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豚鼠肺实质条对多巴胺反应性的药理学分析

Pharmacological analysis of the responsiveness of guinea-pig lung parenchymal strip to dopamine.

作者信息

Cortijo J, Esplugues J, Morcillo E J, Perpiñá M

出版信息

Br J Pharmacol. 1984 Sep;83(1):161-7. doi: 10.1111/j.1476-5381.1984.tb10131.x.

Abstract

Responses to dopamine were examined in the guinea-pig isolated lung parenchymal strip. Complete cumulative concentration-response curves to dopamine exhibited a biphasic pattern with a small initial contraction at concentrations below 10(-5) M followed by a dose-dependent relaxation at higher concentrations. Phentolamine (10(-5) M) completely abolished the contractile component and enhanced sensitivity and maximal relaxation to dopamine. In the presence of phentolamine, propranolol antagonized the dopamine-induced relaxation (pA2 = 8.54 +/- 0.07). In the presence of propranolol (10(-6) M), dopamine produced a dose-related contraction displaced to the right by phentolamine. Incubation with haloperidol (10(-5) M) did not modify the characteristics of the concentration-response curve to dopamine. Pretreatment with reserpine abolished the contraction to dopamine without affecting its relaxant response. Cocaine significantly increased the pD2 value of dopamine in the presence of propranolol. It is concluded that dopamine produced both relaxation of lung parenchymal strip due to direct activation of beta-adrenoceptors and contraction mediated through direct and indirect (catecholamine release) actions at alpha-adrenoceptors. There is no evidence in favour of the existence of specific dopamine-receptors in this preparation.

摘要

在豚鼠离体肺实质条上研究了对多巴胺的反应。多巴胺完整的累积浓度-反应曲线呈现双相模式,在浓度低于10⁻⁵ M时先有一个小的初始收缩,随后在较高浓度时出现剂量依赖性舒张。酚妥拉明(10⁻⁵ M)完全消除了收缩成分,并增强了对多巴胺的敏感性和最大舒张反应。在酚妥拉明存在的情况下,普萘洛尔拮抗多巴胺诱导的舒张(pA₂ = 8.54 ± 0.07)。在普萘洛尔(10⁻⁶ M)存在的情况下,多巴胺产生剂量相关的收缩,酚妥拉明使其向右移位。与氟哌啶醇(10⁻⁵ M)孵育并未改变多巴胺浓度-反应曲线的特征。利血平预处理消除了对多巴胺的收缩反应,而不影响其舒张反应。在普萘洛尔存在的情况下,可卡因显著增加了多巴胺的pD₂值。得出的结论是,多巴胺通过直接激活β-肾上腺素受体使肺实质条舒张,以及通过对α-肾上腺素受体的直接和间接(儿茶酚胺释放)作用介导收缩。没有证据支持该制剂中存在特异性多巴胺受体。

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