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SKF83959

SKU: orb1689198

Description

SKF83959 is a benzazepine analog acting as a selective dopamine D1/D5 receptor partial agonist and a sigma-1 receptor modulator. It is utilized in research models for investigating cognitive dysfunction associated with depression and Alzheimer's disease, in both in vitro and in vivo studies.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Images & Validation

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SKF83959

Key Properties

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CAS Number80751-85-5
MW317.81
Purity99.96% (May vary between batches)
FormulaC18H20ClNO2
SMILESClC1=C2C(C(CN(C)CC2)C3=CC(C)=CC=C3)=CC(O)=C1O
TargetSigma receptor,Dopamine Receptor
SolubilityDMSO:90 mg/mL (283.19 mM)

Bioactivity

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Target IC50
D3 receptor:399 nM (Ki)|D1 receptor:1.18 nM (Ki)|D2 receptor:920 nM (Ki)|D5 receptor:7.56 nM (Ki)
In Vivo
SKF83959 (0.5, 1 mg/kg; i.p.; 1 h; Male ICR male mice) alleviates scopolamine-induced cognitive impairments in the passive avoidance task and Y-Maze test. SKF83959 (1 mg/kg; i.p.; 30 minutes; Male ICR male mice) memory-enhancing effects are hindered by the blockade of the brain-derived neurotrophic factor system. SKF83959 exhibits anti-amnesic activities and reinstates the scopolamine-induced decrease in the BDNF signaling pathway in the hippocampus of mice.
In Vitro
SKF83959 (0.1-30 micromol/L) improved H2O2-reduced cell viability in a dose-dependent manner. Moreover, SKF83959 treatment significantly inhibited H2O2-activated glycogen synthase kinase-3beta (GSK-3beta) which was associated with the drug's neuroprotective effect. Moreover, the application of either SKF83959 or a pharmacological inhibitor of GSK-3beta attenuated the inhibition by H2O2 on the expression of inducible NO synthase and the production of NO. In addition, SKF83959 also effectively decreased the level of lipid peroxidation and increased the activity of GSH-peroxidase altered by H2O2. These results suggest that SKF83959 exerts its neuroprotective effect through both receptor-dependent and independent mechanisms: Inhibition of GSK-3beta and consequently increasing the expression of inducible NO synthase via putative PI-linked DAR; and its anti-oxidative activity which is independent of DAR.

Storage & Handling

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Storage-20°C
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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Dopamine Receptor, DopamineReceptor, D1 receptor
Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at support@biorbyt.com.

Compound Identifiers

PubChem CID
133538 ↗

Key Properties

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No computed properties available.

Protocol Information

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Available Sizes

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1 mg
$ 90.00
5 mg
$ 150.00
1 ml x 10 mM (in DMSO)
$ 160.00
10 mg
$ 220.00
25 mg
$ 420.00
50 mg
$ 600.00
100 mg
$ 840.00
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