Docherty J R, Hyland L
Br J Pharmacol. 1985 Oct;86(2):335-9. doi: 10.1111/j.1476-5381.1985.tb08901.x.
We have examined the pre- and post-junctional effects of a series of alpha-adrenoceptor agonists and antagonists at alpha 2-adrenoceptors in the pithed rat preparation and the human isolated saphenous vein. In the pithed rat, there was no difference in relative agonist and antagonist potencies between pre- and post-junctional alpha 2-adrenoceptors but the absolute potencies of antagonists differed: antagonists were more potent prejunctionally. In the human saphenous vein, the alpha 2-adrenoceptor antagonist yohimbine had pre- and post-junctional actions over the same concentration range. We have no evidence to suggest differences between pre- and post-junctional alpha 2-adrenoceptors: differences in absolute antagonist potencies in the pithed rat may be due to non-equilibrium conditions.
我们已经研究了一系列α-肾上腺素能激动剂和拮抗剂在去大脑大鼠制备物和人离体大隐静脉中对α2-肾上腺素能受体的节前和节后效应。在去大脑大鼠中,节前和节后α2-肾上腺素能受体之间的相对激动剂和拮抗剂效力没有差异,但拮抗剂的绝对效力不同:拮抗剂在节前更有效。在人隐静脉中,α2-肾上腺素能拮抗剂育亨宾在相同浓度范围内具有节前和节后作用。我们没有证据表明节前和节后α2-肾上腺素能受体之间存在差异:去大脑大鼠中拮抗剂绝对效力的差异可能是由于非平衡条件所致。