Louis W J, Jarrott B, Conway E L
Clinical Pharmacology and Therapeutics Unit, Austin Hospital, Heidelberg, Victoria, Australia.
Am J Cardiol. 1988 Feb 24;61(7):15D-17D. doi: 10.1016/0002-9149(88)90458-4.
Alpha 2 agonists including rilmenidine, clonidine and alpha methylnoradrenaline all seem to have a predominantly central action in lowering blood pressure. Studies using the peripheral decarboxylase inhibitor alpha-methyldopa hydrazine in both experimental animals and humans support the predominant central action of the active metabolite of methyldopa, alpha methylnoradrenaline. Comparative studies on the antihypertensive potency of selective alpha 2 agonists like rilmenidine, guanfacine, clonidine and lofexidine suggest that the relative ability to bind to alpha 1 and alpha 2 adrenoceptors is not critical but the ability to enter the central nervous system is essential for antihypertensive efficacy.
包括利美尼定、可乐定和α-甲基去甲肾上腺素在内的α2激动剂在降低血压方面似乎主要起中枢作用。在实验动物和人类中使用外周脱羧酶抑制剂α-甲基多巴肼的研究支持了甲基多巴的活性代谢物α-甲基去甲肾上腺素的主要中枢作用。对利美尼定、胍法辛、可乐定和洛非西定等选择性α2激动剂的降压效力进行的比较研究表明，与α1和α2肾上腺素能受体结合的相对能力并不关键，但进入中枢神经系统的能力对于降压疗效至关重要。
