JTC-801

JTC-801
(IUPAC) ime
	N-(4-amino-2-methylquinolin-6-yl)-2-[(4-ethylphenoxy)methyl]benzamide
Klinički podaci
Identifikatori
CAS broj	244218-51-7
ATC kod	?
PubChem	5311339
Hemijski podaci
Formula	C26H25N3O2
Mol. masa	411.51 g/mol
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
Sinonimi	JTC-801
Farmakoinformacioni podaci
Trudnoća	?
Pravni status

JTC-801 je opioidni analgetik koji se koristi u naučnim istraživanjima.^[3]^[4]

JTC-801 je selektivni antagonist nociceptinskog receptora.^[5] U hronološkom redu otkrića to je bio četvrti opioidni receptor. On je još uvek najmanje istražen. Nociceptinski receptor proizvodi kompleksne efekte koji učestvuju u mnogim procesima vezanim za bol i inflamaciju. Aktivacija ovog receptora može bilo da povisi ili umanji bol u zavisnosti od doze.^[6] Lekovi koji deluju na nociceptinski receptor mogu da imaju uticaj na dejstvo tradicionalnih analgetika kao što su inhibitori prostaglandinske sintetaze (NSAID),^[7] μ-opioidne agoniste,^[8] i kanabinoide.^[9]

JTC-801 je oralno aktivni lek koji blokira nociceptinski receptor i proizvodi analgetske efekte u nizu studija na životinjama. On je posebno koristan u kontroli neuropatskog bola i alodinije vezanih za ozlede nerva.^[10]^[11]^[12]

Povezano

Literatura

↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
↑ Shinkai H, Ito T, Iida T, Kitao Y, Yamada H, Uchida I (2000). „4-Aminoquinolines: novel nociceptin antagonists with analgesic activity”. Journal of medicinal chemistry 43 (24): 4667–77. PMID 11101358.
↑ Yamada H, Nakamoto H, Suzuki Y, Ito T, Aisaka K (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, Riitano D, Del Giudice MR (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, Mori H, Ito S (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.
↑ Okuda-Ashitaka E, Minami T, Matsumura S, Takeshima H, Reinscheid RK, Civelli O, Ito S (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.
↑ Zaveri N, Jiang F, Olsen C, Polgar W, Toll L (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 (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.
↑ Mabuchi T, Matsumura S, Okuda-Ashitaka E, Kitano T, Kojima H, Nagano T, Minami T, Ito S (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. PMID 12713641.
↑ Suyama H, Kawamoto M, Gaus S, Yuge O (2003). „Effect of JTC-801 (nociceptin antagonist) on neuropathic pain in a rat model”. Neuroscience letters 351 (3): 133–6. PMID 14623124.
↑ Tamai H, Sawamura S, Takeda K, Orii R, Hanaoka K (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.

Vanjske veze

	Portal Medicina
	Portal Hemija

[1] Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit

[2] Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.

[3] Shinkai H, Ito T, Iida T, Kitao Y, Yamada H, Uchida I (2000). „4-Aminoquinolines: novel nociceptin antagonists with analgesic activity”. Journal of medicinal chemistry 43 (24): 4667–77. PMID 11101358.

[4] Yamada H, Nakamoto H, Suzuki Y, Ito T, Aisaka K (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.

[5] Sestili I, Borioni A, Mustazza C, Rodomonte A, Turchetto L, Sbraccia M, Riitano D, Del Giudice MR (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.

[6] Muratani T, Minami T, Enomoto U, Sakai M, Okuda-Ashitaka E, Kiyokane K, Mori H, Ito S (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.

[7] Okuda-Ashitaka E, Minami T, Matsumura S, Takeshima H, Reinscheid RK, Civelli O, Ito S (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.

[8] Zaveri N, Jiang F, Olsen C, Polgar W, Toll L (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.

[9] Rawls SM, Schroeder JA, Ding Z, Rodriguez T, Zaveri N (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.

[10] Mabuchi T, Matsumura S, Okuda-Ashitaka E, Kitano T, Kojima H, Nagano T, Minami T, Ito S (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. PMID 12713641.

[11] Suyama H, Kawamoto M, Gaus S, Yuge O (2003). „Effect of JTC-801 (nociceptin antagonist) on neuropathic pain in a rat model”. Neuroscience letters 351 (3): 133–6. PMID 14623124.

[12] Tamai H, Sawamura S, Takeda K, Orii R, Hanaoka K (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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