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.
For research use only. We do not sell to patients.
- CAS No.: 40594-09-0
- Formula: C14H16F2N2
- Molecular Weight:250.29
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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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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Molecular Weight 250.29
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Formula C14H16F2N2
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SMILES
FC=1C=C(F)C=2NC3=C(C2C1)CC(N(C)C)CC3
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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.
Purity & Documentation
References
[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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