhibits nicotine self-administration behavior in rats without affecting food-reinforced responding. AT 1001 can be utilized in the research of nicotine addiction and smoking cessation therapies[1].

[1] Toll L, et al. AT-1001: a high affinity and selective α3β4 nicotinic acetylcholine receptor antagonist blocks nicotine self-administration in rats[J]. Neuropsychopharmacology, 2012, 37(6): 1367-1376. DOI:10.1038/npp.2011.322