8-BROMO-2,3,4,5-TETRAHYDRO-3-METHYL-5-PHENYL-1H-3-BENZAZEPIN-7-OL HYDROBROMIDE

8-BROMO-2,3,4,5-TETRAHYDRO-3-METHYL-5-PHENYL-1H-3-BENZAZEPIN-7-OL HYDROBROMIDE

中文名称8-BROMO-2,3,4,5-TETRAHYDRO-3-METHYL-5-PHENYL-1H-3-BENZAZEPIN-7-OL HYDROBROMIDE
中文同义词化合物SKF-83566
英文名称8-BROMO-2,3,4,5-TETRAHYDRO-3-METHYL-5-PHENYL-1H-3-BENZAZEPIN-7-OL HYDROBROMIDE
英文同义词SKF 83566 HYDROBROMIDE;8-BROMO-2,3,4,5-TETRAHYDRO-3-METHYL-5-PHENYL-1H-3-BENZAZEPIN-7-OL HYDROBROMIDE;(+/-)-SKF-83566 HYDROCHLORIDE SELECTIVE DOPAMINE D1;(±)-SCH-24543, (±)-7-Bromo-8-hydroxy-3-methyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride;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-ol;159021;SKF 83566 hydrobromi
CAS号99295-33-7
分子式C17H18BrNO
分子量332.23
EINECS号604-604-1
相关类别Dopamine receptor
Mol文件99295-33-7.mol
结构式8-BROMO-2,3,4,5-TETRAHYDRO-3-METHYL-5-PHENYL-1H-3-BENZAZEPIN-7-OL HYDROBROMIDE 结构式

8-BROMO-2,3,4,5-TETRAHYDRO-3-METHYL-5-PHENYL-1H-3-BENZAZEPIN-7-OL HYDROBROMIDE 性质

储存条件Desiccate at RT
溶解度45%(w/v)aq2-羟丙基-β-环糊精:≥14 mg/mL
形态固体
颜色驼色

8-BROMO-2,3,4,5-TETRAHYDRO-3-METHYL-5-PHENYL-1H-3-BENZAZEPIN-7-OL HYDROBROMIDE 用途与合成方法

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。

D 1 Receptor

D 5 Receptor

5-HT 2 Receptor

11 nM (Ki)

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, a cocaine analog, 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.

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%).

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.

安全信息

WGK Germany3

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2023/03/20HY-1034308-BROMO-2,3,4,5-TETRAHYDRO-3-METHYL-5-PHENYL-1H-3-BENZAZEPIN-7-OL HYDROBROMIDE
SKF-83566 hydrobromide
99295-33-75mg950元
2023/03/20HY-1034308-BROMO-2,3,4,5-TETRAHYDRO-3-METHYL-5-PHENYL-1H-3-BENZAZEPIN-7-OL HYDROBROMIDE
SKF-83566 hydrobromide
99295-33-710mg1500元

8-BROMO-2,3,4,5-TETRAHYDRO-3-METHYL-5-PHENYL-1H-3-BENZAZEPIN-7-OL HYDROBROMIDE 上下游产品信息

"8-BROMO-2,3,4,5-TETRAHYDRO-3-METHYL-5-PHENYL-1H-3-BENZAZEPIN-7-OL HYDROBROMIDE"相关产品信息
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