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多巴胺D2受体拮抗剂氨基取代苯酰胺类化合物的合成
Dopamine D_2 receptor antaganists synthsis of amino substituted benzamide compounds

多巴胺D2受体拮抗剂氨基取代苯酰胺类化合物的合成

ISSN:0253-3219
1995年第18卷第11期
沈鸣华 龚佳玲 Shen Minghua,Gong Jialing,Wang Qiang,Zhu Tong
上海医科大学药学院,北京师范大学

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.

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ISSN:0253-3219
1995年第18卷第11期

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