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Nicotinic acetylcholine receptor a4b2

Pharmacological and rat studies suggest the
sazetidine A derivative VMY-2-95 could aid smoking cessation. Sazetidine A selectively desensitizes nicotinic acetylcholine receptor a4b2. Chemical modification of sazetidine produced a lead compound, VMY-2-95, with receptor selectivity, affinity and desensitization efficiency similar to those for sazetidine A but with greater blood brain barrier penetration. In a rat model of nicotine addiction, subcutaneously injected
VMY-2-95 decreased nicotine self-administration compared with saline control (p<0.05). Next steps include scale up of VMY-2-95 synthesis to complete preclinical studies for a pre-IND package in smoking cessation.

SciBX 6(40); doi:10.1038/scibx.2013.1135
Published online Oct. 17, 2013

Patent application filed; available for licensing

Yenugonda, V.M. et al. J. Med. Chem.; published Sept. 18, 2013;
Contact: Milton L. Brown, Georgetown University School of Medicine, Washington, D.C.