1354039-86-3
1354039-86-3 structure
- Name: ACT 335827
- Chemical Name: (R)-2-[(S)-(1-3,4-dimethoxybenzyl)-6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl]-N-isopropyl-2-phenylacetamide
- CAS Number: 1354039-86-3
- Molecular Formula: C31H38N2O5
- Molecular Weight: 518.64400
- Catalog: Signaling Pathways GPCR/G Protein Orexin Receptor (OX Receptor)
- Create Date: 2018-01-17 23:08:12
- Modify Date: 2024-01-03 23:28:39
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ACT-335827 is a selective, orally active, brain-penetrant orexin type 1 receptor antagonist. ACT-33582 acts on OXR1 and OXR2 with IC50 values of 6 nM and 417 nM, respectively. ACT-33582 can be used in studies related to neurological disorders[1].
| Name | (R)-2-[(S)-(1-3,4-dimethoxybenzyl)-6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl]-N-isopropyl-2-phenylacetamide |
|---|---|
| Synonyms |
(R)-2-[(S)-1-(3,4-dimethoxy-benzyl)-6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl]-N-isopropyl-2-phenyl-acetamide
(R)-2-[(S)-1-(3,4-dimethoxy-benzyl)6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl]-N-isopropyl-2-phenyl-acetamide (-)-5'-DMH-CBD |
| Description | ACT-335827 is a selective, orally active, brain-penetrant orexin type 1 receptor antagonist. ACT-33582 acts on OXR1 and OXR2 with IC50 values of 6 nM and 417 nM, respectively. ACT-33582 can be used in studies related to neurological disorders[1]. |
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| Related Catalog | |
| Target |
OX1:6 nM (IC50) OX2:417 nM (IC50) |
| In Vitro | ACT-335827 (0-10 μM, 2 h) acts on OXR-1 and OXR-2 with the Kb values of 41 nM and 560 nM, the IC50 values of 120 nM and 2300 nM, respectively in CHO cells[1]. |
| In Vivo | ACT-335827 (oral gavage, 30-100 mg/kg, once) can reduce the fear-induced startle response with no affecting motor or cognitive function in rats[1]. ACT-335827 (oral administration, 300 mg/kg, everyday, 4 weeks) has less effect on metabolic syndrome (MetS), such as diet-induced obesity (DIO) in male Wistar rats[2]. Animal Model: Rats[1] Dosage: 30, 100 or 300 mg/kg Administration: Oral gavage; once Result: Reduced fear-induced startle response at 300 mg/kg. Decreased stress-induced elevated body temperature at 300 mg/kg and accelerated heat rate at 100 or 300 mg/kg but no effect on locomotion and blood pressure. Animal Model: Male Wistar rats weighing160-180g[2] Dosage: 300 mg/kg Administration: Oral administration; everyday; 4 weeks Result: Reduced preference for high fat/sweet diets but no effect on absolute energy intake. Increased water intake and HDL relative to total cholesterol. Resulted in a 4% weight gain compared to the control group. |
| References |
| Molecular Formula | C31H38N2O5 |
|---|---|
| Molecular Weight | 518.64400 |
| Exact Mass | 518.27800 |
| PSA | 69.26000 |
| LogP | 5.45760 |