Nagao T, Narita H, Sato M, Nakajima H, Kiyomoto A
Clin Exp Hypertens A. 1982;4(1-2):285-96. doi: 10.3109/10641968209061591.
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.
我们发现冠状动脉舒张作用存在于新型1,5 - 苯并硫氮杂䓬衍生物中。地尔硫䓬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。尽管地尔硫䓬的血管舒张作用在冠状动脉和椎动脉中最为显著，但它也能扩张包括肾动脉在内的其他外周动脉。地尔硫䓬的降压作用已在多种实验模型中得到证实，如自发性高血压大鼠（SHR）、肾性高血压大鼠和去氧皮质酮/盐水诱导的高血压大鼠。在SHR中观察到了地尔硫䓬的利尿作用。对SHR长期给予地尔硫䓬后，血压升高明显降低，且体液无变化。此外，仅在非常高的剂量下观察到脑室内注射地尔硫䓬的降压作用。我们认为地尔硫䓬的血管舒张作用主要参与了其降压作用的机制。
