Wendling W W, Harakal C
Res Commun Chem Pathol Pharmacol. 1985 Aug;49(2):189-202.
Verapamil and pentobarbital were compared for their actions on isolated canine cerebral (basilar and middle cerebral) and peripheral (mesenteric) arteries of similar diameter. The two agents shared several nonselective actions on canine arteries, but differed widely in potency. Both agents produced direct relaxation of cerebral, but not peripheral, arteries, and both agents inhibited constriction of cerebral and peripheral arteries by KCl and CaCl2 (in K+-depolarizing, Ca2+-deficient media). However, 1 mM pentobarbital was required to produce the same maximal effects as 4 uM verapamil. In addition, verapamil selectively blocked constriction of cerebral arteries by a receptor-mediated agent, prostaglandin F2a, while pentobarbital was nonselective in its blockade. On the basis of their comparative actions on isolated cerebral and peripheral arteries, calcium channel blockers such as verapamil may be a more rational choice in the treatment of cerebral ischemia than the barbiturates.
对维拉帕米和戊巴比妥对直径相似的离体犬脑动脉(基底动脉和大脑中动脉)和外周动脉(肠系膜动脉)的作用进行了比较。这两种药物在犬动脉上有几种非选择性作用,但效价差异很大。两种药物都能直接舒张脑动脉而非外周动脉,并且都能抑制氯化钾和氯化钙(在钾离子去极化、钙离子缺乏的培养基中)引起的脑动脉和外周动脉收缩。然而,需要1 mM戊巴比妥才能产生与4 μM维拉帕米相同的最大效应。此外,维拉帕米可选择性阻断由受体介导的药物前列腺素F2α引起的脑动脉收缩,而戊巴比妥的阻断作用无选择性。基于它们对离体脑动脉和外周动脉的比较作用,像维拉帕米这样的钙通道阻滞剂在治疗脑缺血方面可能比巴比妥类药物更合理。