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Quantitative structure-activity relationships of nicotine analogues as neuronal nicotinic acetylcholine receptor
K H Kim1, N H Lin, D J Anderson
1Pharmaceutical Products Division, Abbott Laboratories, IL 60064, USA.
Bioorganic & Medicinal Chemistry
|December 1, 1996
Abstract:
Quantitative structure-activity relationships of 34 pyrrolidine-modified nicotine agonists are investigated for their binding affinity toward neuronal nicotinic acetylcholine receptor. The results indicate that a large substituent at the R1, R2, and R3 position is detrimental to the binding affinity. Likewise, a large substituent at the R2 alpha or R3 alpha position as well as a hydrogen bond accepting substituent at the R2 beta position are not beneficial to the binding.