Dragović D, Soskić V, Joksimović J
Department of Chemistry, Faculty of Veterinary Medicine, University of Belgrade, Yugoslavia.
Pharmazie. 1995 Oct;50(10):678-80.
Four semirigid dopaminergic biosiosteres (N,N-di-n-propyl-5,6,7,8-tetrahydro-1 H-benz[f]benzimidazol-6-yl-amine [sequence: see text] and three related congeners) were synthesized and chemically characterized. The affinity and selectivity of these compounds for D-1 and D-2 classes of the dopamine receptor were determined in competition binding experiments using synaptosomal membranes of the bovine caudate nuclei and [3H]SCH 23390 (D-1 selective) and [3H]spiperone (D-2 selective) as radioligands. None of the four compounds tested expressed significant affinity for D-1 receptors and all of them competed moderately with [3H]spiperone binding to D-2 receptors under conditions that prevented radioligand binding to serotonin 5HT2 receptors. Some aspects of structure affinity relationship for this class of dopaminergic ligands are discussed.
合成并对四种半刚性多巴胺能生物电子等排体（N,N-二正丙基-5,6,7,8-四氢-1H-苯并[f]苯并咪唑-6-基胺[序列：见原文]及三种相关同系物）进行了化学表征。使用牛尾状核突触体膜以及[3H]SCH 23390（D-1选择性）和[3H]螺哌隆（D-2选择性）作为放射性配体，通过竞争结合实验测定了这些化合物对多巴胺受体D-1和D-2类别的亲和力和选择性。所测试的四种化合物中没有一种对D-1受体表现出显著亲和力，并且在防止放射性配体与5-羟色胺5HT2受体结合的条件下，它们全部与[3H]螺哌隆竞争结合D-2受体，竞争程度适中。讨论了这类多巴胺能配体的结构亲和力关系的一些方面。
