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Cat. No. Name Size Price Add Cart
KI3310JTC-801QuoteQuote

Chemical Characteristic

Product NameJTC-801
CAS No.244218-51-7
Molecular Weight 447.963
FormulaC26H25N3O2.ClH
Chemical NameN-(4-amino-2-methylquinolin-6-yl)-2-((4-ethylphenoxy)methyl)benzamide hydrochloride
SmilesC(=O)(c1c(cccc1)COc1ccc(cc1)CC)Nc1cc2c(cc(nc2cc1)C)N Cl
Chemical Structure

Biological activities

JTC-801 is a potent and selective antagonist for opioid receptor-like1 (ORL1) receptor. JTC-801 inhibits the binding of [3H]nociceptin to human ORL1 receptors expressed in HeLa cells with a Ki value of 8.2 nM. JTC-801 weakly inhibits human µ-, Κ- and δ-opioid receptors, displaying approximately 12.5-, 129- and 1055-times less selectivity than ORL1 receptor, respectively.[1] In ORL1 receptor expressing HeLa cells in vitro, JTC-801 completely antagonizes the suppression of nociceptin on forskolin-induced accumulation of cyclic AMP with an IC50 of 2.58 µM.[2] In vivo, JTC-801 administration (0.01-0.1 mg/kg, i.v. or 1-10 mg/kg, p.o.) attenuates allodynia induced by the intrathecal injection of nociceptin in mice. In mouse hot-plate test, JTC-801 also prolongs escape response latency (ERL) to exposed heat stimulus with minimum effective doses (MED) of 0.01 mg/kg by i.v. or 1 mg/kg by p.o. In addition, JTC-801 reduces both the first and second phases of the nociceptive response with MED of 0.01 mg/kg by i.v. or 1 mg/kg by p.o. in the rat formalin test.[2] When given orally in food, JTC-801 alleviates heat-evoked hyperalgesia in a rat model.[3] Moreover, JTC-801 displays anti-allodynic and anti-hyperalgesic effects in rats after spinal nerve injury and inflammation in vivo.[4] Intraperitoneal administration of JTC-801 suppresses nitrous oxide-induced analgesia in 129Sv mice.[5]

Protocols

In vivo: JTC-801 is dissolved in normal saline.[5]

References

[1] Shinkai H, et al. 4-Aminoquinolines: novel nociceptin antagonists with analgesic activity. J Med Chem. 2000, 43(24): 4667-4677.
[2] Yamada H, et al. Pharmacological profiles of a novel opioid receptor-like1 (ORL(1)) receptor antagonist, JTC-801. Br J Pharmacol. 2002, 135(2): 323-332.
[3] Suyama H, et al. Effect of JTC-801 (nociceptin antagonist) on neuropathic pain in a rat model. Neurosci Lett. 2003, 351(3): 133-136.
[4] Tamai H, et al. Anti-allodynic and anti-hyperalgesic effects of nociceptin receptor antagonist, JTC-801, in rats after spinal nerve injury and inflammation. Eur J Pharmacol. 2005, 510(3): 223-228.
[5] Koyama T, et al. Nociceptin receptor antagonist JTC-801 inhibits nitrous oxide-induced analgesia in mice. J Anesth. 2009, 23(2): 301-303.

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