Cat. No. 4317
Chemical Name: N-(2,4-Dibromophenyl)-N'-[(4S,5S)-2,
Biological ActivitySelective OX2 receptor antagonist (pIC50 = 7.4 for chimeric OX2 receptors; pKB values are 5.9 and 8.5 for OX1 and OX2 receptors respectively). Shows no significant activity in a panel of over 50 other neurotransmitters and neuropeptide receptors. Achieves high level of OX2 receptor occupancy in the rat brain; exhibits sleep-promoting effects in rats.
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 Datasheet
References are publications that support the products' biological activity.
Gozzi et al (2011) Functional magnetic resonance imaging reveals different neural substrates for the effects of orexin-1 and orexin-2 receptor antagonists. PLoS ONE 6 e16406. PMID: 21307957.
Tran et al (2011) Chimeric, mutant orexin receptors show key interactions between orexin receptors, peptides and antagonists. Eur.J.Pharmacol. 667 120. PMID: 21679703.
Dugovic et al (2009) Blockade of orexin-1 receptors attenuates orexin-2 receptor antagonism-induced sleep promotion in the rat. J.Pharmacol.Exp.Ther. 330 142. PMID: 19363060.
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Keywords: JNJ 10397049, supplier, JNJ10397049, Orexins, hypocretins, receptors, antagonists, selective, OX2R, OX2, sleep, Tocris Bioscience, OX2 Receptor Antagonist products