JTC 801

Cat. No. 2481

JTC 801 C26H25N3O2.HCl [244218-51-7]

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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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Tamai et al (2005) Anti-allodynic and anti-hyperalgesic effects of nociceptin receptor antagonist, JTC-801, in rats after spinal nerve injury and inflammation. Eur.J.Pharmacol. 510 223. PMID: 15763246.

Yamada et al (2002) Pharmacological profiles of a novel opioid receptor-like1 (ORL1) receptor antagonist, JTC-801. Br.J.Pharmacol. 135 323. PMID: 11815367.

Shinkai et al (2000) 4-Aminoquinolines: novel nociceptin antagonists with analgesic activity. J.Med.Chem 43 4667. PMID: 11101358.

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Citations are publications that use Tocris products. Selected citations for JTC 801 include:

Zhang et al (2015) Nociceptin/orphanin FQ peptide receptor antagonist JTC-801 reverses pain and anxiety symptoms in a rat model of post-traumatic stress disorder. PLoS One 172 571. PMID: 24666365.

Mahmoud et al (2010) Modulation of silent and constitutively active nociceptin/orphanin FQ receptors by potent receptor antagonists and Na+ ions in rat sympathetic neurons. Mol Pharmacol 77 804. PMID: 20159949.

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Keywords: JTC 801, supplier, Selective, NOP, antagonists, Nociceptin, Receptors, ORL1, OP4, Opioids, JTC801, Tocris Bioscience, NOP Receptor Antagonist products

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