| 中文名称: | SKF-83566 hydrobromide | ||||
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| 英文名称: | SKF-83566 hydrobromide | ||||
| 别名: | 8-溴-2,3,4,5-四氢-3-甲基-5-苯基-1H-3-苯并氮杂卓-7-醇氢溴酸盐 8-Bromo-3-methyl-5-phenyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-ol hydrobromide | ||||
| CAS No: | 108179-91-5 | 分子式: | C17H18BrNO.HBr | 分子量: | 413.15 |
| CAS No: | 108179-91-5 | ||||
| 分子式: | C17H18BrNO.HBr | ||||
| 分子量: | 413.15 | ||||
基本信息
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产品编号： |
S10819 |
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产品名称： |
SKF-83566 hydrobromide |
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CAS: |
108179-91-5 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
二年 |
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分子量： |
413.15 |
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化学名： |
1H-3-Benzazepin-7-ol,8-broMo-2,3,4,5-tetrahydro-3-Methyl-5-phenyl-,hydrobroMide(1:1) |
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Solubility (25°C)： |
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体外:
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DMSO |
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Ethanol |
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Water |
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体内(现配现用): |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
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生物活性
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产品描述 |
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=11nM)。 |
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靶点 |
D1 Receptor |
D5 Receptor |
5-HT2 Receptor 11 nM (Ki) |
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体外研究 |
SKF-83566 (0.1μM-10μM) 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 5μM.The EC50 value of this effect of SKF-83566 is 1.3μM.SKF-83566 inhibited [3H]DA uptake with an IC50 of 5.73μM.Moreover,SKF-83566 more potently inhibits the binding of [3H]CFT,a cocaine analog,with an IC50 of 0.51μM 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 0.77μM in LLc-PK-rDAT cell membrane preparations. |
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体内研究 |
SKF 83566 hydrobromide (oral administration;20µg/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%). |
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Animal Model: |
Male C57BL6/J mice (6-to 9-wk-old) |
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Dosage: |
20µg/mL (Together with nicotine for 7d,followed by the injection of cocaine) |
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Administration: |
Oral administration;7 days |
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Result: |
Blocked nicotine and cocaine-induced facilitation of LTP. |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
