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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]
↑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 Chemistry4: 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 chemistry43 (24): 4667–77. PMID11101358.
↑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 chemistry39 (12): 1047–57. DOI:10.1016/j.ejmech.2004.09.009. PMID15571866.
↑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 therapeutics303 (1): 424–30. DOI:10.1124/jpet.102.036095. PMID12235279.
↑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 neuroscience23 (4): 995–1004. DOI:10.1111/j.1460-9568.2006.04623.x. PMID16519664.
↑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 neuroscience17 (7): 1384–92. PMID12713641.
↑Suyama H, Kawamoto M, Gaus S, Yuge O (2003). „Effect of JTC-801 (nociceptin antagonist) on neuropathic pain in a rat model”. Neuroscience letters351 (3): 133–6. PMID14623124.
↑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 pharmacology510 (3): 223–8. DOI:10.1016/j.ejphar.2005.01.033. PMID15763246.