Flucindole
Flucindole is an orally active dopamine receptor inhibitor (IC50 = 240 nM) that also exhibits affinity for S2 receptors. Flucindole inhibits amphetamine-induced stereotyped behaviors in rats, and increases the levels of dopamine metabolites in the striatum of rats and mice. Flucindole can be used in the research of psychosis.
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- CAS No.: 40594-09-0
- Formule: C14H16F2N2
- Masse moléculaire:250.29
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
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Dopamine Receptor 240 nM (IC50) |
Flucindole binds to dopamine, α1, S1, and S2 receptors in rat brain membrane preparations, with the highest affinity for dopamine receptors (IC50 = 240 nM) and no appreciable binding to α2, β, muscarinic, or tryptamine receptors[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Flucindole (0.1-40 mg/kg; i.p.; single dose) dose-dependently elevates mouse striatal DA metabolites DOPAC, HVA, and 3-MT, with a significant decrease in DA observed only at the highest tested dose of 40.0 mg/kg[2].
Flucindole (0.1-5 mg/kg; i.p.; single dose) dose-dependently elevates rat striatal DOPAC and HVA levels, with a significant decrease in DA observed only at the 5.0 mg/kg dose[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Swiss Hausche (male, 25-30 g)[2]
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Dosage:0.1 mg/kg; 2.0 mg/kg; 5.0 mg/kg; 40.0 mg/kg
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Administration:i.p.; single dose
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Result:Elevated striatal DOPAC, HVA and 3-MT across all doses: 0.1 mg/kg (60 min) raised metabolites to 132-138% baseline with unchanged DA; 2.0 mg/kg boosted metabolites to 242-406% at 30/60 min while DA stayed at 90% control; 5.0 mg/kg (60 min) lifted metabolites to 176-425% with DA at 92% control; 40.0 mg/kg (60 min) pushed metabolites to 170-510% and reduced DA to 75% control.
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Animal Model:Sprague Dawley (male, 170-190 g)[2]
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Dosage:0.1 mg/kg; 0.5 mg/kg; 2.0 mg/kg; 5.0 mg/kg
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Administration:i.p.; single dose
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Result:Showed no striatal DOPAC, HVA or DA alterations at 0.1 mg/kg 60 minutes post-injection.
Elevated DOPAC and HVA without DA changes at 0.5 mg/kg 60 minutes post-injection.
Elevated DOPAC and HVA progressively from 15 min to 120 min before declining at 180 min at 2.0 mg/kg, while DA levels remained unmodified across all time points.
Elevated DOPAC and HVA and reduced DA at 5.0 mg/kg 60 minutes post-injection.
All detected measurable shifts reached statistical significance.
Chemical Information
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CAS No. 40594-09-0
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Masse moléculaire 250.29
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Formule C14H16F2N2
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SMILES
FC=1C=C(F)C=2NC3=C(C2C1)CC(N(C)C)CC3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Edelson J, et al. Disposition of a series of tetrahydrocarbazoles. Drug metabolism reviews. 1980;11(2):263-89. [Content Brief]
[2]. Wood PL, et al. Ciclindole and flucindole: novel tetrahydrocarbazolamine neuroleptics. Progress in neuro-psychopharmacology & biological psychiatry. 1984;8(4-6):773-7. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Flucindole Related Classifications
HY-105760 Related Classifications
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