Orexin receptor 1 (OX1R) and orexin receptor 2 (OX2R) subtypes make up the family of G protein-coupled receptors known as orexin receptors (hypocretin receptors). Orexin receptors play a role in the control of the sleep/wake cycle and are expressed throughout the central nervous system.
Orexin B binds to OX2 with a higher affinity than OX1R, while orexin A binds to OX1R and OX2R with similar affinities. The prefrontal and infralimbic cortex, hippocampus, paraventricular thalamic nucleus, and locus coeruleus are the primary sites of OX1R expression. The cerebral cortex, septal nuclei, lateral hypothalamus, hippocampus, and hypothalamic nuclei are where OX2R is primarily found.
Gq/11 connects the OX1R and OX2R receptors to the activation of phospholipase C, which raises intracellular Ca2+ levels. Furthermore, OX2R connects to the cAMP pathways via Gs and Gi/o.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V69997 | Suntinorexton | 2274802-89-8 | Suntinorexton, a heterocyclic compound, is an orexin type 2 receptor agonist. |
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V1306 | Suvorexant (MK-4305) | 1030377-33-3 | This is a DEA controlled substance schedule IVSuvorexant (also known as MK-4305) is a potent dual OX receptor antagonist with Ki of 0.55 nM and 0.35 nM for OX1 receptor and OX2 receptor, respectively. |
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V3016 | TCS 1102 | 916141-36-1 | TCS 1102 is a potent, non-selective dual orexin receptor antagonist with Ki values of 0.2 and 3 nM for OX2 and OX1 receptors respectively. |
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V2861 | TCS-OX2-29 | 372523-75-6 | TCS-OX2-29 (TCS-OX229, TCS-OX-229), discovered from high throughput screening (HTS), is a potent, selective andnon-peptide OX2 (orexin) receptor antagonist with potential usefulness in the treatment of insomnia. |
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V3411 | TCS-OX2-29 HCl | 1610882-30-8 | TCS-OX2-29 HCl, the hydrochloride salt of TCS-OX229, is a non-peptide and selective OX2 receptor antagonist (IC50 = 40 nM) with potential use in the treatment of insomnia. |
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V69985 | Vornorexant (ORN-0829; TS-142) | 1517965-94-4 | Vornorexant (ORN-0829; TS-142) is a potent dual OX1R and OX2R antagonist (inhibitor) with IC50s of 1.05 nM and 1.27 nM, respectively. |
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V69993 | Xenopus orexin A | 254757-77-2 | Xenopus orexin A is a neuropeptide identified as an endogenous ligand for orphan G protein-coupled receptors. |
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V69994 | Xenopus orexin B | 254757-78-3 | Xenopus orexin B is a neuropeptide identified as an endogenous ligand for orphan G protein-coupled receptors. |
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V69990 | YNT-185 | 1804978-81-1 | YNT-185 is a non-peptide, selective orexin type 2 receptor (OX2R) agonist/activator with EC50s of 0.028 and 2.75 μM for OX2R and OX1R, respectively. |
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V69980 | YNT-185 dihydrochloride | 1804978-82-2 | YNT-185 di-HCl is a non-peptide, selective orexin type 2 receptor (OX2R) agonist/activator with EC50 of 0.028 and 2.75 μM for OX2R and OX1R respectively. |
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