SKF-83566 hydrobromide
Based on 3 publication(s) in Google Scholar
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.
- CAS No.: 108179-91-5
- Formula: C17H19Br2NO
- Molecular Weight:413.15
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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- References
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Publications Citing Use of MedChemExpress (MCE) SKF-83566 hydrobromide
MoreAll Dopamine Receptor Isoforms
MoreAll 5-HT Receptor Isoforms
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Biological Activity
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D1 Receptor |
D5 Receptor |
5-HT2 Receptor 11 nM (Ki) |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL6/J mice (6- to 9-wk-old)[1]
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Dosage:20 µg/mL (Together with nicotine for 7 d, followed by the injection of cocaine)
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Administration:Oral administration; 7 days
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Result:Blocked nicotine and cocaine-induced facilitation of LTP.
Chemical Information
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CAS No. 108179-91-5
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Molecular Weight 413.15
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Formula C17H19Br2NO
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SMILES
OC1=C(Br)C=C2CCN(C)CC(C3=CC=CC=C3)C2=C1.[H]Br
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (3)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
Nigra-Subthalamic Dopaminergic Circuitry Modulates and Represents Distinct Pain Modality in Physiological and Pain States in Mice. [Abstract]2026 Jul;13(37):e19913. PMID: 41944312 -
ACS Chem Neurosci
Estimation of Dopamine D1 Receptor Agonist Binding Kinetics Using Time-Resolved Functional Assays: Relation to Agonist-Induced Receptor Internalization by Investigational Antiparkinsonian Therapeutics. [Abstract]2025 Jul 2;16(13):2502-2512. PMID: 40537032 -
Purity & Documentation
References
[1]. Yan-You Huang, et al.D1/D5 Receptors and Histone Deacetylation Mediate the Gateway Effect of LTP in Hippocampal Dentate Gyrus. [Content Brief]
[2]. Melissa A Stouffer, et al. SKF-83566, a D1-dopamine Receptor Antagonist, Inhibits the Dopamine Transporter. J Neurochem. 2011 Sep;118(5):714-20. [Content Brief]
[3]. E H Ohlstein, et al. SCH 23390 and SK&F 83566 are antagonists at vascular dopamine and serotonin receptors. Eur J Pharmacol. 1985 Jan 22;108(2):205-8. [Content Brief]
[4]. Jason M Conley, et al. Development of a high-throughput screening paradigm for the discovery of small-molecule modulators of adenylyl cyclase: identification of an adenylyl cyclase 2 inhibitor. J Pharmacol Exp Ther. 2013 Nov;347(2):276-87 [Content Brief]
[5]. Yan-You Huang, et al. D1/D5 receptors and histone deacetylation mediate the Gateway Effect of LTP in hippocampal dentate gyrus. Learn Mem. 2014 Feb 18;21(3):153-60. doi: 10.1101/lm.032292.113. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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