Panuramine
Panuramine is a blood-brain barrier permeable, orally active selective 5-HT Receptor antagonist with an IC50 of 22 nM. Panuramine prevents 5-HT reuptake through non-competitive antagonism of 5-HT Receptor, but does not affect dopamine uptake. Panuramine can be used for research on depression.
For research use only. We do not sell to patients.
- CAS No.: 80349-58-2
- Formula: C24H25N3O2
- Molecular Weight:387.47
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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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
In Vitro
Panuramine (30-200 nM; 2 min) is a potent and selective non-competitive inhibitor of 5-HT uptake in rat cortical synaptosomes with an IC50 of 22 nM, and it weakly inhibits [3H] noradrenaline (NA) uptake[1].
Panuramine (up to 10 μM) does not displace the specific binding of [3H]5-HT or [3H] spiroperidol and does not inhibit [3H] dopamine (DA) uptake in rat brain cortical membranes at concentrations up to 10 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wild-type rats, intraperitoneally injected with p-chloroamphetamine (PCA, 20 mg/kg) to induce 5-HT depletion in the brain[1]
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Dosage:50 mg/kg
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Administration:p.o.; single dose; administered 0.5, 1.0, 2.0, 4.0, 16.0, 24.0 hours prior to PCA injection
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Result:Significantly antagonized the PCA-induced depletion of 5-HT in the brain within 2-4 hours after administration.
Panuramine's antagonistic effect on 5-HT depletion was no longer demonstrable 16 hours after administration.
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Animal Model:Wild-type rats, intraperitoneally injected with p-chloroamphetamine (PCA, 20 mg/kg) to induce 5-HT depletion in the brain[1]
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Dosage:3.13, 6.25, 12.5, 25, 50, 100 mg/kg
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Administration:p.o.; single dose; pre-administered 30 minutes prior to PCA injection
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Result:Antagonized the PCA-induced reduction in brain 5-HT levels in a dose-dependent manner.
Panuramine's in vivo ED50 (2 hours after treatment) for this antagonism was calculated to be 15.8 mg/kg.
Chemical Information
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CAS No. 80349-58-2
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Molecular Weight 387.47
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Formula C24H25N3O2
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SMILES
O=C(NC1CCN(CC1)CC2=CC3=C(C=CC=C3)C=C2)NC(C4=CC=CC=C4)=O
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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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Panuramine Related Classifications
HY-187708 Related Classifications
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Keywords
- Panuramine
- 80349-58-2
- 5-HT Receptor
- p-chloroamphetamine-induced depletion of brain 5-HT
- depression
- selective serotonin transporter inhibitor
- 5-HT release
- synaptosomes
- hypothalamic slices
- 5-HT1 or 5-HT2 receptor binding
- rat cortical synaptosomes
- rat
- non-competitive blocker of 5-HT uptake
- Inhibitor
- inhibitor
- inhibit