EMD-61753 AS A FAVORABLE REPRESENTATIVE OF STRUCTURALLY NOVEL ARYLACETAMIDO-TYPE-KAPPA OPIATE RECEPTOR AGONISTS

被引：12

作者：

GOTTSCHLICH, R ^{[1
]}

ACKERMANN, KA ^{[1
]}

BARBER, A ^{[1
]}

BARTOSZYK, GD ^{[1
]}

GREINER, HE ^{[1
]}

机构：

[1] E MERCK AG,BIOL RES DEPT,D-64271 DARMSTADT,GERMANY

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1994年 / 4卷 / 05期

关键词：

D O I：

10.1016/S0960-894X(01)80179-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

K opiate agonists like (-)-U 50488H, (-)-PD 117302, etc. contain an acetamido group which is monosubstituted in the alpha-position by an aromatic moiety. In contrast, EMD 61 753 is disubstituted in this position by two phenyl rings and is thus the first representative of the new class of diarylacetamide-type kappa opiates. Derivates of EMD 61 753 are described and structure-activity relationships are discussed. In the formalin test in mice EMD 61 753 shows a profile similar to that of the antiinflammatory drugs rather than that of the centrally acting opiates.

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页码：677 / 682

页数：6

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