Obuprazine
Obuprazine is an orally active dopamine D3 receptor agonist and 5-HT2A receptor antagonist with IC50 values of 0.37 and 4.19 nM, respectively. Obuprazine acts as a G protein-coupled receptor modulater. Obuprazine can be used for the research of schizophrenia.
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- CAS No.: 2640663-79-0
- Formule: C20H24Cl2N4O2
- Masse moléculaire:423.34
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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
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
D3 Receptor 0.37 nM (IC50) |
5-HT2A Receptor 4.19 nM (IC50) |
In Vitro
Obuprazine acts as a potent agonist in cells stably expressing the dopamine D3 receptor, reducing cAMP levels with an EC50 of 0.6 nM[1].
Obuprazine potently inhibits 5-HT2A receptor-mediated calcium flux in stably expressing cells with an IC50 of 2.21 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
| Species | Dose | Route | Tmax | Cmax | AUC0-t | AUC0-∞ | T1/2 | MRT |
|---|---|---|---|---|---|---|---|---|
| Mice[1] | 5 mg/kg | p.o. | 0.5 h | 673.0 ng/mL | 1844.0 ng·h/mL | 1970.0 ng·h/mL | 1.9 h | 3.1 h |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male F344 rats (6-8 weeks) with schizophrenia[1]
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Dosage:1 mg/kg
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Administration:p.o.; single dose
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Result:Exhibited an avoidance response inhibition rate (CAR value) of 18.5%.
Showed antipsychotic effect on rats.
Chemical Information
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CAS No. 2640663-79-0
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Masse moléculaire 423.34
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Formule C20H24Cl2N4O2
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SMILES
ClC1=C(C=CC=C1Cl)N2CCN(CC2)CC[C@H]3C[C@@H](C3)NC(C4=NC=CO4)=O
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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.
Protocole
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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.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Obuprazine Related Classifications
HY-183734 Related Classifications
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