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JTC-801 je selektivni antagonist nociceptinskog receptora.[3] 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.[4] Lekovi koji deluju na nociceptinski receptor mogu da imaju uticaj na dejstvo tradicionalnih analgetika kao što su inhibitori prostaglandinske sintetaze (NSAID),[5]μ-opioidne agoniste,[6] i kanabinoide.[7]
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.[8][9][10]
^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. PMID15571866. doi:10.1016/j.ejmech.2004.09.009.
^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. PMID12235279. doi:10.1124/jpet.102.036095.
^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. PMID16519664. doi:10.1111/j.1460-9568.2006.04623.x.
^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. PMID12713641.
^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. 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 pharmacology. 510 (3): 223—8. PMID15763246. doi:10.1016/j.ejphar.2005.01.033.