Almorexant (ACT-078573) is a competitive OX1 and OX2 orexin receptor antagonist with IC50 of 13 and 8 nM, respectively. It is rapidly absorbed and distributed and shows no tendency to accumulate with repeated dosing. Preclinical studies in rats and dogs have demonstrated a sleep-promoting effect which resembles physiological sleep; this could be quickly reversed upon sensorimotor stimulation and yet allow resumption of sleep upon its cessation. Almorexant’s (ACT-078573) sleep-promoting effects were confirmed in volunteers and patients with primary insomnia. It dose-dependently increased sleep efficiency and decreased sleep latency and wake time after sleep onset.
iscience. 2023 Aug 22.
Prelimbic area to lateral hypothalamus circuit drives social aggression
Almorexant purchased from AbMole
| Cell Experiment | |
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| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
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| Animal models | Wistar rats. |
| Formulation | Polyethylene glycol (PEG) 400 or 0.25% methylcellulose in water |
| Dosages | ~300 mg/kg |
| Administration | p.o. |
| Molecular Weight | 512.56 |
| Formula | C29H31F3N2O3 |
| CAS Number | 871224-64-5 |
| Form | Solid |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] Jae-Eun Kang, et al. Amyloid-beta dynamics are regulated by orexin and the sleep-wake cycle
[3] David N Neubauer. Almorexant, a dual orexin receptor antagonist for the treatment of insomnia
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| Orexin B, rat, mouse
Orexin B, rat, mouse (Rat orexin B) is an endogenous agonist at Orexin receptor with Kis of 420 and 36 nM for OX1 and OX2, respectively. |
| Hypocretin (70-98), human
Hypocretin (70-98), human is a polypeptide that is capable of binding to an orexin receptor OX1R and promotes apoptosis. |
| Xenopus orexin A
Xenopus orexin A is a neuropeptides that identified as an endogenous ligands for an orphan G-protein-coupled receptor. |
| Xenopus orexin B
Xenopus orexin B is a neuropeptides that identified as an endogenous ligands for an orphan G-protein-coupled receptor. |
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