Orexin Receptor (OX Receptor)
Hypocretin Receptor; HCRT Receptor
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
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Orexin Receptor (OX Receptor) Inhibitors
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Orexin Receptor (OX Receptor) Agonists
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Orexin Receptor (OX Receptor) Antagonists
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Orexin Receptor (OX Receptor) Related Products (130)
Related Products (130)
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Antibodies (2)
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Orexin Receptor (OX Receptor) Isoform Comparison
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Seltorexant (Standard)
0 ImagesCat. No.: HY-109012RCAS No.: 1293281-49-8Synonyms: JNJ-42847922 (Standard)Seltorexant (Standard) is the analytical standard of Seltorexant (HY-109012). This product is intended for research and analytical applications. Seltorexant (JNJ-42847922) is an orally active, high-affinity, and selective orexin-2 receptor (OX2R) antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant (JNJ-42847922) crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain.
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JNJ-10397049 (Standard)
0 ImagesCat. No.: HY-10896RCAS No.: 708275-58-5JNJ-10397049 (Standard) is the analytical standard of JNJ-10397049 (HY-10896). This product is intended for research and analytical applications. JNJ-10397049 is a potent and selective orexin 2 receptor (OX2R) antagonist, with a pKi of 8.3. JNJ-10397049 is 600-fold selective for the OX2R over the OX1R.
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Almorexant hydrochloride (Standard)
0 ImagesCat. No.: HY-10805ARCAS No.: 913358-93-7Synonyms: ACT 078573 hydrochloride (Standard)Almorexant hydrochloride (Standard) is the analytical standard of Almorexant (hydrochloride) (HY-10805A). This product is intended for research and analytical applications. Almorexant (ACT 078573) hydrochloride is an orally active, potent and competitive dual orexin receptor antagonist, with Kd values of 1.3 nM (OX1) and 0.17 nM (OX2), respectively. Almorexant hydrochloride reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant hydrochloride totally blocked the intracellular Ca2+ signal pathway. Almorexant hydrochloride stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis.
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MK-8133
0 ImagesCat. No.: HY-123737CAS No.: 1431472-56-8MK-8133 is an orexin-2 receptor antagonist. MK-8133 can be used in the study of insomnia.
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SB-408124 Hydrochloride (Standard)
0 ImagesSB-408124 (Hydrochloride) (Standard) is the analytical standard of SB-408124 (Hydrochloride). This product is intended for research and analytical applications. SB-408124 Hydrochloride is a selective non-peptide orexin receptor 1 (OX1) receptor antagonist with Kis of 57 nM and 27 nM in whole cell and membrane, respectively. SB-408124 Hydrochloride exhibits 50-fold selectivity over OX2 receptor.
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Almorexant (Standard)
0 ImagesCat. No.: HY-10805RCAS No.: 871224-64-5Synonyms: ACT 078573 (Standard)Almorexant (Standard) is the analytical standard of Almorexant. This product is intended for research and analytical applications. Almorexant (ACT 078573) is an orally active, potent and competitive dual orexin receptor antagonist, with Kd values of 1.3 nM (OX1) and 0.17 nM (OX2), respectively. Almorexant reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant totally blocked the intracellular Ca2+ signal pathway. Almorexant stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis .
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SB-408124 (Standard)
0 ImagesSB-408124 (Standard) is the analytical standard of SB-408124. This product is intended for research and analytical applications. SB-408124 is a non-peptide OX1 receptor antagonist with Kis of 57 nM and 27 nM in whole cell and membrane, respectively. SB-408124 exhibits 50-fold selectivity over OX2 receptor.
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Orexin 1 receptor modulator-1
0 ImagesCat. No.: HY-184879CAS No.: 1628320-31-9Orexin 1 receptor modulator-1 is a highly potent and selective modulator of the orexin 1 receptor (OX1R), with a Ki value of 4 nM for both rat OX1R and human OX1R, and a Ki value of 767 nM for human OX2R. Orexin 1 receptor modulator-1 can be used in studies related to the orexin signaling pathway and the nervous system.
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GSK1059865 (Standard)
0 ImagesCat. No.: HY-101534RCAS No.: 1191044-58-2GSK1059865 (Standard) is the analytical standard of GSK1059865 (HY-101534). This product is intended for research and analytical applications. GSK1059865 is a potent orexin 1 receptor antagonist.
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SB-334867 free base (Standard)
0 ImagesCat. No.: HY-10895ARCAS No.: 792173-99-0Synonyms: SB334867A free base (Standard)SB-334867 free base (Standard) is the analytical standard of SB-334867 (free base) (HY-10895A). This product is intended for research and analytical applications. SB-334867 free base (SB334867A free base) is an excellent, selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo.
