作者:Walfred S. Saari、Wasyl Halczenko、William C. Randall、Victor J. Lotti
DOI:10.1021/jm00366a022
日期:1983.12
A series of 2-(aminomethyl)imidazolines related to the alpha-adrenergic antagonist phentolamine was prepared and evaluated for alpha-adrenergic agonist and antagonist activities in the isolated, field-stimulated rat vas deferens. Affinities for alpha-adrenergic receptors were determined by displacement of [3H]clonidine and [3H]prazosin from membrane binding sites of calf cerebral cortex. This series
制备了一系列与α-肾上腺素拮抗剂酚妥拉明有关的2-(氨基甲基)咪唑啉,并评估了分离的,经田间刺激的大鼠输精管中α-肾上腺素能激动剂和拮抗剂的活性。α-肾上腺素能受体的亲和力是通过从小腿大脑皮质的膜结合位点置换[3H]可乐定和[3H]吡唑嗪来确定的。该系列药物提供了多种α-肾上腺素能谱,其中一些(氨甲基)咪唑啉是非选择性α1-和α2-肾上腺素能拮抗剂,如酚妥拉明,而另一些则是非选择性α1-和α2-激动剂或混合α1。 -激动剂/α2-拮抗剂。