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SKF-83566 hydrobromide

MCE 国际站：SKF-83566 hydrobromide

品牌：MedChemExpress (MCE)

货号：HY-103430

CAS 号：108179-91-5

生物活性：SKF-83566氢溴酸盐是一种强效、可透过血脑屏障且口服有效的D1样多巴胺受体（D1DR）拮抗剂，同时也是血管5-HT2受体的较弱竞争性拮抗剂（Ki=11 nM）[1][3]。SKF-83566是一种竞争性多巴胺转运体（DAT）抑制剂，IC50为5.7 µM[2]。在离体兔胸主动脉中，SKF-83566对腺苷酸环化酶2（AC2）的抑制作用优于AC1和AC5[4]。SKF-83566可用于帕金森病的研究和尼古丁渴求缓解的研究[5]。

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[2].SKF-83566 inhibited [3H]DA uptake with an IC50 of 5.73 µM. Moreover, SKF-83566 more potently inhibits the binding of [3H]CFT, a cocaine analog, with an IC50 of 0.51 µM in [3H]DA uptake and [3H]CFT binding studies.Similarly, in LLc-PK-rDAT cell, SKF-83566 also inhibits [3H]CFT binding with an IC50 of 0.77 µM in LLc-PK-rDAT cell membrane preparations[2]. MCE尚未独立确认这些方法的准确性。 仅供参考。

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%)[1]. MCE尚未独立确认这些方法的准确性。 仅供参考。

分子量：413.15

Formula：C17H19Br2NO

运输条件：美国大陆地区的室温；其他地区可能有所不同。

储存方式：请按照分析证书中推荐的条件储存产品。

文献引用：MCE 顾客使用本产品发表 3 篇科研文献

提供质量检测报告：Data Sheet、产品使用指南

产品活性：SKF-83566 hydrobromide 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尼古丁渴望的缓解。

相关产品：SKF-83566 | SQ22536 | SQ22536 (Standard) | ST034307 | NKH477 | CCPA | SKF-83566 (Standard) | MDL12330A | KH7 | LRE1 | CB⁻⁷921220 | NKY80

热门产品线：抑制剂 | 稳定性同位素标记物 | 脂质 | 糖类

Trending products：Inhibitors | Isotope-Labeled Compounds | Lipids | Saccharides

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 and SK&F 83566 are antagonists at vascular dopamine and serotonin receptors. Eur J Pharmacol. 1985 Jan 22;108(2):205-8.
[4]. Jason M Conley, et al. Development of a high-throughput screening paradigm for the discovery of small-molecule modulators of adenylyl cyclase: identification of an adenylyl cyclase 2 inhibitor. J Pharmacol Exp Ther. 2013 Nov;347(2):276-87
[5]. Yan-You Huang, et al. D1/D5 receptors and histone deacetylation mediate the Gateway Effect of LTP in hippocampal dentate gyrus. Learn Mem. 2014 Feb 18;21(3):153-60. doi: 10.1101/lm.032292.113.