内皮素-1及BQ123对高血压大鼠小动脉和小静脉的作用。

Effect of endothelin-1 and BQ 123 on arterioles and venules of hypertensive rats.

作者信息

Hergenröder S, Münter K, Kirchengast M

机构信息

Knoll AG, Ludwigshafen, Germany.

出版信息

J Cardiovasc Pharmacol. 1995;26 Suppl 3:S226-9.

PMID:8587371

Abstract

We investigated the effect of the ETA-receptor antagonist BQ 123 (1.0, 5.0, and 10 mg/kg/h i.v.) on the endothelin-1 (ET-1) (10(-8) M)-induced vasoconstriction of arterioles in the cremaster muscle preparation of anesthetized SHRs. ET-1 10(-8) M led to a constriction of the arterial microvessels most marked in A4 arterioles (-92.9%) and least marked in A1 (-17.3%). The ET-1-induced constriction of venules was much less pronounced and showed no dependence on the vessel type. BQ 123 1.0 mg/kg/h was ineffective in antagonizing the vasoconstrictor effect of ET-1 in arterioles. With 5.0 mg/kg/h BQ 123, the ET-1-induced arterial vasoconstriction was inhibited by 68% in A4, by 44% in A3, by 39% in A2, and by 10% in A1 arterioles. BQ 123 10 mg/kg/h blocked the vasoconstrictor effect of ET-1 in all arteriole types by 79-93% and also reduced diastolic blood pressure in SHRs significantly at the end of the infusion period (-12.6 mm Hg). The ET-1-induced slight venous constriction was not affected by BQ 123.

摘要

我们研究了内皮素 A 受体拮抗剂 BQ 123（静脉注射，剂量为 1.0、5.0 和 10 mg/kg/h）对麻醉的自发性高血压大鼠（SHRs）提睾肌制备中内皮素 -1（ET-1）（10⁻⁸ M）诱导的小动脉血管收缩的影响。ET-1（10⁻⁸ M）导致动脉微血管收缩，在 A4 小动脉中最为明显（-92.9%），在 A1 小动脉中最不明显（-17.3%）。ET-1 诱导的小静脉收缩则不太明显，且与血管类型无关。BQ 123 1.0 mg/kg/h 对拮抗 ET-1 在小动脉中的血管收缩作用无效。使用 5.0 mg/kg/h 的 BQ 123 时，ET-1 诱导的动脉血管收缩在 A4 小动脉中被抑制 68%，在 A3 小动脉中被抑制 44%，在 A2 小动脉中被抑制 39%，在 A1 小动脉中被抑制 10%。BQ 123 10 mg/kg/h 在所有类型小动脉中阻断 ET-1 的血管收缩作用达 79% - 93%，并且在输注期结束时还显著降低了 SHRs 的舒张压（-12.6 mmHg）。ET-1 诱导的轻微静脉收缩不受 BQ 123 的影响。