Doxey J C, Gadie B, Lane A C, Tulloch I F
Br J Pharmacol. 1983 Sep;80(1):155-61. doi: 10.1111/j.1476-5381.1983.tb11061.x.
Seven alpha 2-adrenoceptor antagonists with diverse chemical structures have been examined for their effects at alpha 2-adrenoceptors in the vas deferens and central nervous system of the rat. Antagonist potency assessed against the presynaptic alpha 2-adrenoceptor agonist action of clonidine in the isolated vas deferens (RX 781094 greater than Wy 26703 greater than yohimbine greater than rauwolscine greater than piperoxan greater than mianserin greater than RS 21361) was highly correlated with the ability of these drugs to displace saturable [3H]-RX 781094 binding from cerebral cortex membranes. Similarly, antagonist potency in the vas deferens was highly correlated with antagonist activity in reversing the centrally-mediated mydriasis induced by the selective alpha 2-adrenoceptor agonist, guanoxabenz, in pentobarbitone-anaesthetized rats. The results indicate that the presynaptic alpha 2-adrenoceptors in the vas deferens are pharmacologically similar to characterized these alpha 2-adrenoceptors in the central nervous system of the rat.
研究了七种化学结构各异的α2-肾上腺素能拮抗剂对大鼠输精管和中枢神经系统中α2-肾上腺素能受体的作用。在离体输精管中，以可乐定的突触前α2-肾上腺素能受体激动作用为对照评估拮抗剂效力（RX 781094＞Wy 26703＞育亨宾＞萝芙辛＞哌罗克生＞米安色林＞RS 21361），这些药物从大脑皮质膜上置换饱和[3H]-RX 781094结合的能力与之高度相关。同样，输精管中的拮抗剂效力与在戊巴比妥麻醉的大鼠中逆转由选择性α2-肾上腺素能激动剂胍那苄引起的中枢介导的散瞳作用的拮抗剂活性高度相关。结果表明，输精管中的突触前α2-肾上腺素能受体在药理学上与大鼠中枢神经系统中已鉴定的这些α2-肾上腺素能受体相似。
