SKF-83566 is a potent, blood-brain permeable and orally active D1-like dopamine receptor (D1DR) antagonist and a weaker competitive antagonist at the vascular 5-HT 2 receptor ( K i =11 nM) SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC 50 of 5.7 μM SKF-83566 also shows selective inhibition for adenylyl cyclase 2 (AC2) over AC 1 and AC 5 in the isolated rabbit thoracic aorta. SKF-83566 can be used for research of parkinson’s disease and nicotine craving alleviation. In Vitro SKF-83566 (0.1 μM-10 μM) causes a concentration-dependent increase in peak evoked extracellular DA concentration ([DA] o )?evoked by single-pulse stimulation, with a maximum 65% increase in peak evoked [DA] o with 5 μM. The EC 50 value of this effect of SKF-83566 is 1.3 μM. SKF-83566 inhibited [ 3 H]DA uptake with an IC 50 ?of 5.73 μM. Moreover, SKF-83566 more potently inhibits the binding of [ 3 H]CFT, with an IC 50 ?of 0.51 μM in [ 3 H]DA uptake and [ 3 H]CFT binding studies. Similarly, in LLc-PK-rDAT cell, SKF-83566 also inhibits [ 3 H]CFT binding with an IC 50 ?of 0.77 μM in LLc-PK-rDAT cell membrane preparations. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo SKF 83566 (oral administration; 20 μg/mL; 7 days) alone has no effects on altering LTP (115%). However, combinnation of SKF 83566 and nicotine significantly blocks the enhancement of long-term synaptic potentiation (LTP) induced by pretreatment with nicotine (SKF 83566+nicotine+cocaine, 120%; nicotine+cocaine, 143%) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. IC50& Target:D 1 Receptor D 5 Receptor 5-HT 2 Receptor 11 nM (Ki)
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SKF-83566
CAS number：99295-33-7(DMSO) molecular formula：C17H18BrNO
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 99295-33-7(DMSO) | molecular formula | C17H18BrNO |
| molecular weight | 332.23 g/mol | Exact mass | 10mM in DMSO |
| PSA | - | logp | - |
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