JTC-801 is a selective antagonist for the nociceptin receptor, also known as the ORL-1 receptor.[3] This was the fourth opioid receptor to be discovered and is still the least understood. The nociceptin receptor has complex effects which are involved in many processes involved in pain and inflammation responses, and activation of this receptor can either increase or reduce pain depending on dose.[4] Drugs acting at the noiciceptin receptor may influence the effects of traditional analgesics such as NSAIDs,[5]μ-opioid agonists,[6] and cannabinoids.[7]
JTC-801 is an orally active drug that blocks the nociceptin receptor and produces analgesic effects in a variety of animal studies, and is particularly useful for neuropathic pain and allodynia associated with nerve injury.[8][9][10]
^Sestili I, Borioni A, Mustazza C, Rodomonte A, Turchetto L, Sbraccia M, et al. (December 2004). "A new synthetic approach of N-(4-amino-2-methylquinolin-6-yl)-2-(4-ethylphenoxymethyl)benzamide (JTC-801) and its analogues and their pharmacological evaluation as nociceptin receptor (NOP) antagonists". European Journal of Medicinal Chemistry. 39 (12): 1047–57. doi:10.1016/j.ejmech.2004.09.009. PMID15571866.
^Okuda-Ashitaka E, Minami T, Matsumura S, Takeshima H, Reinscheid RK, Civelli O, Ito S (February 2006). "The opioid peptide nociceptin/orphanin FQ mediates prostaglandin E2-induced allodynia, tactile pain associated with nerve injury". The European Journal of Neuroscience. 23 (4): 995–1004. doi:10.1111/j.1460-9568.2006.04623.x. PMID16519664. S2CID39006891.
^Mabuchi T, Matsumura S, Okuda-Ashitaka E, Kitano T, Kojima H, Nagano T, et al. (April 2003). "Attenuation of neuropathic pain by the nociceptin/orphanin FQ antagonist JTC-801 is mediated by inhibition of nitric oxide production". The European Journal of Neuroscience. 17 (7): 1384–92. doi:10.1046/j.1460-9568.2003.02575.x. PMID12713641. S2CID36588304.
^Suyama H, Kawamoto M, Gaus S, Yuge O (November 2003). "Effect of JTC-801 (nociceptin antagonist) on neuropathic pain in a rat model". Neuroscience Letters. 351 (3): 133–6. doi:10.1016/S0304-3940(03)00502-0. PMID14623124. S2CID20099481.
^Tamai H, Sawamura S, Takeda K, Orii R, Hanaoka K (March 2005). "Anti-allodynic and anti-hyperalgesic effects of nociceptin receptor antagonist, JTC-801, in rats after spinal nerve injury and inflammation". European Journal of Pharmacology. 510 (3): 223–8. doi:10.1016/j.ejphar.2005.01.033. PMID15763246.