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一种非肽类P物质（NK1）受体拮抗剂在大脑中的结合位点活性与分布

Activity and distribution of binding sites in brain of a nonpeptide substance P (NK1) receptor antagonist.

作者信息

McLean S, Ganong A H, Seeger T F, Bryce D K, Pratt K G, Reynolds L S, Siok C J, Lowe J A, Heym J

机构信息

Department of Neuroscience, Central Research Division, Pfizer Inc., Groton, CT 06340.

出版信息

Science. 1991 Jan 25;251(4992):437-9. doi: 10.1126/science.1703324.

DOI:10.1126/science.1703324
PMID:1703324
Abstract

CP-96,345, a nonpeptide substance P antagonist, is selective for the tachykinin NK1 receptor. The compound binds to a single population of sites in guinea pig brain and potently inhibits substance P-induced excitation of locus ceruleus neurons. CP-96,345 should be a useful tool for studying the action of substance P in the central nervous system.

摘要

CP-96,345是一种非肽类P物质拮抗剂，对速激肽NK1受体具有选择性。该化合物与豚鼠脑内单一的位点群结合，并有效抑制P物质诱导的蓝斑神经元兴奋。CP-96,345应是研究P物质在中枢神经系统中作用的有用工具。

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Activity and distribution of binding sites in brain of a nonpeptide substance P (NK1) receptor antagonist.一种非肽类P物质（NK1）受体拮抗剂在大脑中的结合位点活性与分布
Science. 1991 Jan 25;251(4992):437-9. doi: 10.1126/science.1703324.
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The substance P receptor antagonist CP-96,345 interacts with Ca2+ channels.P物质受体拮抗剂CP-96,345与钙离子通道相互作用。
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Tachykinin NK1 receptor in the guinea-pig isolated proximal urethra: characterization by receptor selective agonists and antagonists.豚鼠离体近端尿道中的速激肽NK1受体：用受体选择性激动剂和拮抗剂进行特性研究
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A potent nonpeptide antagonist of the substance P (NK1) receptor.一种有效的P物质（NK1）受体非肽拮抗剂。
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Two nonpeptide tachykinin antagonists act through epitopes on corresponding segments of the NK1 and NK2 receptors.两种非肽类速激肽拮抗剂通过NK1和NK2受体相应片段上的表位发挥作用。
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Phylogeny of tachykinin receptor localization in the vertebrate central nervous system: apparent absence of neurokinin-2 and neurokinin-3 binding sites in the human brain.脊椎动物中枢神经系统中速激肽受体定位的系统发育：人脑中明显不存在神经激肽-2和神经激肽-3结合位点。
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Species differences between [3H] substance P binding in rat and guinea-pig shown by the use of peptide agonists and antagonists.使用肽激动剂和拮抗剂显示大鼠和豚鼠中[3H]P物质结合的种属差异。
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Radioiodinated substance P, neurokinin A, and eledoisin bind predominantly in NK1 receptors in guinea pig lung.放射性碘化P物质、神经激肽A和eledoisin主要结合于豚鼠肺中的NK1受体。
Mol Pharmacol. 1992 Jan;41(1):147-53.
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Inhibition of neurogenic plasma exudation in guinea-pig airways by CP-96,345, a new non-peptide NK1 receptor antagonist.新型非肽类NK1受体拮抗剂CP-96,345对豚鼠气道神经源性血浆渗出的抑制作用
Br J Pharmacol. 1992 Feb;105(2):261-2. doi: 10.1111/j.1476-5381.1992.tb14243.x.

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