Thurkauf A, Yuan J, Chen X, Wasley J W, Meade R, Woodruff K H, Huston K, Ross P C
Department of Chemistry, Neurogen Corporation, Branford, Connecticut 06405, USA.
J Med Chem. 1995 Dec 8;38(25):4950-2. doi: 10.1021/jm00025a013.
A series of 1-phenyl-3-(aminomethyl)pyrroles were prepared in two steps from aniline and their affinities for D2, D3, and D4 dopamine receptor subtypes determined. A 15-fold selectivity for cloned human D4 receptors over cloned African Green monkey D2 receptors was observed with 1-(2-pyridyl)-4-[[3-(1-phenylpyrrolyl)]methyl]piperazine.
以苯胺为原料，分两步制备了一系列1-苯基-3-(氨甲基)吡咯，并测定了它们对D2、D3和D4多巴胺受体亚型的亲和力。用1-(2-吡啶基)-4-[[3-(1-苯基吡咯基)]甲基]哌嗪观察到对克隆的人D4受体比对克隆的非洲绿猴D2受体有15倍的选择性。
