SB-408124

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SB-408124
SB-408,124.svg
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
ECHA InfoCard 100.164.461
Chemical and physical data
Formula C19H18F2N4O
Molar mass 356.368 g/mol
3D model (JSmol)
 NYesY (what is this?)  (verify)

SB-408124 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-334867. It is used in scientific research into the function of orexinergic neurons in the body.[1][2]

References[edit]

  1. ^ Langmead, CJ; Jerman, JC; Brough, SJ; Scott, C; Porter, RA; Herdon, HJ (2004). "Characterisation of the binding of 3H-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor". British Journal of Pharmacology. 141 (2): 340–6. PMC 1574197Freely accessible. PMID 14691055. doi:10.1038/sj.bjp.0705610. 
  2. ^ Peng, HY; Chang, HM; Chang, SY; Tung, KC; Lee, SD; Chou, D; Lai, CY; Chiu, CH; et al. (2008). "Orexin-A modulates glutamatergic NMDA-dependent spinal reflex potentiation via inhibition of NR2B subunit". American Journal of Physiology. Endocrinology and Metabolism. 295 (1): E117–29. PMID 18477704. doi:10.1152/ajpendo.90243.2008.