2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor 5-HT Receptor G Protein-coupled Receptor Kinase (GRK)
  4. 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.

For research use only. We do not sell to patients.

Obuprazine

Obuprazine Chemical Structure

CAS No. : 2640663-79-0

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Obuprazine Related Antibodies

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Description

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[1].

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.

Obuprazine Related Antibodies
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

Obuprazine (1 mg/kg; p.o.; single dose) exhibits antipsychotic effect on rats[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male F344 rats (6-8 weeks) with schizophrenia[1]
Dosage: 1 mg/kg
Administration: p.o.; single dose
Result: Exhibited an avoidance response inhibition rate (CAR value) of 18.5%.
Showed antipsychotic effect on rats.
Molecular Weight

423.34

Formula

C20H24Cl2N4O2
CAS No.
SMILES

ClC1=C(C=CC=C1Cl)N2CCN(CC2)CC[C@H]3C[C@@H](C3)NC(C4=NC=CO4)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Obuprazine Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Obuprazine2640663-79-0Dopamine Receptor5-HT ReceptorG Protein-coupled Receptor Kinase (GRK)Serotonin Receptor5-hydroxytryptamine ReceptorG protein-coupled receptorcalcium fluxschizophreniadopamine D3 receptor5-HT2A receptorcAMPInhibitorinhibitorinhibit

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