Ferrini R, Miragoli G
Arzneimittelforschung. 1986 Feb;36(2A):312-7.
The pharmacological activity of ibopamine (SB-7505), the 3,4-diisobutyryl ester of N-methyldopamine, was compared with that of epinine (N-methyldopamine) and dopamine on some isolated organs. The results of this study show that ibopamine and epinine exerts a positive inotropic effect on cat papillary muscle by stimulating the cardiac beta 1- and alpha-adrenoceptors; a positive chronotropic effect on cat right atrium by stimulating the cardiac beta 1-adrenoceptors; a relaxing effect on guinea-pig trachea by stimulating beta 2-adrenoceptors; a relaxing effect on rabbit splenic artery pretreated with phenoxybenzamine and contracted with PGF2 alpha by stimulating the DA1 receptors; an inhibitory effect on the vasoconstriction of rabbit ear artery induced by electrical stimuli by stimulating the DA2 receptors. Esterase activation, either by organ or plasma enzymes, appeared to be a prerequisite of ibopamine activity. Suppression of this activity by esterase inhibitors confirmed that the pharmacological responses are related to the formation of epinine. The magnitude and rate of response of some isolated organs to ibopamine appeared to be related to the esterase content of the tissue.
将 N-甲基多巴胺的 3,4-二异丁酯——异波帕明(SB - 7505)的药理活性,与去甲肾上腺素(N-甲基多巴胺)和多巴胺在某些离体器官上的药理活性进行了比较。本研究结果表明,异波帕明和去甲肾上腺素通过刺激心脏β1 - 和α - 肾上腺素能受体,对猫乳头肌产生正性肌力作用;通过刺激心脏β1 - 肾上腺素能受体,对猫右心房产生正性变时作用;通过刺激β2 - 肾上腺素能受体,对豚鼠气管产生舒张作用;通过刺激 DA1 受体,对用酚苄明预处理并用 PGF2α收缩的兔脾动脉产生舒张作用;通过刺激 DA2 受体,对电刺激诱导的兔耳动脉血管收缩产生抑制作用。酯酶激活,无论是由器官酶还是血浆酶引起的,似乎都是异波帕明活性的先决条件。酯酶抑制剂对该活性的抑制证实了药理反应与去甲肾上腺素的形成有关。一些离体器官对异波帕明的反应幅度和速率似乎与组织中的酯酶含量有关。