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Tolazoline

CHEMBL770 Phase 4 Zugelassen Small molecule
Half-Life
—
Bioavailability
—
Protein Binding
—
Molecular Weight
160.2 g/mol
LogP
2.6
Phase
4

Tolazoline is a competitive alpha-adrenergic receptor antagonist with additional direct vasodilatory, histamine H1 agonist, and acetylcholine-mimetic effects that cause vasodilation of pulmonary and systemic vasculature, used historically for persistent pulmonary hypertension of the newborn (PPHN) to reduce pulmonary vascular resistance. It also stimulates gastric acid secretion through histaminergic mechanisms. Its use has been largely replaced by inhaled nitric oxide due to the latter's greater selectivity for the pulmonary vasculature and more favorable adverse effect profile.

Molekularmasse

160,2200 g/mol

LogP

2,60

TPSA

24,40 Ų

Lipinski-Regel der Fünf

Bestanden

Wirkmechanismus

Competitively binds to its target receptor without activating it, blocking the natural ligand from binding and preventing receptor-mediated signaling.

Pharmacokinetics (PK)

Pharmacodynamics (PD)

Mechanismus

Competitively binds to its target receptor without activating it, blocking the natural ligand from binding and preventing receptor-mediated signaling.

2D-Struktur

SVG PNG

Cite this structure


                        

                            
                            
                        

                    

                


                
                

                    

                    

                        
Embed this structure

                        

                        

                            
                            
                        

                    

                

                

                
                

                    
SMILES

                    
c1ccc(CC2=NCCN2)cc1

                

                

                
                

                    
InChI

                    
InChI=1S/C10H12N2/c1-2-4-9(5-3-1)8-10-11-6-7-12-10/h1-5H,6-8H2,(H,11,12)

                

                

                

                    
                    

                        
Molecular Formula

                        
C10H12N2

                    

                    
                    

                        
HBD / HBA

                        
1 / 1

                    

                    
                    

                        
Rotierbare Bindungen

                        
2

                    

                    
                    
                    

                        
Schwere Atome

                        
12

                    

                    
                

            


            
            

                
                


    
    
        
    
    
    
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.

    



                
            


            
            
            

                
Häufig gestellte Fragen

                

                    
                    

                        
                        

                            
Tolazoline is a competitive alpha-adrenergic receptor antagonist with additional direct vasodilatory, histamine H1 agonist, and acetylcholine-mimetic effects that cause vasodilation of pulmonary and systemic vasculature, used historically for persistent pulmonary hypertension of the newborn (PPHN) to reduce pulmonary vascular resistance. It also stimulates gastric acid secretion through histaminergic mechanisms. Its use has been largely replaced by inhaled nitric oxide due to the latter's greater selectivity for the pulmonary vasculature and more favorable adverse effect profile.

                        

                    

                    

                    

                    
                    

                        
                        

                            
Competitively binds to its target receptor without activating it, blocking the natural ligand from binding and preventing receptor-mediated signaling.

                        

                    

                    

                    

                    

                        
                        

                            
Yes, Tolazoline 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).
                CHEMBL770.
                Open-access bioactivity database.
            
        
    • 
        
        
        
  • 
            
            
                PubChem — National Center for Biotechnology Information (NCBI).
                CID 5504.
                Chemical information database.
            
        
    • 
        
        
        
        
    

    
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-28.




        


        
        
    


    



    
Medizinischer Haftungsausschluss

    

        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.