SKF 83959 HYDROBROMIDE
SKF 83959 HYDROBROMIDE structure
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Common Name | SKF 83959 HYDROBROMIDE | ||
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| CAS Number | 80751-85-5 | Molecular Weight | 398.72200 | |
| Density | 1.249g/cm3 | Boiling Point | 464.6ºC at 760 mmHg | |
| Molecular Formula | C18H21BrClNO2 | Melting Point | N/A | |
| MSDS | USA | Flash Point | 234.8ºC | |
Use of SKF 83959 HYDROBROMIDESKF83959 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[1][2][3][4]. |
| Name | N-methyl-6-chloro-1-(3-methylphenyl)-2,3,4,5-tetrahydro-3-benzazepine-7,8-diol |
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| Synonym | More Synonyms |
| Description | 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[1][2][3][4]. |
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| Related Catalog | |
| Target |
D1 Receptor:1.18 nM (Ki) D5 Receptor:7.56 nM (Ki) D2 Receptor:920 nM (Ki) D3 Receptor:399 nM (Ki) Sigma (σ)-1 |
| In Vitro | 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]. |
| In Vivo | SKF83959 (0.5 and 1 mg/kg; i.p.; 1 hour) reverses the scopolamine-induced cognitive impairments in the passive avoidance task and Y-Maze test[1]. 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]. Animal Model: Male ICR male mice (8 weeks)[1] Dosage: 0.5 and 1 mg/kg Administration: I.p.; 1 hour Result: Reversed the scopolamine-induced cognitive impairments in the passive avoidance task and Y-Maze test. Animal Model: Male ICR male mice (8 weeks)[1] Dosage: 1 mg/kg Administration: I.p.; 30 minutes Result: The memory enhancing effects were prevented by BDNF system blockade. |
| References |
| Density | 1.249g/cm3 |
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| Boiling Point | 464.6ºC at 760 mmHg |
| Molecular Formula | C18H21BrClNO2 |
| Molecular Weight | 398.72200 |
| Flash Point | 234.8ºC |
| Exact Mass | 397.04400 |
| PSA | 43.70000 |
| LogP | 4.57540 |
| Index of Refraction | 1.619 |
| Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
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| RIDADR | NONH for all modes of transport |
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SKF83959 is a potent allosteric modulator of sigma-1 receptor.
Mol. Pharmacol. 83(3) , 577-86, (2013) SKF83959 (3-methyl-6-chloro-7,8-hydroxy-1-[3-methylphenyl]-2,3,4,5-tetrahydro-1H-3-benzazepine), an atypical dopamine receptor-1 (D(1) receptor) agonist, has shown many D(1) receptor-independent effec... |
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The D₁ dopamine receptor agonist, SKF83959, attenuates hydrogen peroxide-induced injury in RGC-5 cells involving the extracellular signal-regulated kinase/p38 pathways.
Mol. Vis. 18 , 2882-95, (2012) Oxidative stress is widely implicated in the death of retinal ganglion cells associated with various optic neuropathies. Agonists of the dopamine D(1) receptor have recently been found to be potential... |
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Phosphatidylinositol-linked novel D(1) dopamine receptor facilitates long-term depression in rat hippocampal CA1 synapses.
Neuropharmacology 57(2) , 164-71, (2009) Recent work has demonstrated that a phosphatidylinositol (PI)-linked D(1) dopamine receptor selective agonist, SKF83959, mediates phosphatidylinositol hydrolysis via activation of phospholipase C(beta... |
| 6-Chloro-2,3,4,5-tetrahydro-3-methyl-1-(3-methylphenyl)-1H-3-benzazepine-7,8-diol |