THE NONPEPTIDE NK-2 ANTAGONIST SR 48968 IS ALSO A NK-3 ANTAGONIST IN THE GUINEA-PIG BUT NOT IN THE RAT

被引:57
作者
PETITET, F [1 ]
BEAUJOUAN, JC [1 ]
SAFFROY, M [1 ]
TORRENS, Y [1 ]
GLOWINSKI, J [1 ]
机构
[1] COLL FRANCE, CHAIR NEUROPHARMACOL, INSERM, U114, 11 PL MARCELIN BERTHELOT, F-75231 PARIS 05, FRANCE
关键词
D O I
10.1006/bbrc.1993.1200
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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. © 1993 Academic Press.
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收藏
页码:180 / 187
页数:8
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