913358-93-7
913358-93-7 structure
- Name: Almorexant HCI
- Chemical Name: 2(1H)-Isoquinolineacetamide, 3,4-dihydro-6,7-dimethoxy-N-methyl-α-phenyl-1-[2-[4-(trifluoromethyl)phenyl]ethyl]-, hydrochloride (1:1), (αR,1S)
- CAS Number: 913358-93-7
- Molecular Formula: C29H32ClF3N2O3
- Molecular Weight: 549.024
- Catalog: Biochemical Inhibitor G protein coupled receptor(GPCR & G Protein) OX Receptor Antagonist
- Create Date: 2018-05-12 08:00:00
- Modify Date: 2024-01-20 21:05:25
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Almorexant Hcl (ACT078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively.
| Name | 2(1H)-Isoquinolineacetamide, 3,4-dihydro-6,7-dimethoxy-N-methyl-α-phenyl-1-[2-[4-(trifluoromethyl)phenyl]ethyl]-, hydrochloride (1:1), (αR,1S) |
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| Synonyms |
(2R)-2-[(1S)-6,7-Dimethoxy-1-{2-[4-(trifluoromethyl)phenyl]ethyl}-3,4-dihydro-2(1H)-isoquinolinyl]-N-methyl-2-phenylacetamide hydrochloride (1:1)
(2R)-2-[(1R)-6,7-Dimethoxy-1-{2-[4-(trifluoromethyl)phenyl]ethyl}-3,4-dihydro-2(1H)-isoquinolinyl]-N-methyl-2-phenylacetamide hydrochloride (1:1) Almorexant HCI 2(1H)-Isoquinolineacetamide, 3,4-dihydro-6,7-dimethoxy-N-methyl-α-phenyl-1-[2-[4-(trifluoromethyl)phenyl]ethyl]-, (αR,1R)-, hydrochloride (1:1) 2(1H)-Isoquinolineacetamide, 3,4-dihydro-6,7-dimethoxy-N-methyl-α-phenyl-1-[2-[4-(trifluoromethyl)phenyl]ethyl]-, (αR,1S)-, hydrochloride (1:1) Act-078573 Almorexant HCl Almorexant (hydrochloride) |
| Description | Almorexant Hcl (ACT078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively. |
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| Related Catalog | |
| Target |
IC50 value: 1.3/0.7 nM(OX1/OX2 receptor) [1] [2] |
| In Vitro | [(3)H]Almorexant bound to a single saturable site on hOX(1) and hOX(2) with high affinity (K(d) of 1.3 and 0.17 nM, respectively. In Schild analyses using the [(3)H]inositol phosphates assay, almorexant acted as a competitive antagonist at hOX(1) and as a noncompetitive-like antagonist at hOX(2). In binding kinetic analyses, [(3)H]almorexant had fast association and dissociation rates at hOX(1), whereas it had a fast association rate and a remarkably slow dissociation rate at hOX(2) [1]. in vivo: During the 12-h dark period after dosing, ALM(Almorexant) exacerbated cataplexy in TG mice and increased nonrapid eye movement sleep with heightened sleep/wake fragmentation in both genotypes. ALM showed greater hypnotic potency in WT mice than in TG mice. The 100 mg/kg dose conferred maximal promotion of cataplexy in TG mice and maximal promotion of REM sleep in WT mice. In TG mice, ALM (30 mg/ kg) paradoxically induced a transient increase in active wakefulness [3]. Almorexant 200 mg showed significantly less 'Drug Liking' than both zolpidem doses (p < 0.01), and almorexant 400 mg had smaller effects than zolpidem 20 mg (p < 0.05), while almorexant 1,000 mg was not different from either zolpidem dose [4]. |
| References |
| Molecular Formula | C29H32ClF3N2O3 |
|---|---|
| Molecular Weight | 549.024 |
| Exact Mass | 548.205383 |
| PSA | 50.80000 |
| LogP | 6.87270 |
| Storage condition | -20℃ |