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一些选择性α2-肾上腺素能拮抗剂在大鼠和家兔离体输精管上进行比较时的亲和力差异。

A difference in the affinity of some selective alpha 2-adrenoceptor antagonists when compared on isolated vasa deferentia of rat and rabbit.

作者信息

Lattimer N, Rhodes K F

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1985 May;329(3):278-81. doi: 10.1007/BF00501880.

Abstract

The alpha 2-adrenoceptor antagonist potencies of the benzoquinolizines (Wy 26 703, Wy 25 309, Wy 26 392), the benzodioxans (RX 781 094, RS 21 361), yohimbine and rauwolscine have been compared at presynaptic alpha 2-adrenoceptors in the isolated vasa deferentia of the rat and rabbit. Yohimbine and rauwolscine are of equal potency as antagonists in both the rat and rabbit against the agonists clonidine or UK 14304. The benzoquinolizines and benzodioxans are very weak antagonists of clonidine or UK 14304 at the presynaptic alpha 2-adrenoceptors of the rabbit vas deferens when compared to their potency at the presynaptic alpha 2-adrenoceptors of the rat vas deferens. This suggests that the presynaptic alpha 2-adrenoceptors present in the rat vasa deferentia may be different from those present in the rabbit vasa deferentia.

摘要

已在大鼠和家兔离体输精管的突触前α2 - 肾上腺素能受体上比较了苯并喹嗪类化合物(Wy 26703、Wy 25309、Wy 26392)、苯并二恶烷类化合物(RX 781094、RS 21361)、育亨宾和萝芙木碱的α2 - 肾上腺素能受体拮抗效能。在大鼠和家兔中,育亨宾和萝芙木碱作为针对激动剂可乐定或UK 14304的拮抗剂,效能相当。与它们在大鼠输精管突触前α2 - 肾上腺素能受体上的效能相比,苯并喹嗪类化合物和苯并二恶烷类化合物在兔输精管突触前α2 - 肾上腺素能受体上对可乐定或UK 14304的拮抗作用非常弱。这表明大鼠输精管中存在的突触前α2 - 肾上腺素能受体可能与家兔输精管中存在的不同。

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