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SB-408,124: Wikis

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SB-408,124
Systematic (IUPAC) name
N-(6,8-Difluoro-2-methyl-4-quinolinyl)-N'-[4-(dimethylamino)phenyl]urea
Identifiers
CAS number 288150-92-5
ATC code  ?
Chemical data
Formula C19H18F2N4O 
Mol. mass 356.368 g/mol
SMILES eMolecules & PubChem
Therapeutic considerations
Pregnancy cat.  ?
Legal status

SB-408,124 is a drug which is a non-peptide antagonist selective for the orexin receptor subtype OX1, with around 70x selectivity for OX1 over OX2 receptors, and improved oral bioavailability compared to the older OX1 antagonist SB-334,867. It is used in scientific research into the function of orexinergic neurons in the body.[1][2]

References

  1. ^ Langmead CJ, Jerman JC, Brough SJ, Scott C, Porter RA, Herdon HJ. Characterisation of the binding of [3H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor. British Journal of Pharmacology. 2004 Jan;141(2):340-6. PMID 14691055
  2. ^ Peng HY, Chang HM, Chang SY, Tung KC, Lee SD, Chou D, Lai CY, Chiu CH, Chen GD, Lin TB. Orexin-A modulates glutamatergic NMDA-dependent spinal reflex potentiation via inhibition of NR2B subunit. American Journal of Physiology. Endocrinology and Metabolism. 2008 Jul;295(1):E117-29. PMID 18477704
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