Thurkauf A, Hutchison A, Peterson J, Cornfield L, Meade R, Huston K, Harris K, Ross P C, Gerber K, Ramabhadran T V
Department of Chemistry, Neurogen Corporation, Branford, Connecticut 06405, USA.
J Med Chem. 1995 Jun 9;38(12):2251-5. doi: 10.1021/jm00012a026.
A series of 2-phenyl-4-(aminomethyl)imidazoles were designed as conformationally restricted analogs of the dopamine D2 selective benzamide antipsychotics. The title compounds were synthesized and tested for blockade of [3H]YM-09151 binding in cloned African green monkey dopamine D2 receptor preparations. The binding affinity data thus obtained were compared against that of the benzamides and a previously described series of 2-phenyl-5-(aminomethyl)-pyrroles.
设计了一系列2-苯基-4-（氨基甲基）咪唑作为多巴胺D2选择性苯甲酰胺类抗精神病药物的构象受限类似物。合成了标题化合物，并在克隆的非洲绿猴多巴胺D2受体制剂中测试了其对[3H]YM-09151结合的阻断作用。将由此获得的结合亲和力数据与苯甲酰胺类以及先前描述的一系列2-苯基-5-（氨基甲基）吡咯的结合亲和力数据进行了比较。
