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Aripiprazole

CHEMBL1112 Phase 4 承認済み Small molecule
Half-Life
75 hours
Bioavailability
—
Protein Binding
—
Molecular Weight
448.4 g/mol
LogP
4.6
Phase
4

Unlike antipsychotics that simply block dopamine, aripiprazole acts as a partial agonist at dopamine D2 and serotonin 5-HT1A receptors. As a partial agonist it can either mildly stimulate or restrain these pathways depending on the surrounding level of neurotransmitter, helping to stabilize signaling rather than shut it down. This mechanism supports its use in schizophrenia and bipolar disorder, as an add-on for depression, and for irritability in autism. A small molecule (C23H27Cl2N3O2) with a notably long half-life of about 75 hours, it reaches steady state slowly and sustains its effect between doses. The stabilizing, buffering nature of partial agonism gives it a receptor profile distinct from earlier second-generation agents. Aripiprazole is an approved antipsychotic used across several psychiatric indications.

An atypical antipsychotic that acts as a partial agonist at dopamine and serotonin receptors rather than simply blocking them, helping to stabilize these pathways in schizophrenia and bipolar disorder. It is also approved as an adjunct for depression and for irritability in autism.

分子量

448.3850 g/mol

LogP

4.60

TPSA

44.80 Ų

リピンスキーの五則

適合

治療領域

Cardiovascular Disease Psychiatry Alzheimer's Disease Parkinson's Disease Schizophrenia Bipolar Disorder Generalized Anxiety Disorder Gastroesophageal Reflux Disease Non-Alcoholic Fatty Liver Disease Hyperlipidemia Obesity Type 2 Diabetes Major Depressive Disorder

薬物分類

N — N - Nervous System

作用機序

Partial agonist at D2 and 5-HT1A receptors.

Pharmacokinetics (PK)

Half-Life 75 hours

Pharmacodynamics (PD)

機序

Partial agonist at D2 and 5-HT1A receptors.

2D構造

SVG PNG

Cite this structure


                        

                            
                            
                        

                    

                


                
                

                    

                    

                        
Embed this structure

                        

                        

                            
                            
                        

                    

                

                

                
                

                    
SMILES

                    
O=C1CCc2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2N1

                

                

                
                

                    
InChI

                    
InChI=1S/C23H27Cl2N3O2/c24-19-4-3-5-21(23(19)25)28-13-11-27(12-14-28)10-1-2-15-30-18-8-6-17-7-9-22(29)26-20(17)16-18/h3-6,8,16H,1-2,7,9-15H2,(H,26,29)

                

                

                

                    
                    

                        
Molecular Formula

                        
C23H27Cl2N3O2

                    

                    
                    

                        
HBD / HBA

                        
1 / 4

                    

                    
                    

                        
回転可能結合数

                        
7

                    

                    
                    
                    

                        
重原子数

                        
30

                    

                    
                

            


            
            

                
                

                    
                    

                        

                            DRD2 (Dopamine D2 Receptor)
                            Partial Agonist
                        

                        
                        Primary Target
                        
                    

                    
                    

                        

                            SLC6A4 (Serotonin Transporter)
                            Partial Agonist
                        

                        
                    

                    
                

                
            


            
            

                
                

                    
                    
                        

                            

  
  Major


                            
                                Aripiprazole + Carbamazepine
                            
                        

                        
                        
Carbamazepine dramatically reduces aripiprazole plasma levels through potent CYP3A4 induction, potentially rendering antipsychotic treatment ineffective.

                        
                    
                    
                    
                        

                            

  
  Major


                            
                                Aripiprazole + Levodopa
                            
                        

                        
                        
Aripiprazole acts as a partial D2 agonist/antagonist and can oppose levodopa's dopaminergic therapy, worsening Parkinson's disease symptoms.

                        
                    
                    
                    
                        

                            

  
  Moderate


                            
                                Aripiprazole + Azithromycin
                            
                        

                        
                        
Azithromycin inhibits CYP3A4-mediated aripiprazole metabolism, potentially increasing aripiprazole exposure; both drugs have modest QT-prolonging effects.

                        
                    
                    
                    
                        

                            

  
  Moderate


                            
                                Aripiprazole + Fluconazole
                            
                        

                        
                        
Fluconazole inhibits CYP3A4 and CYP2C19, increasing aripiprazole plasma concentrations and the risk of aripiprazole adverse effects.

                        
                    
                    
                    
                        

                            

  
  Moderate


                            
                                Aripiprazole + Bupropion
                            
                        

                        
                        
Bupropion, a CYP2D6 inhibitor, significantly increases aripiprazole plasma concentrations, increasing the risk of dose-dependent adverse effects.

                        
                    
                    
                    
                        

                            

  
  Moderate


                            
                                Aripiprazole + Fluoxetine
                            
                        

                        
                        
Fluoxetine is a potent CYP2D6 inhibitor that significantly increases aripiprazole plasma concentrations, enhancing both efficacy and adverse effects.

                        
                    
                    
                

                
            


            
            

                
                


    
    
        
    
    
    
No side effects recorded

    
    
Side effect data is not yet available for this drug.

    



                
            


            
            
            

                
よくある質問

                

                    
                    

                        
                        

                            
An atypical antipsychotic that acts as a partial agonist at dopamine and serotonin receptors rather than simply blocking them, helping to stabilize these pathways in schizophrenia and bipolar disorder. It is also approved as an adjunct for depression and for irritability in autism.

                        

                    

                    

                    

                    
                    

                        
                        

                            
Partial agonist at D2 and 5-HT1A receptors.

                        

                    

                    

                    
                    

                        
                        

                            
Key pharmacokinetic parameters for Aripiprazole: Half-life: 75 hours.

                        

                    

                    

                    

                        
                        

                            
Yes, Aripiprazole is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.

                        

                    

                

            

            

            
            

            
            
            

                
Related Drugs


                
                

                    
Same Drug Class

                    

                        
                        
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                            Escitalopram
                            Small molecule
                        
                        
                    

                

                

                
                
                
            

            

            
            
{# References & Data Sources section for drug detail pages.
   Renders standard pharmacological database links plus the drug's data_sources field. #}


    
References & Data Sources

    
    
        
        
  • 
            
            
                ChEMBL — European Bioinformatics Institute (EBI).
                CHEMBL1112.
                Open-access bioactivity database.
            
        
    • 
        
        
        
  • 
            
            
                PubChem — National Center for Biotechnology Information (NCBI).
                CID 60795.
                Chemical information database.
            
        
    • 
        
        
        
        
    

    
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-04.




        


        
        
    


    



    
医学的免責事項

    

        This content is for educational and informational purposes only. It is not a substitute for professional medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before making medication decisions.
    

    

        Data sources:
        ChEMBL,
        PubChem,
        DailyMed.