Mizobe T
Department of Anesthesiology, Kyoto Prefectural, University of Medicine.
Masui. 1997 Jul;46(7):934-41.
Alpha 2 adrenergic agonists will soon be used in the anesthetic management for their sedative/hypnotic, anesthetic-sparing, analgesic and sympatholytic properties. But the clinically available alpha 2 agonists have unwanted side-effects such as acute hypertension and bradycardia following a bolus injection because these agonists do not discriminate between the 3 alpha 2 adrenoceptor subtypes. Molecular biological methods can identify mediating receptor subtype for each response. Knockout mice study reveals that the alpha 2 B adrenoceptor subtype mediates the hypertensive response to alpha 2 agonists. Knockdown study using the antisense technology demonstrates that the alpha 2 A adrenoceptor subtype mediates the hypnotic and analgesic effects of alpha 2 agonists. The next generation of alpha 2 agonists should be alpha 2 A selective to maximize anesthetic and analgesic effects while minimizing hypertensive response.
α2肾上腺素能激动剂因其镇静/催眠、节省麻醉药、镇痛和抗交感神经特性，很快将用于麻醉管理。但临床上可用的α2激动剂存在不良副作用，如单次静脉注射后出现急性高血压和心动过缓，因为这些激动剂无法区分3种α2肾上腺素能受体亚型。分子生物学方法可识别每种反应的介导受体亚型。基因敲除小鼠研究表明，α2B肾上腺素能受体亚型介导α2激动剂的高血压反应。使用反义技术的基因敲低研究表明，α2A肾上腺素能受体亚型介导α2激动剂的催眠和镇痛作用。下一代α2激动剂应具有α2A选择性，以最大程度地发挥麻醉和镇痛作用，同时最小化高血压反应。
