Pesce G, Stefano F J
Acta Physiol Lat Am. 1982;32(2):117-22.
Experiments were designed to study the cardiovascular effects of Bromocriptine (2-Br-alpha-ergocriptine) in the normotensive anesthetized rats. The intravenous administration of bromocriptine (20 micrograms/kg and 200 micrograms/kg) produced a long-lasting and not dose-dependent fall in the mean blood pressure and heart rate. The pressor response to phenylephrine, an alpha adrenergic agonist, was antagonized by bromocriptine in a dose-dependent manner. At a dose of 20 micrograms/kg bromocriptine behaved as a competitive antagonist, whereas at the dose of 200 micrograms/kg produced an insurmountable blockade of the response to phenylephrine. Previous administration of phentolamine (5 mg/kg) prevented the insurmountable blockade of alpha adrenoceptors by bromocriptine. This observation suggests that both drugs compete for the same receptor. It is concluded that blockade of peripheral alpha-adrenoceptors may contribute to cardiovascular effects of bromocriptine.
设计实验研究溴隐亭(2-溴-α-麦角隐亭)对正常血压麻醉大鼠的心血管作用。静脉注射溴隐亭(20微克/千克和200微克/千克)可使平均血压和心率出现持久且非剂量依赖性的下降。溴隐亭以剂量依赖性方式拮抗α肾上腺素能激动剂去氧肾上腺素的升压反应。在20微克/千克的剂量下,溴隐亭表现为竞争性拮抗剂,而在200微克/千克的剂量下,对去氧肾上腺素的反应产生不可克服的阻断作用。预先给予酚妥拉明(5毫克/千克)可防止溴隐亭对α肾上腺素受体产生不可克服的阻断作用。这一观察结果表明两种药物竞争同一受体。得出结论:外周α肾上腺素受体的阻断可能是溴隐亭心血管作用的原因。