Estañ L, Martinez-Mir I, Rubio E, Morales-Olivas F J
Departament de Farmacologia i Farmacotecnia, Facultat de Medicina, Universitat de Valencia, Spain.
Naunyn Schmiedebergs Arch Pharmacol. 1988 Nov;338(5):484-8. doi: 10.1007/BF00179318.
The effect of dopamine was studied on the isolated uterus of diethylstilboestrol-treated rats. Dopamine, at concentrations (10(7)-10(-4) M) produced a concentration-dependent relaxation in the K+-depolarized rat uterus. On a molar basis, dopamine was about 500 times less potent than adrenaline in relaxing the uterus, the maximum degree of relaxation obtained with both drugs was the same. Pretreatment of the rats with reserpine (5 mg/kg) did not produce any modification of the dose-response curve to dopamine. Similarly, cocaine (3 x 10(-6) M) failed to modify the relaxant effect of dopamine. The dopamine induced relaxation was inhibited by propranolol (10(-9)-10(-7) M) in a dose-dependent manner. Prazosin (10(-7) M), SCH 23390 (10(-7) M) and sulpiride (10(-7) M) did not affect the dopamine dose-response curve. In the isolated rat uterus which was not preconstricted by KCl neither dopamine nor adrenaline produced any effect when added to the organ bath. This lack of response to both catecholamines was present even in tissues pretreated with propranolol or sulpiride. It is concluded that dopamine produced a concentration-dependent relaxation of the uterus from diethylstilboestrol-treated rats by direct activation of beta-adrenoceptors. There was no evidence for indirect action (catecholamine release and neuronal uptake mechanisms) and specific dopamine receptor mediated relaxation and alpha-adrenoceptor mediated contractions have not been found in this preparation.
研究了多巴胺对己烯雌酚处理过的大鼠离体子宫的作用。多巴胺在浓度为10⁷ - 10⁻⁴ M时,可使K⁺去极化的大鼠子宫产生浓度依赖性松弛。以摩尔计,多巴胺使子宫松弛的效力约为肾上腺素的1/500,两种药物获得的最大松弛程度相同。用利血平(5 mg/kg)预处理大鼠,并未改变对多巴胺的剂量反应曲线。同样,可卡因(3×10⁻⁶ M)也未能改变多巴胺的松弛作用。多巴胺诱导的松弛被普萘洛尔(10⁻⁹ - 10⁻⁷ M)以剂量依赖性方式抑制。哌唑嗪(10⁻⁷ M)、SCH 23390(10⁻⁷ M)和舒必利(10⁻⁷ M)不影响多巴胺的剂量反应曲线。在未用KCl预收缩的离体大鼠子宫中,加入多巴胺或肾上腺素均未产生任何作用。即使在用普萘洛尔或舒必利预处理的组织中,对这两种儿茶酚胺也缺乏反应。结论是,多巴胺通过直接激活β - 肾上腺素受体,使己烯雌酚处理过的大鼠子宫产生浓度依赖性松弛。没有证据表明存在间接作用(儿茶酚胺释放和神经元摄取机制),并且在该制剂中未发现特异性多巴胺受体介导的松弛和α - 肾上腺素受体介导的收缩。