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Effects of the novel TRPV1 receptor antagonist SB366791 in vitro and in vivo in the rat.
Neurosci Lett. 2005 Sep 09; 385(2):137-42.NL

Abstract

The TRPV1 capsaicin receptor is a non-selective cation channel localized in the cell membrane of a subset of primary sensory neurons and functions as an integrator molecule in nociceptive/inflammatory processes. The present paper characterizes the effects of SB366791, a novel TRPV1 antagonist, on capsaicin-evoked responses both in vitro and in vivo using rat models. SB366791 (100 and 500 nM) significantly inhibited capsaicin-evoked release of the pro-inflammatory sensory neuropeptide substance P from isolated tracheae, while it did not influence electrically induced neuropeptide release. It also decreased capsaicin-induced Ca2+ influx in cultured trigeminal ganglion cells in a concentration-dependent manner (0.5-10 microM) with an IC50 of 651.9 nM. In vivo 500 microg/kg i.p. dose of SB366791 significantly inhibited capsaicin-induced hypothermia, wiping movements and vasodilatation in the knee joint, while 2 mg/kg capsazepine was ineffective, its effect lasted for 1h. However, neither antagonist was able to inhibit capsaicin-evoked hypothermia in Balb/c mice. Based on these data SB366791 is a more selective and in vivo also a more potent TRPV1 receptor antagonist than capsazepine in the rat therefore, it may promote the assessment of the therapeutic utility of TRPV1 channel blockers.

Authors+Show Affiliations

Department of Pharmacology and Pharmacotherapy, Faculty of Medicine, University of Pécs, H-7643 Pécs, Szigeti u. 12, Hungary.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo 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

15950380

Citation

Varga, Angelika, et al. "Effects of the Novel TRPV1 Receptor Antagonist SB366791 in Vitro and in Vivo in the Rat." Neuroscience Letters, vol. 385, no. 2, 2005, pp. 137-42.
Varga A, Németh J, Szabó A, et al. Effects of the novel TRPV1 receptor antagonist SB366791 in vitro and in vivo in the rat. Neurosci Lett. 2005;385(2):137-42.
Varga, A., Németh, J., Szabó, A., McDougall, J. J., Zhang, C., Elekes, K., Pintér, E., Szolcsányi, J., & Helyes, Z. (2005). Effects of the novel TRPV1 receptor antagonist SB366791 in vitro and in vivo in the rat. Neuroscience Letters, 385(2), 137-42.
Varga A, et al. Effects of the Novel TRPV1 Receptor Antagonist SB366791 in Vitro and in Vivo in the Rat. Neurosci Lett. 2005 Sep 9;385(2):137-42. PubMed PMID: 15950380.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effects of the novel TRPV1 receptor antagonist SB366791 in vitro and in vivo in the rat. AU - Varga,Angelika, AU - Németh,József, AU - Szabó,Arpád, AU - McDougall,Jason J, AU - Zhang,Chunfen, AU - Elekes,Krisztián, AU - Pintér,Erika, AU - Szolcsányi,János, AU - Helyes,Zsuzsanna, PY - 2005/02/18/received PY - 2005/04/13/revised PY - 2005/05/09/accepted PY - 2005/6/14/pubmed PY - 2005/10/12/medline PY - 2005/6/14/entrez SP - 137 EP - 42 JF - Neuroscience letters JO - Neurosci Lett VL - 385 IS - 2 N2 - The TRPV1 capsaicin receptor is a non-selective cation channel localized in the cell membrane of a subset of primary sensory neurons and functions as an integrator molecule in nociceptive/inflammatory processes. The present paper characterizes the effects of SB366791, a novel TRPV1 antagonist, on capsaicin-evoked responses both in vitro and in vivo using rat models. SB366791 (100 and 500 nM) significantly inhibited capsaicin-evoked release of the pro-inflammatory sensory neuropeptide substance P from isolated tracheae, while it did not influence electrically induced neuropeptide release. It also decreased capsaicin-induced Ca2+ influx in cultured trigeminal ganglion cells in a concentration-dependent manner (0.5-10 microM) with an IC50 of 651.9 nM. In vivo 500 microg/kg i.p. dose of SB366791 significantly inhibited capsaicin-induced hypothermia, wiping movements and vasodilatation in the knee joint, while 2 mg/kg capsazepine was ineffective, its effect lasted for 1h. However, neither antagonist was able to inhibit capsaicin-evoked hypothermia in Balb/c mice. Based on these data SB366791 is a more selective and in vivo also a more potent TRPV1 receptor antagonist than capsazepine in the rat therefore, it may promote the assessment of the therapeutic utility of TRPV1 channel blockers. SN - 0304-3940 UR - https://www.unboundmedicine.com/medline/citation/15950380/Effects_of_the_novel_TRPV1_receptor_antagonist_SB366791_in_vitro_and_in_vivo_in_the_rat_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0304-3940(05)00561-6 DB - PRIME DP - Unbound Medicine ER -