SKF-83566
目录号: PL01410 纯度: ≥99%
CAS No. :99295-33-7
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中文名称
SKF-83566
中文别名
8-溴-2,3,4,5-四氢-3-甲基-5-苯基-1H-3-苯并氮杂-7-醇
英文名称
SKF-83566
英文别名
1H-3-Benzazepin-7-ol,8-bromo-2,3,4,5-tetrahydro-3-methyl-5-phenyl-;8-Bromo-2,3,4,5-tetrahydro-3-methyl-5-phenyl-1H-3-benzazepin-7-olhydrobromide;SKF 83566
Cas No.
99295-33-7
分子式
C17H18NOBr
分子量
332.23
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
SKF-83566 是一种有效的,可通透血脑屏障的,具有口服活性的 D1 样多巴胺受体 ( D1-like dopamine receptor) 拮抗剂,也可以作为一种较弱的竞争性拮抗剂,作用于血管 5-HT2 受体 (Ki =11 nM)。SKF-83566 是一种竞争性多巴胺转运蛋白 (DAT) 抑制剂,IC50 为 5.7 μM。在离体兔胸主动脉中,SKF-83566 对腺苷基环化酶 2 (AC2) 的选择性高于对 AC1 和 AC5 的。SKF-83566 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。
生物活性
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.
性状
Solid
IC50 & Target[1][2]
D1 Receptor D5 Receptor
体外研究(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 EC50 value of this effect of SKF-83566 is 1.3 μM.
SKF-83566 inhibited [H]DA uptake with an IC50 of 5.73 μM. Moreover, SKF-83566 more potently inhibits the binding of [H]CFT, a cocaine analog, with an IC50 of 0.51 μM in [H]DA uptake and [H]CFT binding studies.
Similarly, in LLc-PK-rDAT cell, SKF-83566 also inhibits [H]CFT binding with an IC50 of 0.77 μM in LLc-PK-rDAT cell membrane preparations.
has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
SKF 83566 hydrobromide (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%).
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Yan-You Huang, et al.D1/D5 Receptors and Histone Deacetylation Mediate the Gateway Effect of LTP in Hippocampal Dentate Gyrus.
[2]. Melissa A Stouffer, et al. SKF-83566, a D1-dopamine Receptor Antagonist, Inhibits the Dopamine Transporter. J Neurochem. 2011 Sep;118(5):714-20.
[3]. E H Ohlstein, et al. SCH 23390
溶解度数据
In Vitro: DMSO : 33.33 mg/mL (100.32 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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