SKF-83566

SKU: orb1219652

Description

SKF-83566 is a blood-brain permeable and orally active antagonist of D1-like dopamine receptor and a weaker competitive 5-HT2 receptor antagonist with Ki of 11 nMSKF-83566 caused a concentration-dependent increase in peak single-pulse evoked extracellular DA concentration, with a maximum increase of 65% in 5 μM SKF-83566. This was accompanied by a concentration-dependent increase in extracellular DA concentration clearance time. Both effects were occluded by nomifensine (1 μM), a dopamine transporter (DAT) inhibitor, suggesting that SKF-83566 acted via the DAT. Tested this by examining [(3)H]DA uptake into LLc-PK cells expressing rat DAT, and confirmed that SKF-83566 is a competitive DAT inhibitor with an IC(50) of 5.7 μM. Binding studies with [(3)H]CFT, a cocaine analog, showed even more potent action of SKF-83566 at the DAT cocaine binding site (IC(50) = 0.51 μM). The facilitation induced by nicotine and cocaine can be blocked by oral administration of the dopamine D1/D5 receptor antagonist (SKF 83566).

Key Properties

• CAS Number: 99295-33-7
• MW: 332.23
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₈BrNO
• SMILES: CN1CCc2cc(Br)c(O)cc2C(C1)c1ccccc1
• Target: Dopamine Receptor
• Solubility: In Vitro: DMSO : 33.33 mg/mL (100.32 mM)

Bioactivity

• In Vivo:
  Animal model: Male C57BL6/J mice (6-to 9-wk-old). Dosage: 20 μg/mL (Together with nicotine for 7 d, followed by the injection of cocaine). Administration: Oral administration; 7 days. Result: Blocked nicotine and cocaine-induced facilitation of LTP.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Dopamine Receptor