Malherbe E, Auguet M, Delaflotte S, Le Hégarat M, Baranes J, Clostre F, Braquet P
I.H.B. Research Labs, Les Ulis, France.
Pharmacol Res Commun. 1988 Sep;20 Suppl 3:121-33. doi: 10.1016/s0031-6989(88)80111-5.
The effects of cicletanine were compared with those of three other antihypertensive drugs: prazosin, a highly selective alpha 1 antagonist, captopril an angiotensin converting enzyme inhibitor and indapamide a diuretic antihypertensive agent, on young stroke-prone SHR rats with high salt diet; furthermore, vascular reactivity to cicletanine was studied on isolated rat aorta. At an equal dose (30 mg/kg per os) all the drugs prevent the onset of hypertension with the same intensity. The minimal effective dose on blood pressure was 1 mg/kg for both cicletanine and captopril, and 3 mg/kg for indapamide. The action on diuresis and electrolyte excretion occurs at a dose of cicletanine 10 to 30 times higher than that required to produce the anti-hypertensive effect. One of the possible mechanisms of the antihypertensive effects of cicletanine could be due to a direct action of the drug on the vascular wall. This vascular impact could be an interaction with the alpha-adrenoceptor system (apparent pA2 cicletanine = 5.12) or a decrease in the vascular spasmogenic response whatever agonist was studied.
哌唑嗪，一种高度选择性的α1拮抗剂；卡托普利，一种血管紧张素转换酶抑制剂；吲达帕胺，一种利尿抗高血压药物。研究对象为食用高盐饮食的年轻易中风SHR大鼠；此外，还在离体大鼠主动脉上研究了西氯他宁的血管反应性。在相同剂量（30毫克/千克口服）下，所有药物均以相同强度预防高血压的发生。西氯他宁和卡托普利对血压的最小有效剂量均为1毫克/千克，吲达帕胺为3毫克/千克。西氯他宁对利尿和电解质排泄的作用发生时的剂量比产生抗高血压作用所需剂量高10至30倍。西氯他宁抗高血压作用的一种可能机制可能是该药物对血管壁的直接作用。这种血管影响可能是与α-肾上腺素能受体系统相互作用（西氯他宁的表观pA2 = 5.12），或者无论研究何种激动剂，血管痉挛性反应均降低。
