Premium
Gingerols: a novel class of vanilloid receptor (VR1) agonists
Author(s) -
Dedov Vadim N,
Tran Van H,
Duke Colin C,
Connor Mark,
Christie MacDonald J,
Mandadi Sravan,
Roufogalis Basil D
Publication year - 2002
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 - 10.1038/sj.bjp.0704925
Subject(s) - capsazepine , gingerol , capsaicin , chemistry , receptor , pharmacology , agonist , antagonist , trpv1 , biochemistry , transient receptor potential channel , medicine , food science
Gingerols, the pungent constituents of ginger, were synthesized and assessed as agonists of the capsaicin‐activated VR1 (vanilloid) receptor. [6]‐Gingerol and [8]‐gingerol evoked capsaicin‐like intracellular Ca 2+ transients and ion currents in cultured DRG neurones. These effects of gingerols were blocked by capsazepine, the VR1 receptor antagonist. The potency of gingerols increased with increasing size of the side chain and with the overall hydrophobicity in the series. We conclude that gingerols represent a novel class of naturally occurring VR1 receptor agonists that may contribute to the medicinal properties of ginger, which have been known for centuries. The gingerol structure may be used as a template for the development of drugs acting as moderately potent activators of the VR1 receptor.British Journal of Pharmacology (2002) 137 , 793–798. doi: 10.1038/sj.bjp.0704925