Himori N, Izumi A, Ishimori T
Eur J Pharmacol. 1978 Feb 1;47(3):341-50. doi: 10.1016/0014-2999(78)90242-x.
The effect of alprenolol and other beta-adrenoceptor antagonists, including d-isomers, on blood flow in femoral, coronary and mesenteric vascular beds was measured in anesthetized dogs. Under conditions of constant perfusion pressure, intra-arterial injection of beta-adrenoceptor antagonists produced vasodilation. Propranolol and alprenolol were approximately equipotent in coronary and mesenteric beds but alprenolol was significantly more potent in the femoral bed. Practolol was virtually inactive in all beds. The vasodilating potency of d-alprenolol and d-propranolol was not significantly different from that of the respective racemic mixtures. The vasodilator response to alprenolol was not affected by pretreatment with atropine, diphenhydramine or propranolol. In conscious normotensive dogs i.v. injections of d,l- and d-alprenolol produced dose-dependent decreases in blood pressure and increases in heart rate. Under similar conditions, i.v. d,l-propranolol was without effect on either measurement. The results suggest that the hypotensive action of alprenolol in dogs may derive from its vasodilator activity.
在麻醉犬身上测量了阿普洛尔及其他β-肾上腺素受体拮抗剂(包括d-异构体)对股动脉、冠状动脉和肠系膜血管床血流量的影响。在恒定灌注压力条件下,动脉内注射β-肾上腺素受体拮抗剂可引起血管舒张。普萘洛尔和阿普洛尔在冠状动脉和肠系膜血管床中的作用大致相当,但阿普洛尔在股动脉血管床中的作用明显更强。醋丁洛尔在所有血管床中几乎没有活性。d-阿普洛尔和d-普萘洛尔的血管舒张效力与各自的外消旋混合物没有显著差异。阿普洛尔引起的血管舒张反应不受阿托品、苯海拉明或普萘洛尔预处理的影响。在清醒的正常血压犬中,静脉注射d,l-阿普洛尔和d-阿普洛尔可引起剂量依赖性的血压下降和心率增加。在类似条件下,静脉注射d,l-普萘洛尔对这两项测量均无影响。结果表明,阿普洛尔在犬体内的降压作用可能源于其血管舒张活性。