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罂粟碱和维拉帕米对去甲肾上腺素和钙引起的血管及非血管平滑肌收缩的作用。

Action of papaverine and verapamil on norepinephrine and calcium evoked contraction of vascular and non vascular smooth muscle.

作者信息

D'Agostino G, Zonta F, Dondi G, Grana E

机构信息

Instituto di Farmacologia, Università di Pavia, Italia.

出版信息

Pharmacol Res Commun. 1983 Nov;15(10):937-49. doi: 10.1016/s0031-6989(83)80023-x.

Abstract

On isolated rat vas deferens both papaverine and verapamil show a non competitive antagonism against norepinephrine and a competitive antagonism against Ca2+. Verapamil is nearly 100 times more active than papaverine. On the main pulmonary artery and on the thoracic aorta of the rabbit, verapamil shows a competitive antagonism against both norepinephrine and Ca2+ but it is more effective (almost 100 times) against Ca2+ than norepinephrine. Papaverine also shows a competitive antagonism against norepinephrine but a non competitive antagonism against Ca2+. The contrasting results obtained on rat vas deferens and rabbit vessels might be due to: 1) mechanism(s) of action of the agonist; 2) properties of the biological object as far concerns receptor activation and mechanism(s) of excitation-contraction coupling; 3) mechanism(s) of action of spasmolytic drugs. All these factors act in a cooperative way in determining the quality and the quantity of the observed responses.

摘要

在离体大鼠输精管上,罂粟碱和维拉帕米对去甲肾上腺素均表现为非竞争性拮抗作用,对Ca2+表现为竞争性拮抗作用。维拉帕米的活性比罂粟碱高近100倍。在兔的主肺动脉和胸主动脉上,维拉帕米对去甲肾上腺素和Ca2+均表现为竞争性拮抗作用,但对Ca2+的作用比对去甲肾上腺素更有效(几乎100倍)。罂粟碱对去甲肾上腺素也表现为竞争性拮抗作用,但对Ca2+表现为非竞争性拮抗作用。在大鼠输精管和兔血管上获得的不同结果可能是由于:1)激动剂的作用机制;2)就受体激活和兴奋-收缩偶联机制而言生物对象的特性;3)解痉药物的作用机制。所有这些因素在决定所观察到的反应的性质和程度时协同起作用。

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