Wallach M B
Department of Neuropharmacology, Syntex Research, Palo Alto, CA 94304.
Prostaglandins Leukot Essent Fatty Acids. 1989 Apr;36(1):35-41. doi: 10.1016/0952-3278(89)90160-9.
The antihypertensive activity of RS-93427, a synthetic prostanoid, was evaluated in conscious restrained spontaneously hypertensive rats. RS-93427 possesses potent antihypertensive activity when administered orally, intraduodenally, intravenously, or subcutaneously but not topically. The blood pressure reducing activity of RS-93427 in normotensive rats was comparable to that in hypertensive animals. No signs of tolerance to the antihypertensive effects were observed following fourteen days of oral administration of RS-93427. The synthetic prostanoid minimally enhanced the orthostatic hypotensive responsiveness to vertical, head up, repositioning of the restrained rats. The relative usefulness of the platelet antiaggregatory and antihypertensive properties of RS-93427 will have to be determined by clinical studies.
在清醒的束缚性自发性高血压大鼠中评估了合成前列腺素RS - 93427的抗高血压活性。RS - 93427经口服、十二指肠内、静脉内或皮下给药时具有强效抗高血压活性，但经皮给药则无此活性。RS - 93427在正常血压大鼠中的降压活性与在高血压动物中的相当。口服RS - 93427十四天后未观察到对其抗高血压作用产生耐受的迹象。该合成前列腺素对束缚大鼠垂直向上重新定位引起的体位性低血压反应性的增强作用极小。RS - 93427的血小板抗聚集特性和抗高血压特性的相对效用必须通过临床研究来确定。
