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.
journal_name
Neurosci Lettjournal_title
Neuroscience lettersauthors
Varga A,Németh J,Szabó A,McDougall JJ,Zhang C,Elekes K,Pintér E,Szolcsányi J,Helyes Zdoi
10.1016/j.neulet.2005.05.015keywords:
subject
Has Abstractpub_date
2005-09-09 00:00:00pages
137-42issue
2eissn
0304-3940issn
1872-7972pii
S0304-3940(05)00561-6journal_volume
385pub_type
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