Kakihana M, Suno M, Nagaoka A
Central Research Division, Takeda Chemical Industries, Ltd., Osaka, Japan.
Jpn J Pharmacol. 1988 Oct;48(2):223-8. doi: 10.1254/jjp.48.223.
The hypotensive action of CV-4093.2HCl (CV-4093), a new calcium antagonist, was studied in spontaneously hypertensive, renal hypertensive, DOCA-salt hypertensive and normotensive rats. CV-4093 (3 and 10 mg/kg, p.o.) dose-dependently decreased systolic blood pressure in the three types of hypertensive rats. At the dose of 10 mg/kg, the compound decreased the blood pressure to the normotensive level between 1 and 3 hr after it was administered; the antihypertensive effect lasted for at least 8 hr. The systolic blood pressure in normotensive rats was also decreased at 3 and 10 mg/kg, p.o., but less evidently than in the hypertensive rats. When the antihypertensive effect of CV-4093 was compared with that of seven known calcium antagonists in spontaneously hypertensive rats, it was the most potent and the most long-lasting.
新型钙拮抗剂盐酸CV - 4093.2（CV - 4093）的降压作用在自发性高血压大鼠、肾性高血压大鼠、去氧皮质酮盐性高血压大鼠和正常血压大鼠中进行了研究。CV - 4093（3毫克/千克和10毫克/千克，口服）剂量依赖性地降低了三种高血压大鼠的收缩压。在10毫克/千克的剂量下，该化合物在给药后1至3小时内将血压降至正常血压水平；降压作用持续至少8小时。正常血压大鼠口服3毫克/千克和10毫克/千克时收缩压也降低，但不如高血压大鼠明显。当在自发性高血压大鼠中将CV - 4093的降压作用与七种已知钙拮抗剂的降压作用进行比较时，它是最有效且持续时间最长的。
