SPECIES-DIFFERENCE IN THE BINDING CHARACTERISTICS OF RES-701-1 - POTENT ENDOTHELIN ET(B) RECEPTOR-SELECTIVE ANTAGONIST

被引：16

作者：

TANAKA, T ^{[1
]}

OGAWA, T ^{[1
]}

MATSUDA, Y ^{[1
]}

机构：

[1] KYOWA HAKKO KOGYO CO LTD,TOKYO RES LABS,MACHIDA,TOKYO 194,JAPAN

来源：

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS | 1995年 / 209卷 / 02期

关键词：

D O I：

10.1006/bbrc.1995.1557

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：

Species-dependency of RES-701-1 (cyclic (Gly1-Asp(9)) (Gly-Asn-Trp-His-Gly-Thr-Ala-Pro-Asp-Trp-Phe-Phe-Asn-Tyr-Tyr-Trp)) has been shown using I-125-ET-1 binding to membranes from various animal tissues. RES-701-1 selectively inhibited the I-125-ET-1 binding to ET(B) receptor from canine, rabbit, porcine, and guinea pig lung tissues in a dose-dependent manner with IC50 values of 60 nM, 20, 4 nM and 13 nM, respectively. Though RES-701-1 retained selectivity for ETB receptor even at higher concentrations, RES-701-1 inhibited the I-125-ET-1 binding to ET(B) receptor from rat lung, heart, and kidney only weakly; IC50 values were calculated to be 1.2 mu M, 0.9 mu M and 0.6 mu M, respectively. These results suggest that RES-701-1 is a potent and specific antagonist for ET(B) receptor in various species of animal, and would be a powerful tool for understanding the physiological roles of ETB receptor, but care must be taken in use of RES-701-1 in experiments with rat. (C) 1995 Academic Press, Inc.

引用

页码：712 / 716

页数：5