ANALGESICALLY ACTIVE BASIC ANILIDES - STEREOSPECIFICITY AND STRUCTURE OF BASIC GROUP
ANALGESICALLY ACTIVE BASIC ANILIDES - STEREOSPECIFICITY AND STRUCTURE OF BASIC GROUP
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DOI：
10.1111/j.2042-7158.1967.tb07988.x
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发表时间：
1967-01-01
影响因子：
3.3
通讯作者：
HASSAN, MMA
中科院分区：
文献类型：
--
作者：
CASY, AF;HASSAN, MMA
本文报道了（RS）-、（R）-和（S）-N-（2-二甲氨基丙基）丙酰胺以及美沙酮和异美沙酮的苄甲氨基类似物的合成。二甲氨基和苄基甲基氨基丙酰苯胺的（S）-对映体在小鼠体内的热板活性大于相应的（RS）-和（R）-形式，而美沙酮和异美沙酮类似物在同一试验中无活性。这些结果支持了3-氨基-1，1-二苯基丙基-和碱性苯胺-镇痛剂与镇痛受体结合方式不同的观点。
The synthesis of (RS)-, (R)- and (S)-N-(2-dimethylaminopropyl)propionaniHde and the benzylmethylamino- analogues of methadone and isomethadone is described. The hot-plate activities in mice of the (S)-enantiomarphs of both the dimethylamino-and benzylmethylaminopropionanilides are greater than those of the corresponding (RS)- and (R)-forms, while the methadone and isomethadone analogues are inactive in the same test. These results support the view that 3-amino-1,1-diphenylpropyl-and basic anilide-analgesics differ in their modes of binding to the analgesic receptor site.