Therapeutic potential of vanilloid receptor TRPV1 agonists and antagonists as analgesics: Recent advances and setbacks
GY Wong, NR Gavva - Brain research reviews, 2009 - Elsevier
The vanilloid receptor TRPV1 is a homotetrameric, non-selective cation channel abundantly
expressed in the nociceptors (c-fibers). TRPV1 is considered as a highly validated pain
target because, i) its agonists such as capsaicin cause desensitization of TRPV1 channels
that relieves pain behaviors in preclinical species, and ii) its antagonists relieve pain
behaviors in rodent models of inflammation, osteoarthritis, and cancer. Hence, both agonists
and antagonists of TRPV1 are being evaluated as potential analgesics in clinical trials …
expressed in the nociceptors (c-fibers). TRPV1 is considered as a highly validated pain
target because, i) its agonists such as capsaicin cause desensitization of TRPV1 channels
that relieves pain behaviors in preclinical species, and ii) its antagonists relieve pain
behaviors in rodent models of inflammation, osteoarthritis, and cancer. Hence, both agonists
and antagonists of TRPV1 are being evaluated as potential analgesics in clinical trials …