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Gene Review:

TRPV1 - transient receptor potential cation...

Canis lupus familiaris

Synonyms: OTRPC1, Osm-9-like TRP channel 1, Transient receptor potential cation channel subfamily V member 1, TrpV1, Vanilloid receptor 1

Gavva, N.R. et al., Nault, M.A. et al., Myrdal, S.E. et al., Karai, L. et al.

Gavva, Bannon, Surapaneni, Hovland, Lehto, Gore, Juan, Deng, Han, Klionsky, Kuang, Le, Tamir, Wang, Youngblood, Zhu, Norman, Magal, Treanor, Louis,

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Disease relevance of TRPV1

Here, we report that TRPV1 antagonists representing various chemotypes cause an increase in body temperature (hyperthermia), identifying a potential issue for their clinical development [1].

High impact information on TRPV1

Deletion of vanilloid receptor 1-expressing primary afferent neurons for pain control [2].
4. Lactic acid-evoked increases in RL were unaffected by VR1 blockade with capsazepine, consistent with a separate lactic acid-induced reflex mechanism [3].
1. Capsaicin activation of the pulmonary C fibre vanilloid receptor (VR1) evokes the pulmonary chemoreflex and reflex bronchoconstriction [3].
The effects of capsazepine are consistent with reversible blockade of the VR1 receptor to abolish C fibre-mediated reflex bronchoconstriction [3].
TRPV1 regulators mediate gentamicin penetration of cultured kidney cells [4].

Chemical compound and disease context of TRPV1

Antagonists that are ineffective against proton activation also caused hyperthermia, indicating that blocking capsaicin and heat activation of TRPV1 is sufficient to produce hyperthermia [1].

Biological context of TRPV1

Together, these results indicate that tonic TRPV1 activation regulates body temperature [1].
TRPV1 antagonists caused hyperthermia in multiple species (rats, dogs, and monkeys), demonstrating that TRPV1 function in thermoregulation is conserved from rodents to primates [1].

Anatomical context of TRPV1

Both kidney epithelial and inner ear sensory cells express TRPV1, are mechanosensors and accumulate the aminoglycoside antibiotic gentamicin [4].

Associations of TRPV1 with chemical compounds

GTTR uptake was enhanced by the TRPV1 agonists, resiniferatoxin and anandamide, in Ca2+-free media [4].

References

The vanilloid receptor TRPV1 is tonically activated in vivo and involved in body temperature regulation. Gavva, N.R., Bannon, A.W., Surapaneni, S., Hovland, D.N., Lehto, S.G., Gore, A., Juan, T., Deng, H., Han, B., Klionsky, L., Kuang, R., Le, A., Tamir, R., Wang, J., Youngblood, B., Zhu, D., Norman, M.H., Magal, E., Treanor, J.J., Louis, J.C. J. Neurosci. (2007) [Pubmed]
Deletion of vanilloid receptor 1-expressing primary afferent neurons for pain control. Karai, L., Brown, D.C., Mannes, A.J., Connelly, S.T., Brown, J., Gandal, M., Wellisch, O.M., Neubert, J.K., Olah, Z., Iadarola, M.J. J. Clin. Invest. (2004) [Pubmed]
Mechanisms of capsaicin- and lactic acid-induced bronchoconstriction in the newborn dog. Nault, M.A., Vincent, S.G., Fisher, J.T. J. Physiol. (Lond.) (1999) [Pubmed]
TRPV1 regulators mediate gentamicin penetration of cultured kidney cells. Myrdal, S.E., Steyger, P.S. Hear. Res. (2005) [Pubmed]

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