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JTC-801

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JTC-801 is an opioid analgesic drug used in scientific research.[1][2]

JTC-801
Clinical data
Other namesJTC-801
Identifiers
  • N-(4-amino-2-methylquinolin-6-yl)-2-[(4-ethylphenoxy)methyl]benzamide
CAS Number
PubChem CID
IUPHAR/BPS
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC26H25N3O2
Molar mass411.51 g/mol g·mol−1
  (verify)

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 noiciceptin receptor has complex effects which are involved in many processes to do with pain and inflammation, 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 including prostaglandin synthetase inhibitors such as NSAIDs,[5] μ-opioid agonist drugs,[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]

See also

References

  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. {{cite journal}}: Cite has empty unknown parameter: |author-name-separator= (help); Unknown parameter |author-separator= ignored (help)
  2. ^ 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. {{cite journal}}: Cite has empty unknown parameter: |author-name-separator= (help); Unknown parameter |author-separator= ignored (help)
  3. ^ 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. {{cite journal}}: Cite has empty unknown parameter: |author-name-separator= (help); Unknown parameter |author-separator= ignored (help)
  4. ^ 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. {{cite journal}}: Cite has empty unknown parameter: |author-name-separator= (help); Unknown parameter |author-separator= ignored (help)
  5. ^ 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. {{cite journal}}: Cite has empty unknown parameter: |author-name-separator= (help); Unknown parameter |author-separator= ignored (help)
  6. ^ 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. {{cite journal}}: Cite has empty unknown parameter: |author-name-separator= (help); Unknown parameter |author-separator= ignored (help)
  7. ^ 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. {{cite journal}}: Cite has empty unknown parameter: |author-name-separator= (help); Unknown parameter |author-separator= ignored (help)
  8. ^ 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. {{cite journal}}: Cite has empty unknown parameter: |author-name-separator= (help); Unknown parameter |author-separator= ignored (help)
  9. ^ 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. {{cite journal}}: Cite has empty unknown parameter: |author-name-separator= (help); Unknown parameter |author-separator= ignored (help)
  10. ^ 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. {{cite journal}}: Cite has empty unknown parameter: |author-name-separator= (help); Unknown parameter |author-separator= ignored (help)
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