Göthert M, Thies F K, Veth N
Arch Int Pharmacodyn Ther. 1976 Dec;224(2):199-214.
The influence of droperidol on the pressor effect of noradrenaline was investigated in pithed rats injected with propranolol. Droperidol induced a dose-dependent shift of the noradrenaline dose-response curve to the right, but proved to be 20 times less potent than phentolamine. Droperidol produced a considerably more pronounced inhibition of the effect of tyramine than of that of noradrenaline.--The influence of droperidol on the increase in tension induced by noradrenaline was determined in isolated aortic strips of rats. The drug caused a marked parallel shift of the noradrenaline concentration-response curve to the right (pA2:7.99). In this preparation droperidol and phentolamine were equieffective.--Droperidol did not produce a significant shift of the noradrenaline concentration-response curves obtained for the positive chronotropic and inotropic effects in spontaneously beating right guinea-pig atria and in electrically driven left atria, respectively.--It is concluded that droperidol is a competitive inhibitor of the vascular alpha-adrenoceptors, leaving the beta-adrenoceptors of the heart unaffected, and that it inhibits the neuronal uptake mechanism of noradrenaline.
在注射了普萘洛尔的脊髓麻醉大鼠中，研究了氟哌利多对去甲肾上腺素升压作用的影响。氟哌利多使去甲肾上腺素剂量 - 反应曲线呈剂量依赖性向右移位，但证明其效力比酚妥拉明低20倍。与去甲肾上腺素相比，氟哌利多对酪胺作用的抑制作用更为明显。——在大鼠离体主动脉条中测定了氟哌利多对去甲肾上腺素所致张力增加的影响。该药物使去甲肾上腺素浓度 - 反应曲线明显平行向右移位（pA2：7.99）。在此实验准备中，氟哌利多和酚妥拉明效果相当。——氟哌利多分别对豚鼠自发性搏动的右心房和电驱动的左心房中去甲肾上腺素引起的正性变时和变力作用所获得的浓度 - 反应曲线未产生明显移位。——得出的结论是，氟哌利多是血管α - 肾上腺素能受体的竞争性抑制剂，对心脏的β - 肾上腺素能受体无影响，并且它抑制去甲肾上腺素的神经元摄取机制。
