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by | Mar 16, 2018 | Hosta

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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 (January 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 1574197. PMID 14691055.
  2. ^ Peng HY, Chang HM, Chang SY, Tung KC, Lee SD, Chou D, et al. (July 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. S2CID 587272.
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