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SR 142801，速激肽NK3受体的首个强效非肽类拮抗剂。

SR 142801, the first potent non-peptide antagonist of the tachykinin NK3 receptor.

作者信息

Emonds-Alt X, Bichon D, Ducoux J P, Heaulme M, Miloux B, Poncelet M, Proietto V, Van Broeck D, Vilain P, Neliat G

机构信息

Sanofi Recherche, Montpellier, France.

出版信息

Life Sci. 1995;56(1):PL27-32. doi: 10.1016/0024-3205(94)00413-m.

DOI:10.1016/0024-3205(94)00413-m
PMID:7830490
Abstract

SR 142801 is the first potent and selective non-peptide antagonist of the tachykinin NK3 receptor. It inhibited [MePhe7]NKB binding to its receptor from various species, including humans. SR 142801 was a competitive antagonist of [MePhe7]NKB-mediated contractions of guinea-pig ileum and inhibited the acetylcholine release following the activation of the guinea-pig ileum tachykinin NK3 receptor. In vivo, SR 142801 potently inhibited the turning behaviour induced by intrastriatal injection of senktide in gerbils, and appears as a powerful tool for investigation of the physiological and pathological role of NKB and its NK3 receptor.

摘要

SR 142801是速激肽NK3受体的首个强效且选择性非肽拮抗剂。它抑制了[甲基苯丙氨酸7]神经激肽B（[MePhe7]NKB）与包括人类在内的多种物种的受体结合。SR 142801是[MePhe7]NKB介导的豚鼠回肠收缩的竞争性拮抗剂，并抑制豚鼠回肠速激肽NK3受体激活后乙酰胆碱的释放。在体内，SR 142801能有效抑制沙土鼠纹状体内注射senktide诱导的旋转行为，并且似乎是研究神经激肽B及其NK3受体的生理和病理作用的有力工具。

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