Work

Synthesis and Pharmacological Evaluation of Novel 9- and 10-Substituted Cytisine Derivatives. Nicotinic Ligands of Enhanced Subtype Selectivity

Year: 2006

Type: article

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.

Source: Journal of Medicinal Chemistry

DOI: 10.1021/jm051196m

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

Institutions: Georgetown University, University of Illinois Chicago

Language: English

Topic: Nicotinic Acetylcholine Receptors Study

Subfield: Molecular Biology

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: green

Funder: National Institute on Drug Abuse