SB-408124

SB-408124
Identifiers
CAS Number 288150-92-5 YesY
PubChem (CID) 4331799
IUPHAR/BPS 1704
ChemSpider 3536200 N
ECHA InfoCard 100.164.461
Chemical and physical data
Formula C19H18F2N4O
Molar mass 356.368 g/mol
3D model (Jmol) Interactive image
 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

  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. doi:10.1038/sj.bjp.0705610. PMC 1574197Freely accessible. PMID 14691055.
  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. doi:10.1152/ajpendo.90243.2008. PMID 18477704.


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