Catalog Number: 4317
Chemical Name: N-(2,4-Dibromophenyl)-N'-[(4S,5S)-2,2-dimethyl-4-phenyl-1,3-dioxan-5-yl]-urea
Biological Activity
Selective 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.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in DMSO and to 100 mM in ethanol
  • Purity:
  • Storage:
    Store at +4°C
  • CAS No:
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. Blockade of orexin-1 receptors attenuates orexin-2 receptor antagonism-induced sleep promotion in the rat.
    Dugovic et al.
    J.Pharmacol.Exp.Ther., 2009;330:142
  2. Chimeric, mutant orexin receptors show key interactions between orexin receptors, peptides and antagonists.
    Tran et al.
    Eur.J.Pharmacol., 2011;667:120
  3. Functional magnetic resonance imaging reveals different neural substrates for the effects of orexin-1 and orexin-2 receptor antagonists.
    Gozzi et al.
    PLoS ONE, 2011;6:e16406
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