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


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.

SUBMITTER: Chellappan SK 

PROVIDER: S-EPMC2504867 | biostudies-literature | 2006 May

REPOSITORIES: biostudies-literature