Understanding the structural requirements of 4-anilidopiperidine analogues for biological activities at μ and δ opioid receptors

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:17

Article

Lee, Yeon Sun ; Nyberg, Joel ; Moye, Sharif ; Agnes, Richard S. ; Davis, Peg ; Ma, Shou-wu ; Lai, Josephine ; Porreca, Frank ; Vardanyan, Ruben ; Hruby, Victor J.

关键词: 4-anilidopiperidine analogues;    fentanyl;    Dmt-Tic;    opioid receptors;    analgesic effects;   

DOI  :  10.1016/j.bmcl.2007.01.114

来源: Elsevier

【 摘 要 】

New 4-anilidopiperidine analogues in which the phenethyl group of fentanyl was replaced by several aromatic ring-contained amino acids (or acids) were synthesized to study the biological effect of the substituents on mu and delta opioid receptor interactions. These analogues showed broad (47 nM-76 mu M) but selective (up to 17-fold) binding affinities at the V opioid receptor over the 6 opioid receptor, as predicted from the message-address concept. (c) 2007 Elsevier Ltd. All rights reserved.

【 授权许可】

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