In vitro TRPV1 activity of piperine derived amides

被引：38

作者：

Andres Correa, Edwin ^{[1
]}

Hogestatt, Edward D. ^{[2
,3
]}

Sterner, Olov ^{[4
]}

Echeverri, Fernando ^{[1
]}

Zygmunt, Peter M. ^{[2
,3
]}

机构：

[1] Univ Antioquia, Inst Quim, Grp Quim Organ Prod Nat, Medellin, Colombia

[2] Lund Univ, Skane Univ Hosp, Div Clin Chem & Pharmacol, SE-22185 Lund, Sweden

[3] Lund Univ, Pain Res Ctr, SE-22185 Lund, Sweden

[4] Lund Univ, Div Organ Chem, SE-22100 Lund, Sweden

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2010年 / 18卷 / 09期

基金：

英国医学研究理事会;

关键词：

Piperine; Piperine-derived amides; Transient receptor potential vanilloid 1; Fluorometric assays; Pain; Analgesic activity; VANILLOID RECEPTORS; CAPSAICIN RECEPTOR; ANTIFUNGAL AMIDES; ANALOGS; PAIN;

D O I：

10.1016/j.bmc.2010.03.013

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of natural and synthetic piperine amides were evaluated for activity on the human TRPV1 expressed in HEK293 cells. The agonistic effect of piperine amides was mainly dependent on the length of the carbon chain. Structural changes of double bonds and stereochemistry in the aliphatic chain of these compounds did not change their potency or efficacy, indicating that increased rigidity or planarity of the piperine structure does not affect the activity. The opening of the methylenedioxy ring or changes in the heterocyclic ring of the piperine molecule reduced or abolished activity. Furthermore, inactive compounds did not display functional antagonistic activity. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：3299 / 3306

页数：8

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