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99295-33-7

中文名稱 8-BROMO-2,3,4,5-TETRAHYDRO-3-METHYL-5-PHENYL-1H-3-BENZAZEPIN-7-OL HYDROBROMIDE
英文名稱 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 結(jié)構(gòu)式 99295-33-7 結(jié)構(gòu)式

基本信息

中文別名
化合物SKF-83566
英文別名
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

物理化學(xué)性質(zhì)

儲存條件Desiccate at RT
溶解度45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: ≥14 mg/mL
形態(tài)solid
顏色light tan

安全數(shù)據(jù)

WGK Germany3
8-BROMO-2,3,4,5-TETRAHYDRO-3-METHYL-5-PHENYL-1H-3-BENZAZEPIN-7-OL HYDROBROMIDE價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
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
2023/03/20HY-1034308-BROMO-2,3,4,5-TETRAHYDRO-3-METHYL-5-PHENYL-1H-3-BENZAZEPIN-7-OL HYDROBROMIDE
SKF-83566 hydrobromide		99295-33-725mg2700元

常見問題列表

生物活性
SKF-83566 是一種有效的，可通透血腦屏障的，具有口服活性的 D1 樣多巴胺受體 ( D1-like dopamine receptor) 拮抗劑，也可以作為一種較弱的競爭性拮抗劑，作用于血管 5-HT2 受體 (Ki =11 nM)。SKF-83566 是一種競爭性多巴胺轉(zhuǎn)運(yùn)蛋白 (DAT) 抑制劑，IC50?為 5.7 μM。在離體兔胸主動脈中，SKF-83566 對腺苷基環(huán)化酶 2 (AC2) 的選擇性高于對 AC1 和 AC5 的。SKF-83566 可用于研究帕金森氏癥和對尼古丁渴望的緩解的相關(guān)研究。
靶點

D 1 Receptor

D 5 Receptor

5-HT 2 Receptor

11 nM (Ki)

體外研究

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.

體內(nèi)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.
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