选择性内皮素ETA受体拮抗剂BQ-123对用去氧皮质酮-盐处理的自发性高血压大鼠的降压作用。

Antihypertensive effects of BQ-123, a selective endothelin ETA receptor antagonist, in spontaneously hypertensive rats treated with DOCA-salt.

作者信息

Okada M, Fukuroda T, Shimamoto K, Takahashi R, Ikemoto F, Yano M, Nishikibe M

机构信息

Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd., Japan.

出版信息

Eur J Pharmacol. 1994 Jul 11;259(3):339-42. doi: 10.1016/0014-2999(94)90665-3.

DOI:10.1016/0014-2999(94)90665-3

PMID:7982465

Abstract

We determined the antihypertensive effects of BQ-123 (cyclo(D-Trp-D-Asp-L-Pro-D-Val-L-Leu-), sodium salt), a selective endothelin ETA receptor antagonist, in spontaneously hypertensive rats treated with deoxycorticosterone acetate-salt (DOCA-salt SHR). BQ-123 (1-30 mg/kg/h) decreased blood pressure in DOCA-salt SHR in a dose-dependent manner, although plasma immunoreactive endothelin-1 did not significantly increase and the maximal contractile response to endothelin-1 in the aorta significantly decreased as compared with values observed in age-matched SHR. These results suggest that endogenous endothelin-1 is involved in the maintenance of hypertension in DOCA-salt SHR, and that circulating endothelin-1 is not sufficient to reflect the physiological role of endothelin-1.

摘要

我们测定了选择性内皮素ETA受体拮抗剂BQ-123（环（D-色氨酸-D-天冬氨酸-L-脯氨酸-D-缬氨酸-L-亮氨酸-）钠盐）对用醋酸脱氧皮质酮-盐（DOCA-盐SHR）处理的自发性高血压大鼠的降压作用。BQ-123（1 - 30毫克/千克/小时）以剂量依赖的方式降低DOCA-盐SHR的血压，尽管血浆免疫反应性内皮素-1没有显著增加，并且与年龄匹配的SHR相比，主动脉对内皮素-1的最大收缩反应显著降低。这些结果表明，内源性内皮素-1参与了DOCA-盐SHR高血压的维持，并且循环内皮素-1不足以反映内皮素-1的生理作用。