2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. Orexin Receptor (OX Receptor)

Orexin Receptor (OX Receptor)

Hypocretin Receptor; HCRT Receptor

Orexin Receptor (OX Receptor)

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The orexin receptors (hypocretin receptors) are a family of G protein-coupled receptors and consist of orexin receptor 1 (OX1R) and orexin receptor 2 (OX2R) subtypes. Orexin receptors are expressed throughout the central nervous system and are involved in the regulation of the sleep/wake cycle.

Orexin A binding to OX1R and OX2R with similar affinity, and orexin B binding to OX2 with higher affinity than OX1R. OX1R is mainly expressed in the prefrontal and infralimbic cortex, hippocampus, paraventricular thalamic nucleus, and locus coeruleus. OX2R is mainly distributed in the cerebral cortex, septal nuclei, lateral hypothalamus, hippocampus, and hypothalamic nuclei.

Both OX1R and OX2R are coupled via Gq/11 to the activation of phospholipase C, leading to an elevation of intracellular Ca2+ levels. Moreover, OX2R also couples via Gs and Gi/o to the cAMP pathways.

Orexin Receptor (OX Receptor) Isoform Specific Products:

Orexin Receptor (OX Receptor) Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-146517
    Orexin receptor antagonist 4
    		Antagonist
    Orexin receptor antagonist 4 is potent and selective orexin 2 receptor (OX2R) antagonist with an IC50 of 4.27 nM. Orexin receptor antagonist 4 is 61-fold selective for the OX2R over the OX1R (IC50 of 295 nM) (WO2018206959A1; example 1).
    Orexin receptor antagonist 4
  • HY-P10080
    Xenopus orexin B
    		Agonist
    Xenopus orexin B is a neuropeptides that identified as an endogenous ligands for an orphan G-protein-coupled receptor. Xenopus orexin B is a potent agonist of OX2R.
    Xenopus orexin B
  • HY-10805S
    Almorexant-13C,d3
    		Antagonist
    Almorexant-13C,d3 is the 13C- and deuterium labeled Almorexant. Almorexant (ACT 078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM, respectively.
    Almorexant-<sup>13</sup>C,d<sub>3</sub>
  • HY-P1339
    Orexin B, human
    		Agonist
    Orexin B, human is an endogenous agonist at Orexin receptor with Kis of 420 and 36 nM for OX1 and OX2, respectively.
    Orexin B, human
  • HY-149014
    OX2R-IN-1
    		Inhibitor
    OX2R-IN-1 (compound 15) is a low cytotoxicity profile OX2R-IN-1 antagonist (a potential OX2R binder) with an IC50 value of 484 μM. OX2R-IN-1 (compound 15) can cross the BBB into the brain with a short half-life.
    OX2R-IN-1
  • HY-163276
    OX2R-IN-2
    		Agonist
    OX2R-IN-2 (compound 63c) is an agonist for orexin receptor type 2 (OX2R) with EC50 of 339 nM. OX2R-IN-2 is able to cross the blood-brain barrier and exhibits no cytotoxicity in cells
    OX2R-IN-2
  • HY-101260
    DORA-22
    		Antagonist
    DORA-22 is an orally active dual orexinergic receptor antagonist, and improves the sleep disruption and memory impairment. DORA-22 can be used for study of insomnia.
    DORA-22
  • HY-134188
    JNJ-54717793
    		Antagonist 98.85%
    JNJ-54717793, as a brain penetrant, is an orally active, selective and high affinity orexin-1 receptor (OX1R) antagonist (plasma EC50=85 ng/mL). The Ki values of JNJ-54717793 for hOX1R (human OX1R) and hOX2R are 16 nM and 700 nM, respectively. JNJ-54717793 is a potent compound of anxiety disorders.
    JNJ-54717793
  • HY-159731
    OX2R agonist 1
    		Agonist
    OX2R agonist 1 is an OX2R antagonist with an EC50 of less than 100 nM. OX2R agonist 1 can be used in research related to excessive daytime sleepiness or narcolepsy.
    OX2R agonist 1
  • HY-113555
    DORA 42
    		Antagonist
    DORA 42 is a dual orexin 1 and orexin 2 receptor antagonist with sleep efficacy in rats. DORA 42 is promising for research of insomnia.
    DORA 42
  • HY-123737
    MK-8133
    		Antagonist
    MK-8133 is an orexin-2 receptor antagonist. MK-8133 can be used in the study of insomnia.
    MK-8133
Cat. No. Product Name / Synonyms Application Reactivity
Orexin Receptor (OX Receptor) Isoform Comparison

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