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  1. Hypocretin (orexin) receptor 2 - Wikipedia

    Orexin receptor type 2 (Ox2R or OX 2), also known as hypocretin receptor type 2 (HcrtR2), is a protein that in humans is encoded by the HCRTR2 gene. [5] It should not be confused for the …

  2. The Orexin/Receptor System: Molecular Mechanism and …

    Orexins, also known as hypocretins, are two neuropeptides secreted from orexin-containing neurons, mainly in the lateral hypothalamus (LH). Orexins orchestrate their effects by binding …

  3. OX2R-selective orexin agonism is sufficient to ameliorate …

    The aim of this study was to examine whether selective activation of OX2R is sufficient to rescue cataplexy and wake fragmentation in the mouse model of narcolepsy, providing a proof-of …

  4. Orexin Receptors: Pharmacology and Therapeutic Opportunities

    The orexin peptides bind selectively to the OX1 and OX2 receptors (OX1R and OX2R, also known as HCRTR1 and HCRTR2) . These are G protein–coupled receptors that have 7 …

  5. Structures of active-state orexin receptor 2 rationalize peptide and ...

    Feb 5, 2021 · Cryo-EM structures of active-state OX2R bound to an endogenous peptide agonist and a small-molecule agonist suggest a molecular mechanism that rationalizes both receptor …

  6. Orexin 2 receptor (OX2R) protein distribution measured by ...

    May 19, 2022 · Orexin, a neuropeptide, performs various physiological functions, including the regulation of emotion, feeding, metabolism, respiration, and sleep/wakefulness, by activating …

  7. Phase 1 Clinical Data with Orexin Receptor 2 (OX2R) Agonist, …

    Apr 7, 2025 · ORX750 is a novel, investigational oral orexin-2 receptor (OX2R) agonist in development for treatment of narcolepsy and idiopathic hypersomnia. Strong wake-promoting …

  8. TAK-861, a potent, orally available orexin receptor 2 ... - Nature

    Sep 6, 2024 · We discovered a parenteral orexin receptor 2 (OX2R) agonist, danavorexton, and an orally available OX2R agonist, TAK-994; both improving NT1 phenotypes in mouse models …

  9. TAK-994, a Novel Orally Available Brain-Penetrant Orexin 2 …

    Sep 15, 2022 · TAK-994 activated recombinant human OX2R (EC 50 value of 19 nM) with > 700-fold selectivity against OX1R and activated OX2R-downstream signaling similar to those by …

  10. Orexin receptor - Wikipedia

    There are two variants, OX 1 and OX 2, each encoded by a different gene (HCRTR1, HCRTR2). [1] Both orexin receptors exhibit a similar pharmacology – the 2 orexin peptides, orexin-A and …

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