Campbell J K, Marshall R J, Winslow E
Eur J Pharmacol. 1982 Dec 24;86(2):217-28. doi: 10.1016/0014-2999(82)90319-3.
The relaxant effects of the antianginal agent bepridil, a drug with calcium antagonistic actions, and verapamil on isolated pig coronary (C) and rabbit aortic (A) smooth muscle were compared. Both drugs competitively antagonised calcium in Tris buffered but not in bicarbonate buffered medium. Both agents relaxed K+-depolarised C and inhibited contractile responses to noradrenaline plus anoxia. Bepridil was approximately 10 fold less potent than verapamil. The two drugs exerted similar calcium antagonistic effects in guinea pig papillary muscle but showed dissimilar profiles in atrial muscle in that responses in the presence of bepridil appeared to be frequency dependent. It is concluded that bepridil inhibits responses to anoxia and competitively antagonises calcium in vascular smooth muscle. On atrial tissue, bepridil, unlike verapamil, appears to exert additional actions possibly involving other ion channels.
比较了抗心绞痛药物苄普地尔(一种具有钙拮抗作用的药物)和维拉帕米对离体猪冠状动脉(C)和兔主动脉(A)平滑肌的舒张作用。两种药物在Tris缓冲液中竞争性拮抗钙,但在碳酸氢盐缓冲液中则不然。两种药物均可使K⁺去极化的C舒张,并抑制对去甲肾上腺素加缺氧的收缩反应。苄普地尔的效力约为维拉帕米的1/10。两种药物在豚鼠乳头肌中发挥相似的钙拮抗作用,但在心房肌中表现出不同的特征,即苄普地尔存在时的反应似乎与频率有关。结论是,苄普地尔抑制对缺氧的反应,并在血管平滑肌中竞争性拮抗钙。在心房组织上,苄普地尔与维拉帕米不同,似乎发挥了可能涉及其他离子通道的额外作用。