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非肽类NK-2拮抗剂SR 48968在豚鼠中也是一种NK-3拮抗剂,但在大鼠中则不是。

The nonpeptide NK-2 antagonist SR 48968 is also a NK-3 antagonist in the guinea but not in the rat.

作者信息

Petitet F, Beaujouan J C, Saffroy M, Torrens Y, Glowinski J

机构信息

Collège de France, INSERM U 114, Paris.

出版信息

Biochem Biophys Res Commun. 1993 Feb 26;191(1):180-7. doi: 10.1006/bbrc.1993.1200.

Abstract

SR 48968 was first described as a NK-2 nonpeptide receptor antagonist; we report here that SR 48968 interacts also with guinea pig but not rat NK-3 cortical binding sites. Furthermore, SR 48968 is shown to inhibit the senktide- (a NK-3 selective agonist) evoked stimulation of phosphoinositide turnover in guinea pig ileum slices. The species difference observed for the NK-3 receptor with SR 48968 was confirmed by the determination of the affinities of NK-3 peptide agonists. [Pro7]neurokinin B particularly was found to have a greater affinity for cortical NK-3 binding sites in the rat than in the guinea pig.

摘要

SR 48968最初被描述为一种NK-2非肽受体拮抗剂;我们在此报告,SR 48968还与豚鼠而非大鼠的NK-3皮质结合位点相互作用。此外,已表明SR 48968可抑制senktide(一种NK-3选择性激动剂)诱发的豚鼠回肠切片中磷酸肌醇代谢的刺激。通过测定NK-3肽激动剂的亲和力,证实了SR 48968在NK-3受体上观察到的物种差异。特别是发现[Pro7]神经激肽B对大鼠皮质NK-3结合位点的亲和力比对豚鼠的更大。

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