SKF 83959
Based on 1 publication(s) in Google Scholar
SKF83959 is a potent and selective dopamine D1-like receptor partial agonist. SKF83959 Ki values for rat D1, D5, D2 and D3 receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 is a potent allosteric modulator of sigma (σ)-1 receptor. SKF83959 belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 can be used for the research of Alzheimer's disease and depression.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.30%
- No. CAS: 80751-85-5
- Fòrmula: C18H20ClNO2
- Peso molecular:317.81
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) SKF 83959
MoreVer todos los productos específicos de isoformas Dopamine Receptor
MoreVer todos los productos específicos de isoformas Sigma Receptor
More
Actividad biológica
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D1 Receptor 1.18 nM (Ki) |
Sigma 1 Receptor |
D5 Receptor 7.56 nM (Ki) |
D2 Receptor 920 nM (Ki) |
D3 Receptor 399 nM (Ki) |
SKF83959 (10~250 μM) stimulates PIP2 hydrolysis in membranes. SKF83959 (0.1~10 μM; PC12 cell) changes the EC50 value of SKF81297 from 0.5 nM in control tissue to 31.6 nM, 251.2 nM and 631.0 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
SKF83959 (1 mg/kg; i.p.; 30 minutes) induced memory enhancing effects are prevented by brain-derived neurotrophic factor system blockade[1].
SKF83959 has anti-amnesic activities and restores the scopolamine-decreased BDNF signaling pathway in the hippocampus in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male ICR male mice (8 weeks)[1]
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Dosage:0.5 and 1 mg/kg
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Administration:I.p.; 1 hour
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Result:Reversed the scopolamine-induced cognitive impairments in the passive avoidance task and Y-Maze test.
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Animal Model:Male ICR male mice (8 weeks)[1]
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Dosage:1 mg/kg
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Administration:I.p.; 30 minutes
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Result:The memory enhancing effects were prevented by BDNF system blockade.
Chemical Information
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No. CAS 80751-85-5
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Appearance Solid
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Peso molecular 317.81
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Fòrmula C18H20ClNO2
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Color White to light yellow
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SMILES
OC1=C(O)C=C2C(C3=CC=CC(C)=C3)CN(C)CCC2=C1Cl
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Nature
2023 Dec;624(7992):672-681. PMID: 37935376
Solvente y solubilidad
DMSO : ≥ 100 mg/mL (314.65 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (282 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Sheng G, et al. SKF83959 Has Protective Effects in the Scopolamine Model of Dementia. Biol Pharm Bull. 2018;41(3):427-434. [Content Brief]
[2]. Jin LQ, et al. SKF83959 selectively regulates phosphatidylinositol-linked D1 dopamine receptors in rat brain. J Neurochem. 2003;85(2):378-386. [Content Brief]
[3]. Neumeyer JL, et al. Receptor affinities of dopamine D1 receptor-selective novel phenylbenzazepines. Eur J Pharmacol. 2003;474(2-3):137-140. [Content Brief]
[4]. Guo L, et al. SKF83959 is a potent allosteric modulator of sigma-1 receptor. Mol Pharmacol. 2013;83(3):577-586. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1465 mL | 15.7327 mL | 31.4653 mL | 78.6634 mL |
| 5 mM | 0.6293 mL | 3.1465 mL | 6.2931 mL | 15.7327 mL | |
| 10 mM | 0.3147 mL | 1.5733 mL | 3.1465 mL | 7.8663 mL | |
| 15 mM | 0.2098 mL | 1.0488 mL | 2.0977 mL | 5.2442 mL | |
| 20 mM | 0.1573 mL | 0.7866 mL | 1.5733 mL | 3.9332 mL | |
| 25 mM | 0.1259 mL | 0.6293 mL | 1.2586 mL | 3.1465 mL | |
| 30 mM | 0.1049 mL | 0.5244 mL | 1.0488 mL | 2.6221 mL | |
| 40 mM | 0.0787 mL | 0.3933 mL | 0.7866 mL | 1.9666 mL | |
| 50 mM | 0.0629 mL | 0.3147 mL | 0.6293 mL | 1.5733 mL | |
| 60 mM | 0.0524 mL | 0.2622 mL | 0.5244 mL | 1.3111 mL | |
| 80 mM | 0.0393 mL | 0.1967 mL | 0.3933 mL | 0.9833 mL | |
| 100 mM | 0.0315 mL | 0.1573 mL | 0.3147 mL | 0.7866 mL |
SKF 83959 Related Classifications
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