3-carboxamido analogues of morphine and naltrexone: Synthesis and opioid receptor binding properties

被引：27

作者：

Wentland, MP

Lou, RL

Dehnhardt, CM

Duan, WH

Cohen, DJ

Bidlack, JM

机构：

[1] Rensselaer Polytech Inst, Dept Chem, Troy, NY 12180 USA

[2] Univ Rochester, Sch Med & Dent, Dept Physiol & Pharmacol, Rochester, NY 14642 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 13期

关键词：

D O I：

10.1016/S0960-894X(01)00278-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In response to the unexpectedly high affinity for opioid receptors observed in a novel series of cyclazocine analogues where the prototypic 8-OH was replaced by a carboxamido group. we have prepared the corresponding 3-CONH2 analogues of morphine and naltrexone. High affinity (K-i = 34 and 1.7 nM) for mu opioid receptors was seen, however, the new targets were 39- and Ii-fold less potent than morphine and naltrexone. respectively. (C) 2001 Elsevier Science Ltd. All rights reserved.

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页码：1717 / 1721

页数：5

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