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

SKF-83566 hydrobromide 

Cat. No.: HY-103430
Handling Instructions

SKF-83566 hydrobromide 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). SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC50 of 5.7 μM. SKF-83566 also shows selective inhibition for adenylyl cyclase 2 (AC2) over AC1 and AC5 in the isolated rabbit thoracic aorta. SKF-83566 can be used for the research of parkinson’s disease and nicotine craving alleviation.

For research use only. We do not sell to patients.

SKF-83566 hydrobromide Chemical Structure

SKF-83566 hydrobromide Chemical Structure

CAS No. : 108179-91-5

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Description

SKF-83566 hydrobromide 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 the 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

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)[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

413.15

Formula

C₁₇H₁₉Br₂NO

CAS No.

108179-91-5

SMILES

OC1=C(Br)C=C2CCN(C)CC(C3=CC=CC=C3)C2=C1.[H]Br

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

SKF-83566SKF83566SKF 83566Dopamine Receptor5-HT ReceptorAdenylate CyclaseSerotonin Receptor5-hydroxytryptamine ReceptorAdenylyl cyclasedentate gyrusDGhippocampusdrug-relatedassociative memorydopamine uptakedorsal striatumInhibitorinhibitorinhibit

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SKF-83566 hydrobromide
Cat. No.:
HY-103430
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