Dabiré H
J Pharmacol. 1986 Apr-Jun;17(2):113-8.
The pharmacological properties of idazoxan, 2-[2-(1,4-benzodioxanyl)]-2-imidazoline, were first described four years ago; since then, this compound has been revealed to be one of the most selective alpha 2-adrenoceptor blocking agent presently available. At peripheral sites, idazoxan antagonized the effects of alpha 2 agonists such as azepexole, B-HT 920, M 7, UK 14,304, alpha-methylnoradrenaline, clonidine but was ineffective against alpha 1 agonists such as cirazoline and phenylephrine. At presynaptic sites idazoxan increased the tachycardia due to the stimulation of the cardioaccelerator nerve of the dog and antagonized the inhibitory effects of alpha 2 agonists in dogs and rats. As compared to the classical alpha 2-adrenoceptor blocking agents, idazoxan was more selective and as potent as yohimbine, rauwolscine, RS 21361, Wy 26703. At central sites, idazoxan has been found to antagonize the sympathoinhibitory effects of alpha 2 agonists. Therefore, idazoxan is a potent and probably the most selective alpha 2-adrenoceptor blocking agent presently available and is now frequently used for the investigation of peripheral and central alpha 2-adrenoceptors.
咪唑克生（2-[2-(1,4-苯并二氧杂环己烯基)]-2-咪唑啉）的药理特性于四年前首次被描述；从那时起，这种化合物已被证明是目前可用的最具选择性的α2-肾上腺素能受体阻断剂之一。在外周部位，咪唑克生可拮抗α2激动剂如阿泽匹唑、B-HT 920、M 7、UK 14,304、α-甲基去甲肾上腺素、可乐定的作用，但对α1激动剂如西拉唑啉和去氧肾上腺素无效。在突触前部位，咪唑克生可增强因刺激犬心加速神经所致的心动过速，并拮抗α2激动剂对犬和大鼠的抑制作用。与经典的α2-肾上腺素能受体阻断剂相比，咪唑克生更具选择性，且与育亨宾、萝芙素、RS 21361、Wy 26703的效力相当。在中枢部位，已发现咪唑克生可拮抗α2激动剂的交感抑制作用。因此，咪唑克生是一种强效且可能是目前可用的最具选择性的α2-肾上腺素能受体阻断剂，现在经常用于外周和中枢α2-肾上腺素能受体的研究。
