Development of diltiazem, a calcium antagonist: coronary vasodilating and antihypertensive actions.
Development of diltiazem, a calcium antagonist: coronary vasodilating and antihypertensive actions.
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钙拮抗剂地尔硫卓的开发：冠状血管舒张和抗高血压作用。
DOI：
10.3109/10641968209061591
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发表时间：
1982
期刊：
影响因子：
--
通讯作者：
A. Kiyomoto
中科院分区：
文献类型：
--
作者：
T. Nagao;H. Narita;M. Sato;H. Nakajima;A. Kiyomoto
我们发现新型 1,5-苯并硫氮杂卓衍生物具有冠状血管舒张作用。地尔硫卓的钙拮抗特性已在血管和内脏平滑肌以及心室肌中得到证实。虽然地尔硫卓的血管舒张作用在冠状动脉和椎动脉中最有效，但它也会扩张其他外周动脉，包括肾动脉。地尔硫卓的抗高血压作用已在多种实验模型中得到证实，例如 SHR、肾高血压和 DOCA/盐水大鼠。在 SHR 中观察到地尔硫卓的利尿作用。 SHR长期服用地尔硫卓后，在不改变体液的情况下，血压增量显着降低。此外，地尔硫卓的降血压作用通过静脉注射。仅在非常高的剂量下才观察到。我们假设地尔硫卓的血管舒张作用主要涉及其抗高血压作用的机制。
We found that the coronary vasodilating action resides in novel 1,5-benzothiazepine derivatives. The calcium antagonistic property of diltiazem has been demonstrated in vascular and visceral smooth muscles as well as in cardiac ventricular muscle. Although the vasodilating action of diltiazem was the most potent in coronary and vertebral artery, it also dilates other peripheral arteries including renal artery. Antihypertensive action of diltiazem has been shown in several experimental models, such as SHR, renal hypertensive and DOCA/saline rats. Diuretic effect of diltiazem was observed in SHR. Following chronic administration of diltiazem to SHR, the increment of blood pressure was significantly lowered without changing body fluid. In addition, hypotensive action of diltiazem by i.c.v. was observed only at a very high dose. We assume that the vasodilating action of diltiazem is primarily involved in the mechanism responsible for its antihypertensive action.