JTC-801 explained

JTC-801 is an opioid analgesic drug used in scientific research.^{[1] [2]}

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]}

See also

• J-113,397
• LY-2940094
• SB-612,111

Notes and References

1. Shinkai H, Ito T, Iida T, Kitao Y, Yamada H, Uchida I . 4-Aminoquinolines: novel nociceptin antagonists with analgesic activity . Journal of Medicinal Chemistry . 43 . 24 . 4667–77 . November 2000 . 11101358 . 10.1021/jm0002073 .
2. 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 . 135 . 2 . 323–32 . January 2002 . 11815367 . 1573142 . 10.1038/sj.bjp.0704478 .
3. Sestili I, Borioni A, Mustazza C, Rodomonte A, Turchetto L, Sbraccia M, Riitano D, Del Giudice MR . 6 . 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 . December 2004 . 15571866 . 10.1016/j.ejmech.2004.09.009 .
4. Muratani T, Minami T, Enomoto U, Sakai M, Okuda-Ashitaka E, Kiyokane K, Mori H, Ito S . 6 . 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 . The Journal of Pharmacology and Experimental Therapeutics . 303 . 1 . 424–30 . October 2002 . 12235279 . 10.1124/jpet.102.036095 . 1162524 .
5. 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 . The European Journal of Neuroscience . 23 . 4 . 995–1004 . February 2006 . 16519664 . 10.1111/j.1460-9568.2006.04623.x . 39006891 .
6. 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 . The AAPS Journal . 7 . 2 . E345-52 . October 2005 . 16353914 . 2750971 . 10.1208/aapsj070234 .
7. Rawls SM, Schroeder JA, Ding Z, Rodriguez T, Zaveri N . NOP receptor antagonist, JTC-801, blocks cannabinoid-evoked hypothermia in rats . Neuropeptides . 41 . 4 . 239–47 . August 2007 . 17512052 . 10.1016/j.npep.2007.03.001 . 19443938 .
8. Mabuchi T, Matsumura S, Okuda-Ashitaka E, Kitano T, Kojima H, Nagano T, Minami T, Ito S . 6 . 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 . April 2003 . 12713641 . 10.1046/j.1460-9568.2003.02575.x . 36588304 .
9. Suyama H, Kawamoto M, Gaus S, Yuge O . Effect of JTC-801 (nociceptin antagonist) on neuropathic pain in a rat model . Neuroscience Letters . 351 . 3 . 133–6 . November 2003 . 14623124 . 10.1016/S0304-3940(03)00502-0 . 20099481 .
10. 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 . 510 . 3 . 223–8 . March 2005 . 15763246 . 10.1016/j.ejphar.2005.01.033 .