Murphy M B, Weber R R, Nelson K, Goldberg L I
University of Chicago, IL 60637.
Clin Pharmacol Ther. 1988 Jul;44(1):49-55. doi: 10.1038/clpt.1988.111.
Fenoldopam, a dopamine-1 receptor agonist, has been reported to exhibit alpha-adrenoceptor-blocking actions in intact and isolated animal preparations. To determine whether alpha-adrenoceptor blockade contributes to its antihypertensive properties in humans, the effects of fenoldopam on the pressor responses to norepinephrine and angiotensin II were compared in eight normal volunteers. Fenoldopam (0.5 micrograms/kg/min) shifted the dose-response curves for both agonists to the right (p less than 0.05). Dose ratios for an increase in mean blood pressure of 10 mm Hg were 3.3 +/- 0.9 for norepinephrine and 3.2 +/- 0.6 for angiotensin II (p not significant). Consequently, fenoldopam is not a selective alpha-adrenoceptor antagonist at therapeutic concentrations in humans.
非诺多泮是一种多巴胺-1受体激动剂，据报道，在完整和分离的动物制剂中它具有α-肾上腺素能受体阻断作用。为了确定α-肾上腺素能受体阻断是否有助于其在人体中的降压特性，在8名正常志愿者中比较了非诺多泮对去甲肾上腺素和血管紧张素II升压反应的影响。非诺多泮（0.5微克/千克/分钟）使两种激动剂的剂量反应曲线右移（p<0.05）。去甲肾上腺素使平均血压升高10毫米汞柱时的剂量比为3.3±0.9，血管紧张素II为3.2±0.6（p无显著性差异）。因此，在人体治疗浓度下，非诺多泮不是一种选择性α-肾上腺素能受体拮抗剂。
