In vitro TRPV1 activity of piperine derived amides

Summary, in English

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.

• Författare: Edwin Andres Correa; Edward Högestätt; Olov Sterner; Fernando Echeverri; Peter Zygmunt
• Avdelning/ar: Avdelningen för klinisk kemi och farmakologi; Centrum för analys och syntes
• Publiceringsår: 2010
• Språk: Engelska
• Sidor: 3299-3306
• Publikation/Tidskrift/Serie: Bioorganic & Medicinal Chemistry
• Volym: 18
• Issue: 9
• Länkar: http://dx.doi.org/10.1016/j.bmc.2010.03.013
• Dokumenttyp: Artikel i tidskrift
• Förlag: Elsevier
• Ämne: Pharmacology and Toxicology; Medicinal Chemistry
• Nyckelord: Fluorometric assays; vanilloid 1; Transient receptor potential; Piperine; Piperine-derived amides; Pain; Analgesic activity
• Status: Published
• ISBN/ISSN/Övrigt: ISSN: 0968-0896