SB-408124 explained

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]

Notes and 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 . 141 . 2 . 340–6 . January 2004 . 14691055 . 1574197 . 10.1038/sj.bjp.0705610 .
  2. Peng HY, Chang HM, Chang SY, Tung KC, Lee SD, Chou D, Lai CY, Chiu CH, Chen GD, Lin TB . 6 . 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 . July 2008 . 18477704 . 10.1152/ajpendo.90243.2008 . 587272 .

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