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5-Iodoresiniferatoxin evokes hypothermia in mice and is a partial transient receptor potential vanilloid 1 agonist in vitro.
J Pharmacol Exp Ther. 2005 Sep; 314(3):1378-85.JP

Abstract

Transient receptor potential vanilloid 1 (TRPV1) is a capsaicin- and heat-gated ion channel required for normal in vivo responses to these painful stimuli. However, growing evidence suggests that TRPV1 also participates in thermoregulation. Therefore, we examined the effects of a selective TRPV1 antagonist, 5-iodoresiniferatoxin (I-RTX), on mouse body temperature. Surprisingly, s.c. administration of I-RTX (0.1-1 micromol/kg) evoked a hypothermic response similar to that evoked by capsaicin (9.8 micromol/kg) in naive wild-type mice, but not in mice pretreated with resiniferatoxin, a potent TRPV1 agonist, or in naive TRPV1-null mice. In response to I-RTX in vitro, HEK293 cells expressing rat TRPV1 exhibited increases in intracellular Ca(2+) (biphasic, EC(50) = 56.7 nM and 9.9 microM) that depended on Ca(2+) influx and outwardly rectifying, capsazepine-sensitive currents that were smaller than those evoked by 1 microM capsaicin. Thus, I-RTX induces TRPV1-dependent hypothermia in vivo and is a partial TRPV1 agonist in vitro.

Authors+Show Affiliations

Department of Biological Chemistry, Johns Hopkins School of Medicine, Baltimore, MD 21205, USA.No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

15947039

Citation

Shimizu, Isao, et al. "5-Iodoresiniferatoxin Evokes Hypothermia in Mice and Is a Partial Transient Receptor Potential Vanilloid 1 Agonist in Vitro." The Journal of Pharmacology and Experimental Therapeutics, vol. 314, no. 3, 2005, pp. 1378-85.
Shimizu I, Iida T, Horiuchi N, et al. 5-Iodoresiniferatoxin evokes hypothermia in mice and is a partial transient receptor potential vanilloid 1 agonist in vitro. J Pharmacol Exp Ther. 2005;314(3):1378-85.
Shimizu, I., Iida, T., Horiuchi, N., & Caterina, M. J. (2005). 5-Iodoresiniferatoxin evokes hypothermia in mice and is a partial transient receptor potential vanilloid 1 agonist in vitro. The Journal of Pharmacology and Experimental Therapeutics, 314(3), 1378-85.
Shimizu I, et al. 5-Iodoresiniferatoxin Evokes Hypothermia in Mice and Is a Partial Transient Receptor Potential Vanilloid 1 Agonist in Vitro. J Pharmacol Exp Ther. 2005;314(3):1378-85. PubMed PMID: 15947039.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - 5-Iodoresiniferatoxin evokes hypothermia in mice and is a partial transient receptor potential vanilloid 1 agonist in vitro. AU - Shimizu,Isao, AU - Iida,Tohko, AU - Horiuchi,Nobuhiko, AU - Caterina,Michael J, Y1 - 2005/06/09/ PY - 2005/6/11/pubmed PY - 2005/10/22/medline PY - 2005/6/11/entrez SP - 1378 EP - 85 JF - The Journal of pharmacology and experimental therapeutics JO - J Pharmacol Exp Ther VL - 314 IS - 3 N2 - Transient receptor potential vanilloid 1 (TRPV1) is a capsaicin- and heat-gated ion channel required for normal in vivo responses to these painful stimuli. However, growing evidence suggests that TRPV1 also participates in thermoregulation. Therefore, we examined the effects of a selective TRPV1 antagonist, 5-iodoresiniferatoxin (I-RTX), on mouse body temperature. Surprisingly, s.c. administration of I-RTX (0.1-1 micromol/kg) evoked a hypothermic response similar to that evoked by capsaicin (9.8 micromol/kg) in naive wild-type mice, but not in mice pretreated with resiniferatoxin, a potent TRPV1 agonist, or in naive TRPV1-null mice. In response to I-RTX in vitro, HEK293 cells expressing rat TRPV1 exhibited increases in intracellular Ca(2+) (biphasic, EC(50) = 56.7 nM and 9.9 microM) that depended on Ca(2+) influx and outwardly rectifying, capsazepine-sensitive currents that were smaller than those evoked by 1 microM capsaicin. Thus, I-RTX induces TRPV1-dependent hypothermia in vivo and is a partial TRPV1 agonist in vitro. SN - 0022-3565 UR - https://www.unboundmedicine.com/medline/citation/15947039/5_Iodoresiniferatoxin_evokes_hypothermia_in_mice_and_is_a_partial_transient_receptor_potential_vanilloid_1_agonist_in_vitro_ L2 - https://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=15947039 DB - PRIME DP - Unbound Medicine ER -