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Orexin Receptors

Orexin receptor antagonists block orexin receptors 1 and 2 (OX1, OX2), which respond to orexin neuropeptides. Orexin A and orexin B were described in 1998 as hypothalamic peptides that act on these two G protein-coupled receptors. In 1999 a mutation in the orexin receptor 2 gene was found to cause canine narcolepsy. Mice lacking orexin showed a narcolepsy-like phenotype in the same year, linking the system to sleep and wakefulness. OX1 is also studied in reward, addiction and stress, and OX2 mainly in arousal. SB 334867, SB-408124 and GSK1059865 are OX1-selective antagonists, and MK-3697 targets OX2. Almorexant, TCS 1102 and nemorexant are dual antagonists that block both orexin receptors.

2 Items

  • Tebideutorexant
    Cat. No.
    A62722
    CAS No.
    1637681-55-0

    Tebideutorexant

    Synonyms: JNJ-61393215

    Tebideutorexant is a selective inhibitor of the orexin receptor 1 (OX1R), demonstrating significant oral bioavailability and the ability to cross the blood-brain barrier. With a human OX1R pKi of 8.17 and a rat OX1R pKi of 8.13, this compound specifically targets OX1R while exerting minimal effects on OX2R. Tebideutorexant is a valuable tool for investigating panic and anxiety disorders in preclinical research settings.

    In stock View Details
    1 mg
    $180.00
    5 mg
    $410.00
    All 6 sizes

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