氟哌利多对离体平滑肌的特异性α-肾上腺素能受体阻断作用。

Specific alpha-adrenoceptor blocking effect of droperidol on isolated smooth muscles.

作者信息

van Nueten J M, Reneman R S, Janssen P A

出版信息

Eur J Pharmacol. 1977 Jul 1;44(1):1-8. doi: 10.1016/0014-2999(77)90109-1.

Abstract

The present study was conducted so as to obtain more insight into the controversies concerning the alpha-adrenoceptor blocking properties of droperidol, a short-acting neuroleptic agent used in neuroleptanalgesia. The effect of droperidol on the vasoconstriction induced by norepinephrine, sympathetic nerve stimulation, histamine and potassium ions was studied on isolated, perfused ear arteries; its effect on norepinephrine-induced contraction was studied on isolated aorta, spleen and vas deferens. In addition, the onset and duration of action of droperidol was studied. Low doses of droperidol inhibit the vasoconstriction induced by norepinephrine and sympathetic nerve stimulation in the ear artery of the rabbit (3.3 X 10(-9) M and 1.3 X 10(-8) M respectively). At similar low doses, droperidol inhibits norepinephrine-induced contractions in the other tissues studied and has a potency comparable to that of phentolamine; its action is rapid in onset and of short duration. High doses of droperidol (10(-6) M) also inhibit the vasoconstriction of the ear artery induced by histamine and by potassium ions. These findings indicate that a low doses, droperidol has specific and competitive alpha-adrenoceptor blocking effects.

摘要

本研究旨在更深入地了解有关氟哌利多（一种用于神经安定镇痛的短效抗精神病药物）α-肾上腺素能受体阻断特性的争议。在离体灌注的兔耳动脉上研究了氟哌利多对去甲肾上腺素、交感神经刺激、组胺和钾离子诱导的血管收缩的影响；在离体主动脉、脾脏和输精管上研究了其对去甲肾上腺素诱导的收缩的影响。此外，还研究了氟哌利多的起效时间和作用持续时间。低剂量的氟哌利多可抑制兔耳动脉中去甲肾上腺素和交感神经刺激诱导的血管收缩（分别为3.3×10⁻⁹ M和1.3×10⁻⁸ M）。在类似的低剂量下，氟哌利多可抑制去甲肾上腺素在其他研究组织中诱导的收缩，其效力与酚妥拉明相当；其作用起效迅速且持续时间短。高剂量的氟哌利多（10⁻⁶ M）也可抑制组胺和钾离子诱导的兔耳动脉血管收缩。这些发现表明，低剂量时，氟哌利多具有特异性和竞争性α-肾上腺素能受体阻断作用。