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

Key Properties

• CAS Number: 80751-85-5
• MW: 317.81
• Purity: 99.96% (May vary between batches)
• Formula: C₁₈H₂₀ClNO₂
• SMILES: ClC1=C2C(C(CN(C)CC2)C3=CC(C)=CC=C3)=CC(O)=C1O
• Target: Sigma receptor,Dopamine Receptor
• Solubility: DMSO:90 mg/mL (283.19 mM)

Bioactivity

• 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

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Dopamine Receptor, DopamineReceptor, D1 receptor

Compound Identifiers

PubChem CID

133538