| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| S655034-1ml |
1ml |
期货  |
|
| 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。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 产品介绍 |
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) |
| Isomeric SMILES | CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Br |
|---|---|
| 关联CAS | 99295-33-7 |
| PubChem CID | 1243 |
| 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 |
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