store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SKF-83566 是一种具有血脑渗透性和口服活性的 D1 样多巴胺受体拮抗剂和一种较弱的竞争性 5-HT2 受体拮抗剂,Ki 为 11 nM。它是竞争性多巴胺转运蛋白抑制剂,可用于研究帕金森氏症和对尼古丁渴望的缓解的相关研究。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 468 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 982 | 现货 |
产品描述 | 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 |
靶点活性 | 5-HT2 receptor:11 nM (Ki) |
体外活性 | 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]. |
体内活性 | The facilitation induced by nicotine and cocaine can be blocked by oral administration of the dopamine D1/D5 receptor antagonist (SKF 83566) |
分子量 | 332.23 |
分子式 | C17H18BrNO |
CAS No. | 99295-33-7 |
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 10 mM
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.01 mL | 15.0498 mL | 30.0996 mL | 75.2491 mL |
5 mM | 0.602 mL | 3.01 mL | 6.0199 mL | 15.0498 mL | |
10 mM | 0.301 mL | 1.505 mL | 3.01 mL | 7.5249 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
SKF-83566 99295-33-7 GPCR/G Protein Neuroscience Dopamine Receptor 5-HT Receptor AChR nicotine craving dorsal striatum Inhibitor SKF 83566 Adenylate Cyclase dentate gyrus SKF83566 dopamine uptake 5-hydroxytryptamine Receptor inhibit associative memory Serotonin Receptor Adenylyl cyclase hippocampus parkinson’s disease drug-related inhibitor