文章基本信息

标题：EFFECT OF PIPERIDINE AND RELATED ALICYCLIC AMINES ON NICOTINIC AND MUSCARINIC AGONIST BINDING SITES IN THE MAMMALIAN BRAIN
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作者：SHIZUO YAMADA ; YOSHIYUKI KAGAWA ; HIDETO USHIJIMA 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：1986
卷号：9
期号：7
页码：620-625
DOI：10.1248/bpb1978.9.620
出版社：The Pharmaceutical Society of Japan
摘要：The effect of piperidine and related alicyclic amines on central nicotinic and muscarinic cholinoceptors was investigated by measuring specific binding of [³H] nicotine and [³H] cismethyldioxolane (CD) in rat cerebral cortical membranes. Piperidine, pyrrolidine, 4-hydroxypiperidine and piperazine at concentrations of 1μM-30 mM completed dosedependently with [³H] nicotine and [³H] CD for the binding sites. Among these compounds, piperidine was the most potent competitor of brain [³H] nicotine binding sites. Piperidine and pyrrolidine showed a greater affinity for [³H] nicotine binding sites in the rat cerebral cortex than of [³H] CD binding sites. In contrast, 4-hydroxypiperidine and piperazine displayed approximately 10 times greater affinity for [³H] CD binding sites. Pipecolic acid had little effect on these cholinoceptor agonist binding sites. The inhibitory effect of brain [³H] nicotine binding by piperidine did not differ between brain regions or during development. In addition, there was little difference in the piperidine-induced inhibition of brain [³H] nicotine binding between species such as rat, mouse, guinea-pig and rabbit. Thus, the present study demonstrates a high affinity of piperidine for nicotinic cholinoceptors in the mammalian brain.
关键词：[3H] nicotine