JTC-801

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IUPAC_name = N-(4-amino-2-methylquinolin-6-yl)-2- [(4-ethylphenoxy)methyl] benzamide


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CAS_number = 244218-51-7
synonyms = JTC-801
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PubChem = 5311339
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C = 26 | H = 25 | N = 3 | O = 2
molecular_weight = 411.51 g/mol
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JTC-801 is an opioid analgesic drug used in scientific research. [Shinkai H, Ito T, Iida T, Kitao Y, Yamada H, Uchida I. 4-Aminoquinolines: novel nociceptin antagonists with analgesic activity. "Journal of Medicinal Chemistry". 2000 Nov 30;43(24):4667-77. PMID 11101358] [Yamada H, Nakamoto H, Suzuki Y, Ito T, Aisaka K. Pharmacological profiles of a novel opioid receptor-like1 (ORL(1)) receptor antagonist, JTC-801. "British Journal of Pharmacology". 2002 Jan;135(2):323-32. PMID 11815367]

JTC-801 is a selective antagonist for the nociceptin receptor, also known as the ORL-1 receptor. [Sestili I, Borioni A, Mustazza C, Rodomonte A, Turchetto L, Sbraccia M, Riitano D, Del Giudice MR. 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". 2004 Dec;39(12):1047-57. PMID 15571866] This was the fourth opioid receptor to be discovered, and is still the least understood. The noiciceptin receptor has complex effects which are involved in many processes to do with pain and inflammation, and activation of this receptor can either increase or reduce pain depending on dose. [Muratani T, Minami T, Enomoto U, Sakai M, Okuda-Ashitaka E, Kiyokane K, Mori H, Ito S. Characterization of nociceptin/orphanin FQ-induced pain responses by the novel receptor antagonist N-(4-amino-2-methylquinolin-6-yl)-2-(4-ethylphenoxymethyl) benzamide monohydrochloride. "Journal of Pharmacology and Experimental Therapeutics". 2002 Oct;303(1):424-30. PMID 12235279] Drugs acting at the noiciceptin receptor may influence the effects of traditional analgesics including prostaglandin synthetase inhibitors such as NSAIDs, [Okuda-Ashitaka E, Minami T, Matsumura S, Takeshima H, Reinscheid RK, Civelli O, Ito S. The opioid peptide nociceptin/orphanin FQ mediates prostaglandin E2-induced allodynia, tactile pain associated with nerve injury. "European Journal of Neuroscience". 2006 Feb;23(4):995-1004. PMID 16519664] μ-opioid agonist drugs, [Zaveri N, Jiang F, Olsen C, Polgar W, Toll L. Small-molecule agonists and antagonists of the opioid receptor-like receptor (ORL1, NOP): ligand-based analysis of structural factors influencing intrinsic activity at NOP. "AAPS Journal". 2005 Oct 5;7(2):E345-52. PMID 16353914] and cannabinoids. [Rawls SM, Schroeder JA, Ding Z, Rodriguez T, Zaveri N. NOP receptor antagonist, JTC-801, blocks cannabinoid-evoked hypothermia in rats. "Neuropeptides". 2007 Aug;41(4):239-47. PMID 17512052]

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. [Mabuchi T, Matsumura S, Okuda-Ashitaka E, Kitano T, Kojima H, Nagano T, Minami T, Ito S. Attenuation of neuropathic pain by the nociceptin/orphanin FQ antagonist JTC-801 is mediated by inhibition of nitric oxide production. "European Journal of Neuroscience". 2003 Apr;17(7):1384-92. PMID 12713641] [Suyama H, Kawamoto M, Gaus S, Yuge O. Effect of JTC-801 (nociceptin antagonist) on neuropathic pain in a rat model. "Neuroscience Letters". 2003 Nov 20;351(3):133-6. PMID 14623124] [Tamai H, Sawamura S, Takeda K, Orii R, Hanaoka K. Anti-allodynic and anti-hyperalgesic effects of nociceptin receptor antagonist, JTC-801, in rats after spinal nerve injury and inflammation. "European Journal of Pharmacology". 2005 Mar 14;510(3):223-8. PMID 15763246]

References