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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.
|Storage||Desiccate at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 447.96. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.23 mL||11.16 mL||22.32 mL|
|5 mM||0.45 mL||2.23 mL||4.46 mL|
|10 mM||0.22 mL||1.12 mL||2.23 mL|
|50 mM||0.04 mL||0.22 mL||0.45 mL|
References are publications that support the biological activity of the product.
Shinkai et al (2000) 4-Aminoquinolines: novel nociceptin antagonists with analgesic activity. J.Med.Chem 43 4667 PMID: 11101358
Yamada et al (2002) Pharmacological profiles of a novel opioid receptor-like1 (ORL1) receptor antagonist, JTC-801. Br.J.Pharmacol. 135 323 PMID: 11815367
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
If you know of a relevant reference for JTC 801, please let us know.
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Keywords: JTC 801, JTC 801 supplier, Selective, NOP, antagonists, Nociceptin, Receptors, ORL1, OP4, Opioids, JTC801, 2481, Tocris Bioscience
3 Citations for JTC 801
Citations are publications that use Tocris products. Selected citations for JTC 801 include:
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
Delaney et al (2012) Role of nociceptin/orphanin FQ and NOP receptors in the response to acute and repeated restraint stress in rats. J Neuroendocrinol 24 1527 PMID: 22835008
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
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Literature in this Area
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Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.