Journal of Medicinal Chemistry 2006-05-04

Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity.

Sheela K Chellappan, Yingxian Xiao, Werner Tueckmantel, Kenneth J Kellar, Alan P Kozikowski

Index: J. Med. Chem. 49 , 2673-2676, (2006)

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Abstract

We report the synthesis and pharmacological properties of several cytisine derivatives. Among them, two 10-substituted derivatives showed much higher selectivities for the alpha4beta2 nAChR subtype in binding assays than cytisine. The 9-vinyl derivative was found to have a very similar agonist activity profile to that of cytisine.

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