JTC-801: Difference between revisions

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'''JTC-801''' is an [[opioid]] [[analgesic]] drug used in scientific research.<ref>{{cite journal | last1vauthors = Shinkai | first1 = H | last2 =, Ito | first2 = T | last3 =, Iida | first3 = T | last4 =, Kitao | first4 = Y | last5 =, Yamada | first5 = H | last6 =, Uchida | first6 = I | title = 4-Aminoquinolines: novel nociceptin antagonists with analgesic activity | journal = Journal of medicinalMedicinal chemistryChemistry | volume = 43 | issue = 24 | pages = 4667–77 | yeardate = November 2000 | pmid = 11101358 | author-separatordoi =, | author-name-separator= | doi=10.1021/jm0002073 }}</ref><ref>{{cite journal | last1vauthors = Yamada | first1 = H | last2 =, Nakamoto | first2 = H | last3 =, Suzuki | first3 = Y | last4 =, Ito | first4 = T | last5 =, Aisaka | first5 = K | title = Pharmacological profiles of a novel opioid receptor-like1 (ORL1ORL(1)) receptor antagonist, JTC-801 | journal = British journalJournal of pharmacologyPharmacology | volume = 135 | issue = 2 | pages = 323–32 | yeardate = January 2002 | pmid = 11815367 | author-separator =, | author-name-separator= | pmc = 1573142 | doi = 10.1038/sj.bjp.0704478 }}</ref>

JTC-801 is a selective antagonist for the [[nociceptin receptor]], also known as the ORL-1 receptor.<ref>{{cite journal | last1vauthors = Sestili | first1 = I | last2 =, Borioni | first2 = A | last3 =, Mustazza | first3 = C | last4 =, Rodomonte | first4 = A | last5 =, Turchetto | first5 = L | last6 =, Sbraccia | first6 = M | last7 =, Riitano | first7 = D | last8 =, Del Giudice MR | first8display-authors = MR6 | title = 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 | journal = European journalJournal of medicinalMedicinal chemistryChemistry | volume = 39 | issue = 12 | pages = 1047–57 | yeardate = December 2004 | pmid = 15571866 | author-separator =, | author-name-separator= | doi = 10.1016/j.ejmech.2004.09.009 }}</ref> This was the fourth opioid receptor to be discovered, and is still the least understood. The noiciceptinnociceptin receptor has complex effects which are involved in many processes toinvolved do within pain and inflammation responses, and activation of this receptor can either increase or reduce pain depending on dose.<ref>{{cite journal | last1vauthors = Muratani | first1 = T | last2 =, Minami | first2 = T | last3 =, Enomoto | first3 = U | last4 =, Sakai | first4 = M | last5 =, Okuda-Ashitaka | first5 = E | last6 =, Kiyokane | first6 = K | last7 =, Mori | first7 = H, |Ito last8 = ItoS | first8display-authors = S6 | title = 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 = The Journal of pharmacologyPharmacology and experimentalExperimental therapeuticsTherapeutics | volume = 303 | issue = 1 | pages = 424–30 | yeardate = October 2002 | pmid = 12235279 | author-separatordoi =, 10.1124/jpet.102.036095 | author-name-separators2cid = 1162524 | doiurl = 10.1124https:/jpet/semanticscholar.102.036095org/paper/249f8d3cc1b82e7edce4458e27b7b6aa0f1a3d29 }}</ref> Drugs acting at the noiciceptin receptor may influence the effects of traditional analgesics including prostaglandin synthetase inhibitors such as [[NSAID]]s,<ref>{{cite journal | last1vauthors = Okuda-Ashitaka | first1 = E | last2 =, Minami | first2 = T | last3 =, Matsumura | first3 = S | last4 =, Takeshima | first4 = H | last5 =, Reinscheid | first5 = RK | last6 =, Civelli | first6 = O | last7 =, Ito | first7 = S | title = The opioid peptide nociceptin/orphanin FQ mediates prostaglandin E2-induced allodynia, tactile pain associated with nerve injury | journal = The European journalJournal of neuroscienceNeuroscience | volume = 23 | issue = 4 | pages = 995–1004 | yeardate = February 2006 | pmid = 16519664 | author-separator =, | author-name-separator= | doi = 10.1111/j.1460-9568.2006.04623.x | s2cid = 39006891 }}</ref> [[mu opioid receptor|μ-opioid]] agonist drugsagonists,<ref>{{cite journal | last1vauthors = Zaveri | first1 = N | last2 =, Jiang | first2 = F | last3 =, Olsen | first3 = C | last4 =, Polgar | first4 = W | last5 =, Toll | first5 = L | title = Small-molecule agonists and antagonists of the opioid receptor-like receptor (ORL1, NOP): Ligandligand-based analysis of structural factors influencing intrinsic activity at NOP | journal = The AAPS journalJournal | volume = 7 | issue = 2 | pages = E345–52E345-52 | yeardate = October 2005 | pmid = 16353914 | author-separator =, | author-name-separator= | pmc = 2750971 | doi = 10.1208/aapsj070234 }}</ref> and [[cannabinoids]].<ref>{{cite journal | last1vauthors = Rawls | first1 = SM | last2 =, Schroeder | first2 = JA | last3 =, Ding | first3 = Z | last4 =, Rodriguez | first4 = T | last5 =, Zaveri | first5 = N | title = NOP receptor antagonist, JTC-801, blocks cannabinoid-evoked hypothermia in rats | journal = Neuropeptides | volume = 41 | issue = 4 | pages = 239–47 | yeardate = August 2007 | pmid = 17512052 | author-separator =, | author-name-separator= | doi = 10.1016/j.npep.2007.03.001 | s2cid = 19443938 }}</ref>

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.<ref>{{cite journal | last1vauthors = Mabuchi | first1 = T | last2 =, Matsumura | first2 = S | last3 =, Okuda-Ashitaka | first3 = E | last4 =, Kitano | first4 = T | last5 =, Kojima | first5 = H | last6 =, Nagano | first6 = T | last7 =, Minami | first7 = T, |Ito last8 = ItoS | first8display-authors = S6 | title = Attenuation of neuropathic pain by the nociceptin/orphanin FQ antagonist JTC-801 is mediated by inhibition of nitric oxide production | journal = The European journalJournal of neuroscienceNeuroscience | volume = 17 | issue = 7 | pages = 1384–92 | yeardate = April 2003 | pmid = 12713641 | author-separator =, | author-name-separator= | doi = 10.1046/j.1460-9568.2003.02575.x | s2cid = 36588304 }}</ref><ref>{{cite journal | last1vauthors = Suyama | first1 = H | last2 =, Kawamoto | first2 = M | last3 =, Gaus | first3 = S | last4 =, Yuge | first4 = O | title = Effect of JTC-801 (nociceptin antagonist) on neuropathic pain in a rat model | journal = Neuroscience lettersLetters | volume = 351 | issue = 3 | pages = 133–6 | yeardate = November 2003 | pmid = 14623124 | author-separatordoi =, | author-name-separator= | doi=10.1016/S0304-3940(03)00502-0 | s2cid = 20099481 }}</ref><ref>{{cite journal | last1vauthors = Tamai | first1 = H | last2 =, Sawamura | first2 = S | last3 =, Takeda | first3 = K | last4 =, Orii | first4 = R | last5 =, Hanaoka | first5 = K | title = Anti-allodynic and anti-hyperalgesic effects of nociceptin receptor antagonist, JTC-801, in rats after spinal nerve injury and inflammation | journal = European journalJournal of pharmacologyPharmacology | volume = 510 | issue = 3 | pages = 223–8 | yeardate = March 2005 | pmid = 15763246 | author-separator =, | author-name-separator= | doi = 10.1016/j.ejphar.2005.01.033 }}</ref>

== See also ==

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