SKF-83566

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SKF-83566 是一种血脑渗透性、口服活性的 D1 样多巴胺受体拮抗剂，也是一种竞争性较弱的 5-HT2 受体拮抗剂，Ki 为 11 nMSKF-83566 引起单脉冲诱发细胞外 DA 峰值浓度呈浓度依赖性增加，在 5 μM SKF-83566 中最大增加 65%。

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).

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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 daysResult:Blocked nicotine and cocaine-induced facilitation of LTP.

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GPCR/G Protein

Dopamine Receptor

D1|D5|5-HT2

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99295-33-7

332.23

C17H18BrNO

>98% (HPLC)

In Vitro:?DMSO : 33.33 mg/mL (100.32 mM)

CN1CCc2cc(Br)c(O)cc2C(C1)c1ccccc1

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(-20℃)

With Ice Pack

≥ 2 years