ACTIVITY OF SPANTIDE-I AND SPANTIDE-II AT VARIOUS TACHYKININ RECEPTORS AND NK-2 TACHYKININ RECEPTOR SUBTYPES

被引:24
作者
MAGGI, CA [1 ]
PATACCHINI, R [1 ]
FENG, DM [1 ]
FOLKERS, K [1 ]
机构
[1] UNIV TEXAS,INST BIOMED RES,AUSTIN,TX 78712
关键词
TACHYKININS; NK-1; RECEPTORS; TACHYKININ RECEPTOR SUBTYPES; PULMONARY ARTERY (RABBIT); TRACHEA (HAMSTER); (COMPETITIVE ANTAGONISTS);
D O I
10.1016/0014-2999(91)90648-A
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
We compared the ability of spantide I and II to antagonize tachykinins in monoreceptor bioassays. Both peptides antagonized the response to substance P methylester in the guinea-pig ileum (NK-1 receptor-mediated) with greater affinity than the responses mediated by NK-2 or NK-3 receptors in other bioassays. Spantide II was about 10 times more potent than spantide I as an NK-1 antagonist and also possessed some selectivity for the NK-2 receptor subtype present in the hamster trachea. Spantide II is a suitable tool to assess the role of NK-1 receptors in the central and peripheral nervous system.
引用
收藏
页码:127 / 129
页数:3
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