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1. 上海医科大学药学院
2. 北京师范大学
3. 上海医科大学药学院北京师范大学
Published:01 November 1995
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[1]沈鸣华,龚佳玲,王蔷,朱桐,刘伯里,孟昭兴,唐志刚.多巴胺D_2受体拮抗剂氨基取代苯酰胺类化合物的合成[J].核技术,1995(11):651-654.
Dopamine D2 receptor antaganists synthsis of amino substituted benzamide compounds[J]. Nuclear techniques, 1995, (11).
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分析证明,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.
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