速激肽拮抗剂I：对平滑肌收缩活性具有特异性、竞争性和组织选择性的神经激肽B拮抗剂。

Tachykinin antagonist I: Specific, competitive and tissue-selective neurokinin B antagonists on contractile activity in smooth muscles.

作者信息

Hashimoto T, Uchida Y, Naminohira S, Sakai T

机构信息

School of Pharmacy, Hokuriku University, Kanazawa, Japan.

出版信息

Jpn J Pharmacol. 1987 Dec;45(4):570-3. doi: 10.1254/jjp.45.570.

DOI:10.1254/jjp.45.570

PMID:3481842

Abstract

Two neurokinin B (NKB) analogs, [Gly6]-NKB [3-10] and [Arg3, D-Ala6]-NKB [3-10], were tested for agonistic activity as well as for their ability to antagonize the myotropic actions of NKB, neurokinin A, substance P, physalaemin and eledoisin in isolated guinea-pig ileum, guinea-pig urinary bladder, rat duodenum, rat vas deferens and rat portal vein. [Gly6]-NKB [3-10] in the guinea-pig ileum and rat portal vein and [Arg3, D-Ala6]-NKB [3-10] in the guinea-pig ileum were found to be the first specific and competitive antagonists against NKB.

摘要

对两种神经激肽B（NKB）类似物，即[甘氨酸6]-NKB[3-10]和[精氨酸3，D-丙氨酸6]-NKB[3-10]，进行了激动活性测试，以及它们在离体豚鼠回肠、豚鼠膀胱、大鼠十二指肠、大鼠输精管和大鼠门静脉中拮抗NKB、神经激肽A、P物质、雨蛙肽和蛙皮素肌动作用的能力测试。发现[甘氨酸6]-NKB[3-10]在豚鼠回肠和大鼠门静脉中，以及[精氨酸3，D-丙氨酸6]-NKB[3-10]在豚鼠回肠中，是首批针对NKB的特异性竞争性拮抗剂。