In vitro TRPV1 activity of piperine derived amides

Research output: Contribution to journalArticle

Abstract

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.

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Authors
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Research areas and keywords

Subject classification (UKÄ) – MANDATORY

  • Pharmacology and Toxicology
  • Medicinal Chemistry

Keywords

  • Fluorometric assays, vanilloid 1, Transient receptor potential, Piperine, Piperine-derived amides, Pain, Analgesic activity
Original languageEnglish
Pages (from-to)3299-3306
JournalBioorganic & Medicinal Chemistry
Volume18
Issue number9
Publication statusPublished - 2010
Publication categoryResearch
Peer-reviewedYes

Bibliographic note

The information about affiliations in this record was updated in December 2015. The record was previously connected to the following departments: Division of Clinical Chemistry and Pharmacology (013250300), Organic chemistry (S/LTH) (011001240)