| Target Validation Information | |||||
|---|---|---|---|---|---|
| TTD ID | T73482 | ||||
| Target Name | Orexin receptor type 1 (HCRTR1) | ||||
| Type of Target |
Clinical trial |
||||
| Drug Potency against Target | Almorexant | Drug Info | IC50 = 3.4~6.5 nM | ||
| Suvorexant | Drug Info | IC50 = 50 nM | |||
| Action against Disease Model | Almorexant | Drug Info | In rats, dogs and h uMans, somnolence is induced by pharmacological blockade of both orexin OX(1) and OX(2) receptors. When administered orally during the active period of the circadian cycle, a dual antagonist increased, in rats, electrophysiological indices of both non-REM and, particularly, REM sleep, in contrast to GABA(A) receptor modulators; in dogs, it caused somnolence and increased surrogate markers of REM sleep; and in h uMans, it caused subjective and objective electrophysiological signs of sleep. | [1] | |
| References | |||||
| REF 1 | Promotion of sleep by targeting the orexin system in rats, dogs and humans. Nat Med. 2007 Feb;13(2):150-5. | ||||
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