Orexin Receptor(OX Receptor)
The orexin receptor is a G-protein-coupled receptor that binds the neuropeptide orexin. There are two variants, OX1 and OX2, each encoded by a different gene (HCRTR1, HCRTR2). Both orexin receptors exhibit a similar pharmacology - the 2 orexin peptides, orexin-A and orexin-B, bind to both receptors and, in each case, agonist binding results in an increase in intracellular calcium levels. However, orexin-B shows a 10-fold selectivity for orexin receptor type 2, whilst orexin-A is equipotent at both receptors. Several orexin receptor antagonists are in development for potential use in sleep disorders. Only the crystal structure of OX2 is known.
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Alverine citrate is a drug used for functional gastrointestinal disorders.
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Suvorexant是OX受体拮抗剂,对OX1和OX2受体的Ki分别为0.55 nM和0.35 nM。
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TCS OX2 29是活性的,选择性 OX2 拮抗剂。
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SB 674042是活性选择性非肽类 OX1 拮抗剂。
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SB 408124是选择性非肽类 OX1 拮抗剂。
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