Bevan J A
Am J Cardiol. 1982 Feb 18;49(3):519-24. doi: 10.1016/s0002-9149(82)80005-2.
Diltiazem selectively reduces the second equilibrium phase of contraction of several arteries and veins in the rabbit to a number of agonists, including norepinephrine, serotonin, histamine and potassium. Its effect is consistent with blockage of the entry of activator calcium from the extracellular space into the vascular smooth muscle cell. It has a preferential action on responses of the basilar artery in comparison with those of the ear and mesenteric arteries and saphenous vein. Although the spontaneously developing, maintained intrinsic tone of the basilar artery and facial vein are very resistant to diltiazem, the spontaneous rhythmic activity of the portal vein is sensitive to its antagonistic action. Findings reported here are consistent with the possibility that diltiazem preferentially blocks receptor-operated and potential-sensitive slow calcium channels of the cerebral artery compared with other systemic vessels tested but has little effect on the mechanisms responsible for maintained intrinsic tone development.
地尔硫䓬可选择性地将家兔的几条动脉和静脉对多种激动剂(包括去甲肾上腺素、5-羟色胺、组胺和钾)收缩的第二个平衡期缩短。其作用与阻止激活钙从细胞外间隙进入血管平滑肌细胞一致。与耳动脉、肠系膜动脉和隐静脉相比,它对基底动脉的反应具有优先作用。虽然基底动脉和面部静脉自发产生并维持的内在张力对地尔硫䓬非常耐药,但门静脉的自发节律性活动对其拮抗作用敏感。此处报告的研究结果与以下可能性一致:与所测试的其他全身血管相比,地尔硫䓬优先阻断脑动脉的受体操纵性和电位敏感性慢钙通道,但对负责维持内在张力形成的机制影响很小。