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

doi:10.1021/jm051196m

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

Research output: Contribution to journal › Article › peer-review

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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 α4β2 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.

Original language	English (US)
Pages (from-to)	2673-2676
Number of pages	4
Journal	Journal of medicinal chemistry
Volume	49
Issue number	9
DOIs	https://doi.org/10.1021/jm051196m
State	Published - May 4 2006
Externally published	Yes

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

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10.1021/jm051196m

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title = "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 α4β2 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.",

author = "Chellappan, {Sheela K.} and Yingxian Xiao and Werner Tueckmantel and Kellar, {Kenneth J.} and Kozikowski, {Alan P.}",

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AU - Xiao, Yingxian

AU - Tueckmantel, Werner

AU - Kellar, Kenneth J.

AU - Kozikowski, Alan P.

PY - 2006/5/4

Y1 - 2006/5/4

N2 - We report the synthesis and pharmacological properties of several cytisine derivatives. Among them, two 10-substituted derivatives showed much higher selectivities for the α4β2 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.

AB - We report the synthesis and pharmacological properties of several cytisine derivatives. Among them, two 10-substituted derivatives showed much higher selectivities for the α4β2 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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Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity

Abstract

ASJC Scopus subject areas

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