Schwinger R H, Schulz C, Brixius K, Böhm M, Müller-Ehmsen J, Erdmann E
Klinik III für Innere Medizin, Universität zu Köln, Germany.
Naunyn Schmiedebergs Arch Pharmacol. 1996 Aug-Sep;354(3):343-7. doi: 10.1007/BF00171066.
The present study aimed to characterize the effects of epinine, the active metabolite of ibopamine on tension development in human renal arteries.
Experiments were performed on isolated human renal arteries rings obtained during surgery due to kidney tumors (n = 12). Epinine concentration-dependently relaxed isolated precontracted (PGF2 alpha) human renal artery rings (P < 0.05) in the presence of phentolamine, as effectively (epinine -30 +/- 4 mN, dopamine -31 +/- 5 mN) and with the same potency as dopamine (epinine EC50 0.7 mumol/l (0.4-1.2 mumol/l), dopamine 0.5 mumol/l (0.2-1.7 mumol/l). This effect was antagonized by the specific D1-receptor-antagonist SCH 23390. Effective beta-adrenoceptor antagonistic concentrations of propranolol did not affect epinine-induced vasorelaxation. In the absence of alpha- and beta-adrenoceptor-antagonists the potency of epinine to contract renal artery rings was significantly higher compared to dopamine indicating a higher affinity of epinine to alpha-adrenoceptors.
The present study provides evidence for direct vasodilatory effects of epinine via activation of D1-receptors on human renal arteries.
本研究旨在描述异波帕胺的活性代谢产物依匹宁对人肾动脉张力发展的影响。
对因肾肿瘤手术获取的离体人肾动脉环进行实验（n = 12）。在酚妥拉明存在的情况下，依匹宁浓度依赖性地舒张离体预收缩（前列腺素F2α）的人肾动脉环（P < 0.05），其效果（依匹宁 -30 ± 4 mN，多巴胺 -31 ± 5 mN）与多巴胺相同，且效力相当（依匹宁 EC50 为0.7 μmol/l（0.4 - 1.2 μmol/l），多巴胺为0.5 μmol/l（0.2 - 1.7 μmol/l））。这种效应被特异性D1受体拮抗剂SCH 23390拮抗。普萘洛尔的有效β肾上腺素能受体拮抗浓度不影响依匹宁诱导的血管舒张。在不存在α和β肾上腺素能受体拮抗剂的情况下，依匹宁收缩肾动脉环的效力显著高于多巴胺，表明依匹宁对α肾上腺素能受体的亲和力更高。
本研究为依匹宁通过激活人肾动脉上的D1受体产生直接血管舒张作用提供了证据。
