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[N-甲基野靛碱——中枢神经系统中乙酰胆碱烟碱受体的选择性配体]

[N-methylcytisine--a selective ligand of nicotinic receptors of acetylcholine in the CNS].

作者信息

Pliashkevich Iu G, Demushkin V P

出版信息

Biull Eksp Biol Med. 1987 Dec;104(12):690-2.

PMID:3689962
Abstract

The ability of cytisine and its N-methyl derivatives to bind to nicotinic acetylcholine receptors (nAChR) from different tissues was studied. Cytisine and N-methylcytisine have high affinity (KD = 50 nM) to nAChR from squid optical ganglia. N,N-dimethylcytisine did not show high affinity to this receptor. In the case of nAChR from T. marmorata, cytisine was the only effective inhibitor of 14C-tubocurarine specific binding (Ki = 700 nM). N-methyl- and N,N-dimethylcytisine did not displace 14C-tubocurarine at a concentration of 0.1 mM. The results obtained indicate that there are some differences in the structure of nAChR binding sites from squid and T. marmorata optical ganglia.

摘要

研究了金雀花碱及其N-甲基衍生物与不同组织烟碱型乙酰胆碱受体(nAChR)结合的能力。金雀花碱和N-甲基金雀花碱对鱿鱼视神经节的nAChR具有高亲和力(KD = 50 nM)。N,N-二甲基金雀花碱对该受体未显示出高亲和力。对于大理石纹背鲈的nAChR,金雀花碱是14C-筒箭毒碱特异性结合的唯一有效抑制剂(Ki = 700 nM)。N-甲基和N,N-二甲基金雀花碱在0.1 mM浓度下不能取代14C-筒箭毒碱。所得结果表明,鱿鱼和大理石纹背鲈视神经节的nAChR结合位点结构存在一些差异。

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