99295-33-7

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

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

CAS 99295-33-7

分子式 C17H18BrNO

分子量 332.23

MOL 文件 99295-33-7.mol

更新日期 2023/03/27 16:20:57

99295-33-7 结构式

基本信息物理化学性质安全数据图谱信息 8-BROMO-2,3,4,5-TETRAHYDRO-3-METHYL-5-PHENYL-1H-3-BENZAZEPIN-7-OL HYDROBROMIDE价格(试剂级) 常见问题列表

基本信息

中文别名

化合物SKF-83566

英文别名

159021
SKF 83566 HYDROBROMIDE
(+/-)-SKF-83566 HYDROCHLORIDE SELECTIVE DOPAMINE D1
8-bromo-2,3,4,5-tetrahydro-3-methyl-5-phenyl-1H-3-benzazepin-7-ol
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 HYDROBROMIDE
(±)-SCH-24543, (±)-7-Bromo-8-hydroxy-3-methyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride

物理化学性质

储存条件Desiccate at RT

溶解度45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: ≥14 mg/mL

形态solid

颜色light tan

安全数据

WGK Germany3

图谱信息

8-BROMO-2,3,4,5-TETRAHYDRO-3-METHYL-5-PHENYL-1H-3-BENZAZEPIN-7-OL HYDROBROMIDE(99295-33-7)核磁图(¹HNMR)

8-BROMO-2,3,4,5-TETRAHYDRO-3-METHYL-5-PHENYL-1H-3-BENZAZEPIN-7-OL HYDROBROMIDE价格(试剂级)

报价日期	产品编号	产品名称	CAS号	包装	价格
2023/03/20	HY-103430	8-BROMO-2,3,4,5-TETRAHYDRO-3-METHYL-5-PHENYL-1H-3-BENZAZEPIN-7-OL HYDROBROMIDE SKF-83566 hydrobromide	99295-33-7	5mg	950元
2023/03/20	HY-103430	8-BROMO-2,3,4,5-TETRAHYDRO-3-METHYL-5-PHENYL-1H-3-BENZAZEPIN-7-OL HYDROBROMIDE SKF-83566 hydrobromide	99295-33-7	10mg	1500元
2023/03/20	HY-103430	8-BROMO-2,3,4,5-TETRAHYDRO-3-METHYL-5-PHENYL-1H-3-BENZAZEPIN-7-OL HYDROBROMIDE SKF-83566 hydrobromide	99295-33-7	25mg	2700元

常见问题列表

生物活性

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。

靶点

D ₁ Receptor

D ₅ Receptor

5-HT ₂ Receptor

11 nM (Ki)

体外研究

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.

体内研究

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.