Brown J, Doxey J C, Handley S
Eur J Pharmacol. 1980 Oct 3;67(1):33-40. doi: 10.1016/0014-2999(80)90005-9.
The effects of alpha-adrenoceptor agonists and antagonists and of antidepressant drugs were studied on pre- and postsynaptic alpha-adrenoceptors. The rat vas deferens, stimulated at low frequency (0.1 Hz) was used for presynaptic studies. The rat anococcygeus muscle was used in postsynaptic studies. In the agonist studies clonidine and guanfacine were selective for presynaptic alpha-adrenoceptors, methoxamine and phenylephrine were selective for postsynaptic alpha-adrenoceptors and noradrenaline and alpha-methylnoradrenaline were equipotent at pre- and post-synaptic alpha-adrenoceptors. In the antagonist studies piperoxane and yohimbine were selective for presynaptic alpha-adrenoceptors, phentolamine was equipotent at pre- and postsynaptic alpha-adrenoceptors and prazosin was a selective postsynaptic alpha-adrenoceptor antagonist. In the series of antidepressants studied, mianserin was the most potent antagonist at presynaptic alpha-adrenoceptors, followed by trazodone, amitriptyline and nortriptyline in descending order of potency. Mianserin was approximately two hundred times less potent than piperoxane as a presynaptic alpha-adrenoceptor antagonist. Viloxazine and desipramine were inactive. With the exception of viloxazine all of the antidepressants examined possessed postsynaptic alpha-adrenoceptor antagonist properties.
研究了α-肾上腺素能受体激动剂、拮抗剂及抗抑郁药对突触前和突触后α-肾上腺素能受体的作用。以低频（0.1Hz）刺激的大鼠输精管用于突触前研究。大鼠肛门尾骨肌用于突触后研究。在激动剂研究中，可乐定和胍法辛对突触前α-肾上腺素能受体具有选择性，甲氧明和去氧肾上腺素对突触后α-肾上腺素能受体具有选择性，去甲肾上腺素和α-甲基去甲肾上腺素对突触前和突触后α-肾上腺素能受体的作用相当。在拮抗剂研究中，哌罗克生和育亨宾对突触前α-肾上腺素能受体具有选择性，酚妥拉明对突触前和突触后α-肾上腺素能受体的作用相当，哌唑嗪是一种选择性突触后α-肾上腺素能受体拮抗剂。在所研究的一系列抗抑郁药中，米安色林是突触前α-肾上腺素能受体最有效的拮抗剂，其次是曲唑酮、阿米替林和去甲替林，效力依次递减。作为突触前α-肾上腺素能受体拮抗剂，米安色林的效力比哌罗克生约低200倍。维洛沙嗪和地昔帕明无活性。除维洛沙嗪外，所有检测的抗抑郁药都具有突触后α-肾上腺素能受体拮抗剂特性。
