A NOVEL ENDOTHELIN ET(A) RECEPTOR ANTAGONIST, BQ-485, AND ITS PREVENTIVE EFFECT ON EXPERIMENTAL CEREBRAL VASOSPASM IN DOGS

被引：99

作者：

ITOH, S ^{[1
]}

SASAKI, T ^{[1
]}

IDE, K ^{[1
]}

ISHIKAWA, K ^{[1
]}

NISHIKIBE, M ^{[1
]}

YANO, M ^{[1
]}

机构：

[1] BANYU PHARMACEUT CO LTD, TSUKUBA RES INST, IBARAKI 30033, JAPAN

来源：

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS | 1993年 / 195卷 / 02期

关键词：

D O I：

10.1006/bbrc.1993.2139

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：

Because endothelin-1 has a potent and long-lasting vasoconstrictive action, it has been proposed that it plays some important roles in the pathogenesis of delayed cerebral vasospasm following subarachnoid hemorrhage. We examined the preventive effect of a novel ETA receptor antagonist, BQ-485, on experimental vasospasm using canine two-hemorrhage model of subarachnoid hemorrhage. The IC50 value of BQ-485 on [125I]endothelin-1 binding was 3.4×10-9 M for ETA receptor and 26×10-6 M for ETB receptor. Systemic continuous administration of 120 mg/day of the agent inhibited the narrowing of canine basilar artery on day 7 following experimental subarachnoid hemorrhage (75.0% vs 59.9% (control), p<0.01). The present results suggest that endothelin-1 and ETA receptor participate in the pathogenesis of delayed cerebral vasospasm. © 1993 Academic Press, Inc.

引用

页码：969 / 975

页数：7

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