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SKF-83566 hydrobromide

CAS No. : 108179-91-5

MCE 站：SKF-83566 hydrobromide

产品活性：SKF-83566 hydrobromide 是一种有效的，可通透血脑屏障的，具有口服活性的多巴胺 D1/D5 受体 (dopamine D1/D5 receptor) 拮抗剂。SKF-83566 hydrobromide 是一种竞争性 DAT 多巴胺转运蛋白抑制剂，IC₅₀ 为 5.7 μM，可减弱动物实验模型的体内可卡因的作用。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Dopamine Receptor

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 EC₅₀ value of this effect of SKF-83566 is 1.3 μM.
SKF-83566 inhibited [³H]DA uptake with an IC₅₀?of 5.73 μM. Moreover, SKF-83566 more potently inhibits the binding of [³H]CFT, a cocaine analog, with an IC₅₀?of 0.51 μM 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 0.77 μM in LLc-PK-rDAT cell membrane preparations.

In Vivo: SKF 83566 hydrobromide (oral administration; 20 ?g/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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