Schümann H J, Görlitz B D, Wagner J
Naunyn Schmiedebergs Arch Pharmacol. 1975;289(4):409-18. doi: 10.1007/BF00508414.
The effects of papaverine and of the organic calcium-antagonistic agents D 600 and nifedipine on the contraction induced by noradrenaline and calcium were studied on the isolated aorta and mesenteric artery. The affinities of both agonists, given as pD2-values, were significantly higher on the aorta than on the mesenteric artery. Under our experimental conditions D 600, nifedipine and papaverine were found to act as antagonists against calcium and noradrenaline in a non-competitive fashion. In either vessel, the calcium-antagonistic activity of D 600 and nifedipine was about 1000-fold greater than that of papaverine, whereas their antagonistic activity against noradrenaline was bout 1000-times weaker, i.e. D 600 as well as nifedipine were about equipotent with papaverine. The comparison between the calcium- and the noradrenaline-antagonistic activity offers the possiblity to evaluate the specifcity of calcium antagonistic agents.
在离体主动脉和肠系膜动脉上研究了罂粟碱以及有机钙拮抗剂D 600和硝苯地平对去甲肾上腺素和钙诱导的收缩的影响。以pD2值表示的两种激动剂在主动脉上的亲和力明显高于肠系膜动脉。在我们的实验条件下,发现D 600、硝苯地平和罂粟碱以非竞争性方式作为钙和去甲肾上腺素的拮抗剂。在任一血管中,D 600和硝苯地平的钙拮抗活性比罂粟碱大约强1000倍,而它们对去甲肾上腺素的拮抗活性大约弱1000倍,即D 600和硝苯地平与罂粟碱的效力大致相当。钙拮抗活性与去甲肾上腺素拮抗活性之间的比较为评估钙拮抗剂的特异性提供了可能性。