JTC-801

JTC-801
Clinical data
Other names	JTC-801
Identifiers
	IUPAC name N-(4-amino-2-methylquinolin-6-yl)-2-[(4-ethylphenoxy)methyl]benzamide;
CAS Number	244218-51-7 ;
PubChem CID	5311340;
IUPHAR/BPS	1692;
ChemSpider	4470841 ;
UNII	7I21WLZ2FP;
CompTox Dashboard (EPA)	DTXSID301158085 ;
Chemical and physical data
Formula	C26H25N3O2
Molar mass	411.505 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES O=C(c1ccccc1COc2ccc(cc2)CC)Nc3ccc4nc(cc(c4c3)N)C;
	InChI InChI=1S/C26H25N3O2/c1-3-18-8-11-21(12-9-18)31-16-19-6-4-5-7-22(19)26(30)29-20-10-13-25-23(15-20)24(27)14-17(2)28-25/h4-15H,3,16H2,1-2H3,(H2,27,28)(H,29,30) ; Key:VTGBZWHPJFMTKS-UHFFFAOYSA-N ;
	(what is this?) (verify)

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]

References

^ Shinkai H, Ito T, Iida T, Kitao Y, Yamada H, Uchida I (November 2000). "4-Aminoquinolines: novel nociceptin antagonists with analgesic activity". Journal of Medicinal Chemistry. 43 (24): 4667–77. doi:10.1021/jm0002073. PMID 11101358.
^ Yamada H, Nakamoto H, Suzuki Y, Ito T, Aisaka K (January 2002). "Pharmacological profiles of a novel opioid receptor-like1 (ORL(1)) receptor antagonist, JTC-801". British Journal of Pharmacology. 135 (2): 323–32. doi:10.1038/sj.bjp.0704478. PMC 1573142. PMID 11815367.
^ 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. PMID 15571866.
^ Muratani T, Minami T, Enomoto U, Sakai M, Okuda-Ashitaka E, Kiyokane K, et al. (October 2002). "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. doi:10.1124/jpet.102.036095. PMID 12235279. S2CID 1162524.
^ 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. PMID 16519664. S2CID 39006891.
^ Zaveri N, Jiang F, Olsen C, Polgar W, Toll L (October 2005). "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. doi:10.1208/aapsj070234. PMC 2750971. PMID 16353914.
^ Rawls SM, Schroeder JA, Ding Z, Rodriguez T, Zaveri N (August 2007). "NOP receptor antagonist, JTC-801, blocks cannabinoid-evoked hypothermia in rats". Neuropeptides. 41 (4): 239–47. doi:10.1016/j.npep.2007.03.001. PMID 17512052. S2CID 19443938.
^ 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. PMID 12713641. S2CID 36588304.
^ 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. PMID 14623124. S2CID 20099481.
^ 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. PMID 15763246.

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[1] Shinkai H, Ito T, Iida T, Kitao Y, Yamada H, Uchida I (November 2000). "4-Aminoquinolines: novel nociceptin antagonists with analgesic activity". Journal of Medicinal Chemistry. 43 (24): 4667–77. doi:10.1021/jm0002073. PMID 11101358.

[2] Yamada H, Nakamoto H, Suzuki Y, Ito T, Aisaka K (January 2002). "Pharmacological profiles of a novel opioid receptor-like1 (ORL(1)) receptor antagonist, JTC-801". British Journal of Pharmacology. 135 (2): 323–32. doi:10.1038/sj.bjp.0704478. PMC 1573142. PMID 11815367.

[3] 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. PMID 15571866.

[4] Muratani T, Minami T, Enomoto U, Sakai M, Okuda-Ashitaka E, Kiyokane K, et al. (October 2002). "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. doi:10.1124/jpet.102.036095. PMID 12235279. S2CID 1162524.

[5] 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. PMID 16519664. S2CID 39006891.

[6] Zaveri N, Jiang F, Olsen C, Polgar W, Toll L (October 2005). "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. doi:10.1208/aapsj070234. PMC 2750971. PMID 16353914.

[7] Rawls SM, Schroeder JA, Ding Z, Rodriguez T, Zaveri N (August 2007). "NOP receptor antagonist, JTC-801, blocks cannabinoid-evoked hypothermia in rats". Neuropeptides. 41 (4): 239–47. doi:10.1016/j.npep.2007.03.001. PMID 17512052. S2CID 19443938.

[8] 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. PMID 12713641. S2CID 36588304.

[9] 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. PMID 14623124. S2CID 20099481.

[10] 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. PMID 15763246.

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See also

References