1. GPCR/G Protein
    Neuronal Signaling
  2. Dopamine Receptor
    5-HT Receptor
    Adenylate Cyclase
  3. SKF-83566

SKF-83566 

目录号: HY-103430A 纯度: 99.86%
产品使用指南

SKF-83566 是一种有效的,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 =11 nM)。SKF-83566 是一种竞争性多巴胺转运蛋白 (DAT) 抑制剂,IC50 为 5.7 μM。在离体兔胸主动脉中,SKF-83566 对腺苷基环化酶 2 (AC2) 的选择性高于对 AC1 和 AC5 的。SKF-83566 可用于研究帕金森氏症和对尼古丁渴望的缓解的相关研究。

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SKF-83566 Chemical Structure

SKF-83566 Chemical Structure

CAS No. : 99295-33-7

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Description

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-HT2 receptor (Ki=11 nM)[1][3]. SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC50 of 5.7 μM[2]. SKF-83566 also shows selective inhibition for adenylyl cyclase 2 (AC2) over AC1 and AC5 in the isolated rabbit thoracic aorta[4]. SKF-83566 can be used for research of parkinson’s disease and nicotine craving alleviation[5].

IC50 & Target[1]

D1 Receptor

 

D5 Receptor

 

5-HT2 Receptor

11 nM (Ki)

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[2].
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[2].

In Vivo

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%)[1].

Animal Model: Male C57BL6/J mice (6- to 9-wk-old)[1]
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.
Molecular Weight

332.23

Formula

C₁₇H₁₈BrNO

CAS No.

99295-33-7

SMILES

OC1=C(Br)C=C2CCN(C)CC(C3=CC=CC=C3)C2=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
References
  • 摩尔计算器

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Keywords:

SKF-83566SKF83566SKF 83566Dopamine Receptor5-HT ReceptorAdenylate CyclaseSerotonin Receptor5-hydroxytryptamine ReceptorAdenylyl cyclasedentate gyrusDGhippocampusdrug-relatedassociative memorydopamine uptakedorsal striatumparkinson’s diseasenicotine cravingInhibitorinhibitorinhibit

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产品名称:
SKF-83566
目录号:
HY-103430A
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