NAPHTHO AND BENZO ANALOGS OF THE KAPPA OPIOID AGONIST TRANS-(+/-)-3,4-DICHLORO-N-METHYL-N-[2-(1-PYRROLIDINYL)CYCLOHEXYL]BENZENEACETAMIDE

被引：31

作者：

FREEMAN, JP ^{[1
]}

MICHALSON, ET ^{[1
]}

DANDREA, SV ^{[1
]}

BACZYNSKYJ, L ^{[1
]}

VONVOIGTLANDER, PF ^{[1
]}

LAHTI, RA ^{[1
]}

SMITH, MW ^{[1
]}

LAWSON, CF ^{[1
]}

SCAHILL, TA ^{[1
]}

MIZSAK, SA ^{[1
]}

SZMUSZKOVICZ, J ^{[1
]}

机构：

[1] UPJOHN CO,KALAMAZOO,MI 49001

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1991年 / 34卷 / 06期

关键词：

D O I：

10.1021/jm00110a021

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Further elaboration on the structure-activity relationships in our U-50,488 series has revealed that benzologation of this cyclohexane-1,2-diamine derivative provides compounds which either maintain the interaction with the kappa-receptor (e.g. compounds 3a and 5a in the phenylacetamido series) or eliminate the mu-receptor mediated analgesia (e.g. compounds 3-6 in the benzamido series). Naphthologation also caused the elimination of mu-receptor mediated analgesia (e.g. compounds 17a and 17b).

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页码：1891 / 1896

页数：6

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