Development of subtype-selective ligands as antagonists at nicotinic receptors mediating nicotine-evoked dopamine release
Development of subtype-selective ligands as antagonists at nicotinic receptors mediating nicotine-evoked dopamine release
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DOI：
10.1016/j.bmcl.2003.10.074
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发表时间：
2004-04-19
影响因子：
2.7
通讯作者：
Dwoskin, LP
中科院分区：
文献类型：
--
作者：
Crooks, PA;Ayers, JT;Dwoskin, LP
尼古丁的N-n-烷基化使其从神经元烟碱乙酰胆碱受体亚型的激动剂转化为拮抗剂，介导尼古丁诱发的多巴胺释放。构象限制的类似物在该位点表现出高亲和力和选择性，并且由于它们作为血脑屏障胆碱转运蛋白的底物的能力而能够进入大脑。(C)2004爱思唯尔有限公司保留所有权利。
N-n-Alkylation of nicotine converts it from an agonist into an antagonist at neuronal nicotinic acetylcholine receptor subtypes mediating nicotine-evoked dopamine release. Conformationally restricted analogues exhibit both high affinity and selectivity at this site, and are able to access the brain due to their ability to act as substrates for the blood-brain barrier choline transporter. (C) 2004 Elsevier Ltd. All rights reserved.