The orexin receptor (also referred to as the hypocretin receptor) is a G-protein-coupled receptor that binds the neuropeptide hormone 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.
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Famous quotes containing the word receptor:
“The disinterest [of my two great-aunts] in anything that had to do with high society was such that their sense of hearing ... put to rest its receptor organs and allowed them to suffer the true beginnings of atrophy.”
—Marcel Proust (18711922)