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

SKF-83566 

Cat. No.: HY-103430A Purity: 99.86%
Handling Instructions

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). 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 research of parkinson’s disease and nicotine craving alleviation.

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

SKF-83566 Chemical Structure

SKF-83566 Chemical Structure

CAS No. : 99295-33-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 95 In-stock
Estimated Time of Arrival: December 31
5 mg USD 95 In-stock
Estimated Time of Arrival: December 31
10 mg USD 150 In-stock
Estimated Time of Arrival: December 31
25 mg USD 270 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

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

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
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (100.32 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0100 mL 15.0498 mL 30.0996 mL
5 mM 0.6020 mL 3.0100 mL 6.0199 mL
10 mM 0.3010 mL 1.5050 mL 3.0100 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.52 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.52 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.52 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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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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