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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-other | 2006 May

REPOSITORIES: biostudies-other

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

Chellappan Sheela K SK Xiao Yingxian Y Tueckmantel Werner W Kellar Kenneth J KJ Kozikowski Alan P AP

Journal of medicinal chemistry 20060501 9

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. ...[more]

PMID: 16640326

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