D'Agostino G, Zonta F, Dondi G, Grana E
Instituto di Farmacologia, Università di Pavia, Italia.
Pharmacol Res Commun. 1983 Nov;15(10):937-49. doi: 10.1016/s0031-6989(83)80023-x.
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.
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。