Saari W S, Halczenko W, Randall W C, Lotti V J
J Med Chem. 1983 Dec;26(12):1769-72. doi: 10.1021/jm00366a022.
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 provided a variety of alpha-adrenergic profiles, with some of the (aminomethyl)imidazolines being nonselective alpha 1- and alpha 2-adrenergic antagonists like phentolamine, while others were either nonselective alpha 1- and alpha 2-agonists or mixed alpha 1-agonists/alpha 2-antagonists.
制备了一系列与α-肾上腺素能拮抗剂酚妥拉明相关的2-(氨甲基)咪唑啉，并在离体的、经场刺激的大鼠输精管中评估其α-肾上腺素能激动剂和拮抗剂活性。通过[3H]可乐定和[3H]哌唑嗪从小牛大脑皮质膜结合位点的置换来测定对α-肾上腺素能受体的亲和力。该系列呈现出多种α-肾上腺素能特征，其中一些(氨甲基)咪唑啉是像酚妥拉明一样的非选择性α1和α2肾上腺素能拮抗剂，而其他的则要么是非选择性α1和α2激动剂，要么是α1激动剂/α2拮抗剂的混合物。
