JTC-801

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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[1][2] 5311339
Hemijski podaci
Formula C26H25N3O2 
Mol. masa 411.51 g/mol
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]

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Literatura[uredi - уреди | uredi izvor]

  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. PMID 20970519. doi:10.1016/j.drudis.2010.10.003.  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. PMC 1573142. PMID 11815367. doi:10.1038/sj.bjp.0704478. 
  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. PMID 15571866. doi:10.1016/j.ejmech.2004.09.009. 
  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. PMID 12235279. doi:10.1124/jpet.102.036095. 
  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. PMID 16519664. doi:10.1111/j.1460-9568.2006.04623.x. 
  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. PMC 2750971. PMID 16353914. doi:10.1208/aapsj070234. 
  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. PMID 17512052. doi:10.1016/j.npep.2007.03.001. 
  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. PMID 15763246. doi:10.1016/j.ejphar.2005.01.033. 

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