6-（2-苯乙基）尼古丁：一种新型烟碱型胆碱能受体配体。

6-(2-Phenylethyl)nicotine: a novel nicotinic cholinergic receptor ligand.

作者信息

Ramunno Anna, Dukat Małgorzata, Lee Mase, Young Richard, El-Zahabi Mohamed, Damaj M Imad, Martin Billy, Glennon Richard A

机构信息

Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298-0540, USA.

出版信息

Bioorg Med Chem Lett. 2005 Jul 1;15(13):3237-40. doi: 10.1016/j.bmcl.2005.04.072.

DOI:10.1016/j.bmcl.2005.04.072

Abstract

6-(2-Phenylethyl)nicotine (1b; K(i)=15 nM) was unexpectedly found to bind at alpha4beta2 nicotinic cholinergic (nACh) receptors. Although this compound failed to produce nicotine-like agonist action in several functional assays, 1b antagonized the antinociceptive effects of nicotine (mouse tail-flick assay) in a dose-dependent fashion when administered via an intrathecal route.

摘要

意外发现6-(2-苯乙基)尼古丁（1b；K(i)=15纳摩尔）能与α4β2烟碱型胆碱能（nACh）受体结合。尽管该化合物在多项功能试验中未能产生尼古丁样激动剂作用，但当通过鞘内途径给药时，1b能以剂量依赖方式拮抗尼古丁的抗伤害感受作用（小鼠甩尾试验）。

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