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SKF-83566

CAT: 0013-GTR19156883-01Size: 100 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19156883-01Size:100 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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) .
CAS Number
99295-33-7
Purity
>98% (HPLC)
Solubility
In Vitro: DMSO : 33.33 mg/mL (100.32 mM)
Smiles
CN1CCc2cc (Br) c (O) cc2C (C1) c1ccccc1
Molecular Formula
C17H18BrNO
Molecular Weight
332.23
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.

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