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Effect of chirality and lipophilicity in the functional activity of evodiamine and its analogues at TRPV1 channels
Author(s) -
De Petrocellis Luciano,
Schiano Moriello Aniello,
Fontana Gabriele,
Sacchetti Alessandro,
Passarella Daniele,
Appendino Giovanni,
Di Marzo Vincenzo
Publication year - 2014
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/bph.12320
Subject(s) - evodiamine , trpv1 , chemistry , capsazepine , agonist , pharmacology , resiniferatoxin , transient receptor potential channel , in vivo , capsaicin , lipophilicity , stereochemistry , biochemistry , receptor , medicine , biology , microbiology and biotechnology , chromatography
Evodiamine, a racemic quinazolinocarboline alkaloid isolated from the traditional Chinese medicine Evodiae fructus, has been reported to act as an agonist of the transient receptor potential vanilloid type-1 (TRPV1) cation channel both in vitro and in vivo. Evodiamine is structurally different from all known TRPV1 activators, and has significant clinical potential as a thermogenic agent. Nevertheless, the molecular bases for its actions are still poorly understood.