Gingerols: a novel class of vanilloid receptor (VR1) agonists
نویسندگان
چکیده
منابع مشابه
The transient receptor potential vanilloid receptor 1, TRPV1 (VR1) inhibits peristalsis in the mouse jejunum.
BACKGROUND The transient receptor potential vanilloid receptor 1, TRPV1 [previously termed the capsaicin or vanilloid receptor 1 (VR1)] is a nonselective cation channel that has been cloned and is expressed predominantly in sensory neurons. TRPV1 is activated by protons as well as capsaicin. Despite extensive research, the physiological function of TRPV1 in the gastrointestinal tract and other ...
متن کاملAnandamide activates vanilloid receptor 1 (VR1) at acidic pH in dorsal root ganglia neurons and cells ectopically expressing VR1.
The vanilloid receptor type 1 (VR1) is a heat-activated ionophore preferentially expressed in nociceptive neurons of trigeminal and dorsal root ganglia (DRG). VR1, which binds and is activated by capsaicin and other vanilloid compounds, was noted to interact with the endocannabinoid anandamide (ANA) and certain inflammatory metabolites of arachidonic acid in a pH-dependent manner. At pH < or = ...
متن کاملHigh-affinity partial agonists of the vanilloid receptor.
The vanilloid receptor VR1 is a polymodal nociceptor sensitive to capsaicin, protons, and heat. Because VR1 represents an attractive therapeutic target for conditions ranging from long-term pain to bladder hyperreflexia, we and other groups have sought to develop novel ligands with enhanced potencies and novel pharmacological properties. Here, we characterize two compounds, N-[2-(3,4-dimethylbe...
متن کاملDistribution of mRNA for vanilloid receptor subtype 1 (VR1), and VR1-like immunoreactivity, in the central nervous system of the rat and human.
The cloned vanilloid receptor VR1 has attracted recent attention as a molecular integrator of painful stimuli on primary sensory neurons. The existence of vanilloid-sensitive neurons in the brain is, however, controversial. In this study, we have used an antibody and a complementary RNA probe to explore the distribution of neurons that express VR1 in rat and in certain areas of human brain. In ...
متن کاملVanilloid Receptor 1 Agonists, Capsaicin and Resiniferatoxin, Enhance MHC Class I-restricted Viral Antigen Presentation in Virus-infected Dendritic Cells
DCs, like the sensory neurons, express vanilloid receptor 1 (VR1). Here we demonstrate that the VR1 agonists, capsaicin (CP) and resiniferatoxin (RTX), enhance antiviral CTL responses by increasing MHC class I-restricted viral antigen presentation in dendritic cells (DCs). Bone marrow-derived DCs (BM-DCs) were infected with a recombinant vaccinia virus (VV) expressing OVA (VV-OVA), and then tre...
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ژورنال
عنوان ژورنال: British Journal of Pharmacology
سال: 2002
ISSN: 0007-1188
DOI: 10.1038/sj.bjp.0704925