Miyagishi A, Nakahara H, Hara Y, Nakatani H
Arch Int Pharmacodyn Ther. 1983 Feb;261(2):222-37.
The effects of the new beta-adrenoceptor blocking agent, S-596, on the peripheral autonomic nervous system and smooth muscles were studied in comparison with propranolol. In urethane or alpha-chloralose anesthetized cats S-596 (10 micrograms/kg, i.v.) antagonized the cardiovascular responses induced by isoproterenol. S-596, in doses ranging from 100 to 300 micrograms/kg (i.v.) reduced the contractions of the nictitating membrane induced by electrical stimulation of preganglionic and postganglionic fibers to the superior cervical ganglion. Higher doses of S-596 were required to depress the effects of noradrenaline and tyramine. In spinal cats the tyramine and noradrenaline dose-response curve was shifted to the right by S-596. In isolated rat aortic strips S-596 displaced the noradrenaline dose-response curve to the right in a parallel fashion indicating a competitive antagonism. Its potency was about one tenth of that of phentolamine. These results suggest that S-596 possesses both alpha-and beta-adrenoceptor blocking activities.
将新型β-肾上腺素能受体阻滞剂S-596与普萘洛尔相比，研究了其对外周自主神经系统和平滑肌的作用。在氨基甲酸乙酯或α-氯醛糖麻醉的猫中，S-596（10微克/千克，静脉注射）可拮抗异丙肾上腺素引起的心血管反应。静脉注射剂量为100至300微克/千克的S-596可减少电刺激颈上神经节节前和节后纤维所诱导的瞬膜收缩。需要更高剂量的S-596才能抑制去甲肾上腺素和酪胺的作用。在脊髓猫中，S-596使酪胺和去甲肾上腺素的剂量反应曲线右移。在离体大鼠主动脉条中，S-596使去甲肾上腺素的剂量反应曲线平行右移，表明存在竞争性拮抗作用。其效力约为酚妥拉明的十分之一。这些结果表明S-596具有α和β肾上腺素能受体阻断活性。
