title: Effect of JTC-801 (nociceptin antagonist) on neuropathic pain in a rat model.
abstract: JTC-801, a nociceptin antagonist, may alleviate neuropathic pain because nociceptin has been shown to produce pain modulation. We report that JTC-801 alleviates heat-evoked hyperalgesia and investigated the possible protective effect on osteoporosis induced by chronic constriction injury (CCI) in rats. JTC-801 was given orally to rats with CCI at 0% (vehicle), 0.03% (low dose), or 0.06% (high dose) in food. Paw withdrawal latency (PWL) to heat, bone mineral content (BMC) and bone mineral density (BMD) of the whole tibial bone were measured. JTC-801 dose-dependently normalized PWL. Although JTC-801 did not inhibit a CCI-induced decrease in BMC and BMD, it inhibited an increase in the number of osteoclasts in the JTC-801 groups. JTC-801, given orally in food, alleviated heat-evoked hyperalgesia in CCI rats, suggesting that it is useful for the treatment of neuropathic pain.
authors: Department of Anesthesiology and Critical Care, Graduate School of Biomedical Sciences, Hiroshima University, Kasumi 1-2-3, Minami-ku, Hiroshima 734-8551, Japan. h.suyama@ccv.ne.jp
authors: Hidemichi
authors: H
authors: Suyama
authors: Masashi
authors: M
authors: Kawamoto
authors: Syafruddin
authors: S
authors: Gaus
authors: Osafumi
authors: O
authors: Yuge
mesh_terms: D000634:Aminoquinolines / Q000008:administration & dosage*; D000818:Animals; D001549:Benzamides / Q000008:administration & dosage*; D004195:Disease Models, Animal; D006930:Hyperalgesia / Q000188:drug therapy* / Q000473:pathology; D008297:Male; D018847:Opioid Peptides / Q000037:antagonists & inhibitors*; D010147:Pain Measurement / Q000187:drug effects*; D051381:Rats; D017207:Rats, Sprague-Dawley; D000097629:Nociceptin
chemical_list: D000634:Aminoquinolines; D001549:Benzamides; D018847:Opioid Peptides; D000097629:Nociceptin; C433236:N-(4-amino-2-methylquinolin-6-yl)-2-(4-ethylphenoxymethyl)benzamide