Márquez M T, Puntoni de Mikulić L E, Aramendía P
Acta Physiol Lat Am. 1977;27(3):102-7.
Ethylephrine, a sympathomimetic amine which belongs to the phenolamine group, was assayed on the driven left rat atrium. The frequency response curve was performed for norepinephrine and ethylephrine. The maxima was attained for both compounds at 1 Hz. The agonist under study has an inotropic action less potent than the classical catecholamines. Propranolol (10(-8) and 10(-7) M) produced a parallel shift to the right in the log dose-response curves of ethylephrine with no decrease in the maximal response, indicating that the antagonism was competitive. In the presence of cocaine or with reserpine-pretreatment the sensitivity of the preparation to the amine did not vary. The alpha-blocker, phentolamine (10(-8) to 3.10(-5) M) did not possess an inotropic effect per se. In contrast, phentolamine, delivered to the bath beforehand, did not block the agonist. However at 10(-8) and 10(-7) M increase the maximal response both in normal and reserpinized preparations. It is suggested that ethylephrine is a direct inotropic preparation. It is suggested that ethylephrine is a direct inotropic agent on the driven left rat atrium and its effects are mediated by beta-receptors. The results also indicate the lack of evidence that ethylephrine has any action on the alpha-receptors.
乙基肾上腺素是一种属于酚胺类的拟交感胺,在离体大鼠左心房上进行了测定。对去甲肾上腺素和乙基肾上腺素进行了频率响应曲线实验。两种化合物在1Hz时均达到最大值。所研究的激动剂的正性肌力作用比经典儿茶酚胺弱。普萘洛尔(10^(-8)和10^(-7)M)使乙基肾上腺素的对数剂量-反应曲线平行右移,最大反应无下降,表明拮抗作用是竞争性的。在可卡因存在或利血平预处理的情况下,制剂对该胺的敏感性没有变化。α受体阻滞剂酚妥拉明(10^(-8)至3×10^(-5)M)本身没有正性肌力作用。相反,预先加入浴槽中的酚妥拉明不会阻断激动剂。然而,在10^(-8)和10^(-7)M时,在正常和利血平化的制剂中均增加最大反应。提示乙基肾上腺素是一种直接正性肌力制剂。提示乙基肾上腺素对离体大鼠左心房是一种直接正性肌力药物,其作用由β受体介导。结果还表明,没有证据表明乙基肾上腺素对α受体有任何作用。