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Astemizole

CHEMBL296419 Phase 4 Одобрено Small molecule
Half-Life
—
Bioavailability
—
Protein Binding
—
Molecular Weight
458.6 g/mol
LogP
6.0
Phase
4

A second-generation antihistamine that blocks H1 histamine receptors to relieve allergy symptoms without causing significant drowsiness, though it was withdrawn from many markets due to a risk of serious cardiac arrhythmias at high doses.

Молекулярная масса

458,6000 g/mol

LogP

6,00

TPSA

42,30 Ų

Правило пяти Липинского

Соответствует

Механизм действия

Competitively blocks histamine H1 receptors on effector cells, preventing histamine-mediated vasodilation, increased vascular permeability, bronchoconstriction, and pruritus. First-generation agents also cross the blood-brain barrier, causing sedation.

Pharmacokinetics (PK)

Pharmacodynamics (PD)

Механизм

Competitively blocks histamine H1 receptors on effector cells, preventing histamine-mediated vasodilation, increased vascular permeability, bronchoconstriction, and pruritus. First-generation agents also cross the blood-brain barrier, causing sedation.

2D Структура

SVG PNG

Cite this structure


                        

                            
                            
                        

                    

                


                
                

                    

                    

                        
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SMILES

                    
COc1ccc(CCN2CCC(Nc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)cc1

                

                

                
                

                    
InChI

                    
InChI=1S/C28H31FN4O/c1-34-25-12-8-21(9-13-25)14-17-32-18-15-24(16-19-32)30-28-31-26-4-2-3-5-27(26)33(28)20-22-6-10-23(29)11-7-22/h2-13,24H,14-20H2,1H3,(H,30,31)

                

                

                

                    
                    

                        
Molecular Formula

                        
C28H31FN4O

                    

                    
                    

                        
HBD / HBA

                        
1 / 5

                    

                    
                    

                        
Вращаемые Связи

                        
8

                    

                    
                    
                    

                        
Тяжёлые Атомы

                        
34

                    

                    
                

            


            
            

                
                


    
    
        
    
    
    
No targets recorded

    
    
Target interaction data is not yet available for this drug.

    



                
            


            
            

                
                


    
    
        
    
    
    
No interactions recorded

    
    
Drug interaction data is not yet available for this compound.

    



                
            


            
            

                
                


    
    
        
    
    
    
No side effects recorded

    
    
Side effect data is not yet available for this drug.

    



                
            


            
            
            

                
Часто задаваемые вопросы

                

                    
                    

                        
                        

                            
A second-generation antihistamine that blocks H1 histamine receptors to relieve allergy symptoms without causing significant drowsiness, though it was withdrawn from many markets due to a risk of serious cardiac arrhythmias at high doses.

                        

                    

                    

                    

                    
                    

                        
                        

                            
Competitively blocks histamine H1 receptors on effector cells, preventing histamine-mediated vasodilation, increased vascular permeability, bronchoconstriction, and pruritus. First-generation agents also cross the blood-brain barrier, causing sedation.

                        

                    

                    

                    

                    

                        
                        

                            
Yes, Astemizole is an approved drug. It has reached clinical phase 4. It is classified as a 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).
                CHEMBL296419.
                Open-access bioactivity database.
            
        
    • 
        
        
        
  • 
            
            
                PubChem — National Center for Biotechnology Information (NCBI).
                CID 2247.
                Chemical information database.
            
        
    • 
        
        
        
        
    

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




        


        
        
    


    



    
Медицинский отказ от ответственности

    

        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.