Catalog Number: 2481
Chemical Name: N-(4-Amino-2-methyl-6-quinolinyl)-2-[(4-ethylphenoxy)methyl]benzamide hydrochloride
Biological Activity
High affinity, selective NOP receptor antagonist (Ki = 8.2 nM). Displays approximately 12.5-, 129- and 1055-fold selectivity over human μ-, κ- and δ-opioid receptors respectively. Exhibits anti-nociceptive effects in acute pain models in vivo. Orally active.
Technical Data
  • M.Wt:
    447.96
  • Formula:
    C26H25N3O2.HCl
  • Solubility:
    Soluble to 100 mM in DMSO and to 20 mM in ethanol
  • Purity:
    >98%
  • Storage:
    Desiccate at RT
  • CAS No:
    244218-51-7
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Pharmacological profiles of a novel opioid receptor-like1 (ORL1) receptor antagonist, JTC-801.
    Yamada et al.
    Br.J.Pharmacol., 2002;135:323
  2. 4-Aminoquinolines: novel nociceptin antagonists with analgesic activity.
    Shinkai et al.
    J.Med.Chem, 2000;43:4667
  3. Anti-allodynic and anti-hyperalgesic effects of nociceptin receptor antagonist, JTC-801, in rats after spinal nerve injury and inflammation.
    Tamai et al.
    Eur.J.Pharmacol., 2005;510:223
Citations:

The citations listed below are publications that use Tocris products. Selected citations for JTC 801 include:

2 Citations: Showing 1 - 2
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  1. Nociceptin/orphanin FQ peptide receptor antagonist JTC-801 reverses pain and anxiety symptoms in a rat model of post-traumatic stress disorder.
    Authors: Zhang Et al.
    PLoS One 2015;172:571
  2. Modulation of silent and constitutively active nociceptin/orphanin FQ receptors by potent receptor antagonists and Na+ ions in rat sympathetic neurons.
    Authors: Mahmoud Et al.
    Mol Pharmacol 2010;77:804

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