计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
SKF-83566 is a potent, blood-brain permeable and orally active D1-like dopamine receptor (D1DR) antagonist and a weaker competitive antagonist at the vascular 5-HT 2 receptor ( K i =11 nM) SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC 50 of 5.7 μM SKF-83566 also shows selective inhibition for adenylyl cyclase 2 (AC2) over AC 1 and AC 5 in the isolated rabbit thoracic aorta. SKF-83566 can be used for research of parkinson’s disease and nicotine craving alleviation.
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 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, 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
SKF 83566 (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%) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.
IC50& Target:D 1 Receptor D 5 Receptor 5-HT 2 Receptor 11 nM (Ki)
规格
规格或纯度
10mM in DMSO
英文名称
SKF-83566
生化机理
SKF-83566 是一种强效、xa0 血脑渗透性和口服活性 D1 类多巴胺受体（D1DR）拮抗剂，也是血管 5-HT 2 受体（K i =11 nM）的较弱竞争性拮抗剂。SKF-83566 是一种竞争性 DAT（多巴胺转运体）拮抗剂。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
分子类型
小分子
Isomeric SMILES
CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Br
关联CAS
PubChem CID
MeSH Entry Terms
1H-3-benzazepin-7-ol, 8-bromo-2,3,4,5-tetrahydro-3-methyl-5-phenyl-;1H-3-benzazepin-7-ol, 8-bromo-2,3,4,5-tetrahydro-3-methyl-5-phenyl-, (S-isomer);7-bromo-8-hydroxy-3-methyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine;8-bromo-2,3,4,5-tetrahydro-3-methyl
分子量
332.23
技术文档
高级数据
关联靶点（人）
DRD1
Tclin
D（1A）多巴胺受体(D(1A) dopamine receptor)
(0 活性数据)
DRD5
Tchem
D（1B）多巴胺受体(D(1B) dopamine receptor)
(0 活性数据)
安全和危险性（GHS）
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
常见问题
本产品应如何储存？
请于?80 °C条件下保存。需超低温保存以维持规定的有效期。
本产品如何运输？
本产品采用干冰配冷袋冷冻运输。收货后请立即拆包，并按上述储存条件保存；处理干冰时请戴隔热手套并保持通风。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 99295-33-7，分子式为 C17H18BrNO，分子量为 332.23 g/mol。
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