Nomenclature | OX1 receptor | OX2 receptor |
HGNC, UniProt | HCRTR1, O43613 | HCRTR2, O43614 |
Rank order of potency | orexin‐A (HCRT, O43612) >orexin‐B (HCRT, O43612) | orexin‐A (HCRT, O43612) = orexin‐B (HCRT, O43612) |
Selective agonists | – | [Ala11, D‐Leu15]orexin‐B (pEC50 9.9) [62] |
(Sub)family‐selective antagonists | suvorexant (pK i 9.3) [377], SB‐649868 (pK i 9.1) [419], filorexant (pK i 8.6) [2035], almorexant (pIC50 7.9) [216] | filorexant (pK i 9.5) [2035], suvorexant (pK i 9.5) [377], SB‐649868 (pK i 8.9) [419], almorexant (pIC50 8.1) [216] |
Selective antagonists | SB‐408124 (pK i 7.2–7.6) [1042, 1190], SB‐334867 (pK i 7.4–7.5) [1190, 1518] | EMPA (pK i 9) [1189], JNJ 10397049 (pK i 7.9–8.6) [1238], TCS‐OX2‐29 (pK i 7.4) [760] |
Labelled ligands | [3H]SB‐674042 (Antagonist) (pK d 8.3–9.1) [1042, 1190, 1193] | – |