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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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S647449-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $95.90 | |
S647449-10mg | 10mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $150.90 | |
S647449-25mg | 25mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $270.90 |
Synonyms | SKF-83566 | 8-bromo-2,3,4,5-tetrahydro-3-methyl-5-phenyl-1h-3-benzazepin-7-ol | SK83566 | SK-83566 | CHEBI:91747 | PDSP1_000503 | 8-Bromo-3-methyl-5-phenyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-ol | 8-Bromo-3-methyl-5-phenyl-2,3,4,5-tetrahydro-1H-3-benza |
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Specifications & Purity | ≥99% |
Biochemical and Physiological Mechanisms | SKF-83566 is a potent,xa0blood-brain permeable and orally active D1-like dopamine receptor (D1DR) antagonist and a weaker competitive antagonist at the vascular 5-HT 2 receptor ( K i =11 nM). SKF-83566 is a competitive DAT (dopamine transporter) |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Product 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-HT 2 receptor ( K i =11 nM) SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC 50 of 5.7 μM SKF-83566 also shows selective inhibition for adenylyl cyclase 2 (AC2) over AC 1 and AC 5 in the isolated rabbit thoracic aorta. SKF-83566 can be used for research of parkinson’s disease and nicotine craving alleviation. 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 EC 50 value of this effect of SKF-83566 is 1.3 μM. SKF-83566 inhibited [ 3 H]DA uptake with an IC 50 ?of 5.73 μM. Moreover, SKF-83566 more potently inhibits the binding of [ 3 H]CFT, with an IC 50 ?of 0.51 μM in [ 3 H]DA uptake and [ 3 H]CFT binding studies. Similarly, in LLc-PK-rDAT cell, SKF-83566 also inhibits [ 3 H]CFT binding with an IC 50 ?of 0.77 μM in LLc-PK-rDAT cell membrane preparations. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo SKF 83566 (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%) . 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) 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. Form:Solid IC50& Target:D 1 Receptor D 5 Receptor 5-HT 2 Receptor 11 nM (Ki) |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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Dopamine D2 receptor antagonist | ANTAGONIST | ALA217 | Dopamine D2 receptor | SINGLE PROTEIN | Homo sapiens | ||
Dopamine D2 receptor antagonist | ANTAGONIST | ALA217 | Dopamine D2 receptor | SINGLE PROTEIN | Homo sapiens | ||
Dopamine D2 receptor antagonist | ANTAGONIST | ALA217 | Dopamine D2 receptor | SINGLE PROTEIN | Homo sapiens | ||
Dopamine D2 receptor antagonist | ANTAGONIST | ALA217 | Dopamine D2 receptor | SINGLE PROTEIN | Homo sapiens | ||
Dopamine D2 receptor modulator | MODULATOR | ALA217 | Dopamine D2 receptor | SINGLE PROTEIN | Homo sapiens | ||
Dopamine D2 receptor antagonist | ANTAGONIST | ALA217 | Dopamine D2 receptor | SINGLE PROTEIN | Homo sapiens | ||
Dopamine D2 receptor antagonist | ANTAGONIST | ALA217 | Dopamine D2 receptor | SINGLE PROTEIN | Homo sapiens | ||
Dopamine D2 receptor agonist | AGONIST | ALA217 | Dopamine D2 receptor | SINGLE PROTEIN | Homo sapiens | ||
Dopamine D2 receptor antagonist | ANTAGONIST | ALA217 | Dopamine D2 receptor | SINGLE PROTEIN | Homo sapiens | ||
Dopamine D2 receptor antagonist | ANTAGONIST | ALA217 | Dopamine D2 receptor | SINGLE PROTEIN | Homo sapiens |
IUPAC Name | 8-bromo-3-methyl-5-phenyl-1,2,4,5-tetrahydro-3-benzazepin-7-ol |
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INCHI | InChI=1S/C17H18BrNO/c1-19-8-7-13-9-16(18)17(20)10-14(13)15(11-19)12-5-3-2-4-6-12/h2-6,9-10,15,20H,7-8,11H2,1H3 |
InChi Key | XFTVOHWWEQGXLS-UHFFFAOYSA-N |
Canonical SMILES | CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Br |
Isomeric SMILES | CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)Br |
Alternate CAS | 99295-33-7 |
PubChem CID | 1243 |
MeSH Entry Terms | 1H-3-benzazepin-7-ol, 8-bromo-2,3,4,5-tetrahydro-3-methyl-5-phenyl-;1H-3-benzazepin-7-ol, 8-bromo-2,3,4,5-tetrahydro-3-methyl-5-phenyl-, (S-isomer);7-bromo-8-hydroxy-3-methyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine;8-bromo-2,3,4,5-tetrahydro-3-methyl |
Molecular Weight | 332.23 |
Solubility | DMSO : 33.33 mg/mL (100.32 mM; Need ultrasonic) |
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