Vizi E S, Toth I, Somogyi G T, Szabo L, Harsing L G, Szantay C
J Med Chem. 1987 Aug;30(8):1355-9. doi: 10.1021/jm00391a015.
The alpha-adrenoceptor blocking properties of some berbanes have been studied and compared with those of idazoxan, yohimbine, phentolamine, and prazosin. Their effects on presynaptic alpha 2-adrenoceptors were studied on chemical neurotransmission of isolated rat vas deferens and longitudinal muscle strip of guinea pig ileum; xylazine or norepinephrine was employed as agonist. The alpha 1-adrenoceptor blocking activities of the berbanes were tested on isolated rat vas deferens and rabbit pulmonary artery by using phenylephrine or norepinephrine as agonist. The antagonistic activity of the berbanes and the reference compounds on alpha 2- and alpha 1-adrenoceptors was characterized by the apparent pA2 values. Of the compounds studied, [8aS*-(8a alpha,12a alpha,13a alpha)]-11 alpha-hydroxy-5,6,8a,9,10,11,12a,13,13,a-decahydro-8H-benzo[g]-1,3 -benzodioxolo[5,6-a]quinoli zine, 6d, proved to be the most selective antagonist at the presynaptic alpha 2-adrenoceptors (alpha 1:alpha 2 ratio = 1659). Since blockade of alpha 2-adrenoceptors located on noradrenergic axon terminals leads to an increase of norepinephrine release, this compound could have potential as an antidepressant agent.
已对一些小檗胺类化合物的α-肾上腺素能受体阻断特性进行了研究，并与咪唑克生、育亨宾、酚妥拉明和哌唑嗪的特性进行了比较。在离体大鼠输精管和豚鼠回肠纵行肌条的化学神经传递上研究了它们对突触前α₂-肾上腺素能受体的作用；使用赛拉嗪或去甲肾上腺素作为激动剂。通过使用去氧肾上腺素或去甲肾上腺素作为激动剂，在离体大鼠输精管和兔肺动脉上测试了小檗胺类化合物的α₁-肾上腺素能受体阻断活性。小檗胺类化合物和参比化合物对α₂-和α₁-肾上腺素能受体的拮抗活性通过表观pA₂值来表征。在所研究的化合物中，[8aS*-(8aα,12aα,13aα)]-11α-羟基-5,6,8a,9,10,11,12a,13,13,a-十氢-8H-苯并[g]-1,3-苯并二氧杂环戊烯并[5,6-a]喹嗪，6d，被证明是突触前α₂-肾上腺素能受体最具选择性的拮抗剂（α₁:α₂比率 = 1659）。由于位于去甲肾上腺素能轴突终末的α₂-肾上腺素能受体被阻断会导致去甲肾上腺素释放增加，该化合物可能具有作为抗抑郁药的潜力。
