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SKF-83566

Catalog No. T8702 CAS 99295-33-7

SKF-83566 is a blood-brain permeable and orally active antagonist of D1-like dopamine receptor and a weaker competitive 5-HT2 receptor antagonist with Ki of 11 nM

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SKF-83566, CAS 99295-33-7

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Purity: 95.00%

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Description	SKF-83566 is a blood-brain permeable and orally active antagonist of D1-like dopamine receptor and a weaker competitive 5-HT2 receptor antagonist with Ki of 11 nM
Targets&IC50	5-HT2 receptor:11 nM (Ki)
In vitro	SKF-83566 caused a concentration-dependent increase in peak single-pulse evoked extracellular DA concentration, with a maximum increase of 65% in 5 μM SKF-83566.?This was accompanied by a concentration-dependent increase in extracellular DA concentration clearance time.?Both effects were occluded by nomifensine (1 μM), a dopamine transporter (DAT) inhibitor, suggesting that SKF-83566 acted via the DAT.?Tested this by examining [(3)H]DA uptake into LLc-PK cells expressing rat DAT, and confirmed that SKF-83566 is a competitive DAT inhibitor with an IC(50) of 5.7 μM.?Binding studies with [(3)H]CFT, a cocaine analog, showed even more potent action of SKF-83566 at the DAT cocaine binding site (IC(50) = 0.51 μM)[1].
In vivo	The facilitation induced by nicotine and cocaine can be blocked by oral administration of the dopamine D1/D5 receptor antagonist (SKF 83566)

Molecular Weight	332.23
Formula	C17H18BrNO
CAS No.	99295-33-7

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 10 mM

References and Literature

1. Melissa A Stouffer, et al. SKF-83566, a D1-dopamine Receptor Antagonist, Inhibits the Dopamine Transporter. J Neurochem. 2011 Sep;118(5):714-20. 2. Yan-You Huang, et al.D1/D5 Receptors and Histone Deacetylation Mediate the Gateway Effect of LTP in Hippocampal Dentate Gyrus. 3. 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.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Parkinson's Disease Compound Library Anti-Hypertension Compound Library NO PAINS Compound Library Anti-Alzheimer's Disease Compound Library Anti-Neurodegenerative Disease Compound Library

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Keywords

SKF-83566 99295-33-7 GPCR/G Protein Neuroscience Dopamine Receptor 5-HT Receptor AChR nicotine craving dorsal striatum Inhibitor SKF 83566 Adenylate Cyclase dentate gyrus SKF83566 dopamine uptake 5-hydroxytryptamine Receptor inhibit associative memory Serotonin Receptor Adenylyl cyclase hippocampus parkinson’s disease drug-related inhibitor

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