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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.

  • SB-334867 EY1621

    SB-334867游离碱是非肽类食欲肽OX1受体拮抗剂，pKb为7.2。

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