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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- No. CAS: 2640663-79-0
- Fòrmula: C20H24Cl2N4O2
- Peso molecular:423.34
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Actividad biológica
Descripciòn
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.
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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No. CAS 2640663-79-0
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Peso molecular 423.34
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Obuprazine Related Classifications
HY-183734 Related Classifications
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