合成了11个消旋氨基取代的苯酰胺类化合物,以^3H-Sulpiride为标记配体进行放射受体竞争结合证明,这些化合物是多巴胺D2受体拮抗剂,IC50测定表明,其中含卤素和氨基取代的苯酰胺类化合物对D2受体的亲和力比Sulpiride大十几倍。
Eleven (RS)-amino substitated benzamide compounds not yet reported in literature were synthesised. Radioligand competitive binding assay using 3H-sulpiride as the radioligand proved that these compounds were dopamine D2receptor antagonists. Determination of IC50 showed that the affinity for D2 receptor of the amino substituted and halogen-containing benzamide compounds were about ten times higher than that of sulpiride.