依那普利拉与选定的α-肾上腺素能受体拮抗剂在离体大鼠尾动脉中的相互作用。

The interaction between enalaprilat and selected alpha-adrenoceptor antagonists in isolated rat tail arteries.

Marwood J F

Clinical Pharmacology Department, Royal North Shore Hospital, St Leonards, New South Wales, Australia.

Clin Exp Pharmacol Physiol. 1994 May;21(5):417-25. doi: 10.1111/j.1440-1681.1994.tb02536.x.

Abstract

Isolated perfused rat tail artery preparations were used to investigate the effects of the angiotensin converting enzyme inhibitor enalaprilat on the actions of a series of alpha-adrenoceptor antagonists. The agonist used was phenylephrine. 2. Enalaprilat (1 mumol/L) potentiated the competitive alpha 1-adrenoceptor antagonist actions of phentolamine (10-100 nmol/L) and yohimbine (0.3-3.0 mumol/L) as well as the non-competitive antagonist action of phenoxybenzamine (50-100 pmol/L). 3. The competitive alpha 1-adrenoceptor antagonist action of prazosin (1-10 nmol/L) was not affected by enalaprilat. 4. For the competitive alpha 1-adrenoceptor antagonists, including prazosin, there appeared to be an inverse relationship between antagonist potency and the extent of potentiation by enalaprilat. 5. The results support the hypothesis and angiotensin II modulates vascular smooth muscle alpha 1-adrenoceptor function.

摘要

采用离体灌注大鼠尾动脉标本，研究血管紧张素转换酶抑制剂依那普利拉对一系列α-肾上腺素能受体拮抗剂作用的影响。所用激动剂为去氧肾上腺素。
依那普利拉（1 μmol/L）增强了酚妥拉明（10 - 100 nmol/L）和育亨宾（0.3 - 3.0 μmol/L）的竞争性α1-肾上腺素能受体拮抗剂作用，以及酚苄明（50 - 100 pmol/L）的非竞争性拮抗剂作用。
依那普利拉不影响哌唑嗪（1 - 10 nmol/L）的竞争性α1-肾上腺素能受体拮抗剂作用。
对于包括哌唑嗪在内的竞争性α1-肾上腺素能受体拮抗剂，拮抗剂效价与依那普利拉增强作用的程度之间似乎呈负相关。
这些结果支持血管紧张素II调节血管平滑肌α1-肾上腺素能受体功能这一假说。