| Name | SKF-83566 |
| 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 nM |
| In vitro | SKF-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)[1]. |
| In vivo | The facilitation induced by nicotine and cocaine can be blocked by oral administration of the dopamine D1/D5 receptor antagonist (SKF 83566) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 10 mM, Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (6.02 mM), Sonication is recommended.
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| Keywords | SKF-83566 | SKF83566 | SKF 83566 | Serotonin Receptor | parkinson's disease | nicotine craving | Inhibitor | inhibit | hippocampus | drug-related | dorsal striatum | DopamineReceptor | dopamine uptake | Dopamine Receptor | Dopamine | dentate gyrus | D5 | D1 | associative memory | Adenylyl cyclase | Adenylate Cyclase | 5-hydroxytryptamine Receptor | 5HTReceptor | 5-HT2 | 5-HT Receptor | 5HT Receptor |
| Inhibitors Related | Alverine citrate | Dapoxetine hydrochloride | Cefaclor monohydrate | Hexamethonium Bromide | Octopamine hydrochloride | 1,8-Cineole | L-DOPA | Creatine | Oxolinic acid | Mianserin hydrochloride | Trazodone hydrochloride | Cinchonidine |
| Related Compound Libraries | Bioactive Compound Library | Neuronal Signaling Compound Library | Neurotransmitter Receptor Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Compound Library | Serotonin Receptor-Targeted Compound Library | Anti-Hypertension Compound Library |
United States
