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2-吲哚啉酮类化合物的合成及其体外活性研究 被引量：1

Synthesis and biological evaluation of 2-indolinone derivatives as dopamine D4 receptor ligands
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摘要 为开发新型多巴胺D4受体配基,以2-吲哚啉酮和1,4-二溴丁烷为原料,制得目标化合物1-(4-(4-(4-苯甲基)-1-哌嗪基)丁基)-2-吲哚啉酮、1-(4-(4-(4-氯苯甲基)-1-哌嗪基)丁基)-2-吲哚啉酮、1-(4-(4-(4-甲基苯甲基)-1-哌嗪基)丁基)-2-吲哚啉酮。通过体外受体结合分析,测定了这3个目标化合物对多巴胺D2、D3、D4.2受体的亲和性。实验结果表明:化合物1-(4-(4-(4-氯苯甲基)-1-哌嗪基)丁基)-2-吲哚啉酮对D4受体亲和选择性较大,其亲和常数(Ki)为0.5 nmol/L。 To develop novel dopamine D4 receptor ligands,1-（4-（4-（4-benzyl）-1-piperazinyl）butyl）indolin-2-one,1-（4-（4-（4-chlorobenzyl）-1-piperazinyl）butyl）indolin-2-one and 1-（4-（4-（4-methylbenzyl）-1-piperazinyl）butyl）indolin-2-one were synthesized from 2-indolinone and 1,4-dibromobutane.Through invitro receptor binding studies,the affinities of the three compounds at D2,D3,D4 receptor subtypes were determined.The experimental results showed that 1-（4-（4-（4-chlorobenzyl）-1-piperazinyl）butyl）-2-indolinone exhibited a remarkable affinity to D4 receptor with Ki value of 0.5 nmol/L.
作者 李谷才 张儒 蒋开军
机构地区 湖南工程学院化学化工学院
出处 《化学试剂》 CAS CSCD 北大核心 2012年第7期593-596,600,共5页 Chemical Reagents
基金 湖南省自然科学基金资助项目(07JJ6014)
关键词 2-吲哚啉酮 配体 多巴胺D4受体 生物学评价 2-indolinone ligand dopamine D4 receptor biological evaluation
分类号 O626 [理学—有机化学]
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参考文献20

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共引文献108

同被引文献11

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化学试剂
2012年 第7期

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