JTC 801 | Opioid Receptors | Selective ORL1 Antagonist | JTC801

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Cat.No.	Product Name
2481	JTC 801

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JTC 801

Chemical Name: N-(4-Amino-2-methyl-6-quinolinyl)-2-[(4-ethylphenoxy)me thyl]benzamide hydrochloride

Biological Activity:

High affinity, selective ORL₁ receptor antagonist (K_i = 8.2 nM). Displays approximately 12.5-, 129- and 1055-fold selectivity over human μ-, κ- and δ-opioid receptors respectively. In vivo shows anti-nociceptive effects in acute pain models. Orally active.

Technical Data:

M.Wt:	447.96
Formula:	C₂₆H₂₅N₃O₂.HCl
Storage:	Desiccate at RT
Solubility:	Soluble to 5 mM in Water and to 100 mM in DMSO
Purity:	>98%
CAS No:	[244218-51-7]

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References:

Shinkai et al (2000) 4-Aminoquinolines: novel nociceptin antagonists with analgesic activity. J.Med.Chem 43 4667. Yamada et al (2002) Pharmacological profiles of a novel opioid receptor-like1 (ORL1) receptor antagonist, JTC-801. Br.J.Pharmacol. 135 323. 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.

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Keywords: JTC 801, Opioid Receptors, Selective ORL1 Antagonist, JTC801, Tocris Bioscience

Literature in this Area

Scientific Reviews

Opioid Receptors
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