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Tolazoline

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

Several vasodilator mechanisms operate together in tolazoline: competitive alpha-adrenergic receptor antagonism, direct vasodilator activity, histamine H1 agonism and acetylcholine-mimetic effects. The combined result is dilation of both pulmonary and systemic vessels, and the agent was used historically in persistent pulmonary hypertension of the newborn to lower pulmonary vascular resistance. Its histaminergic activity also stimulates gastric acid secretion, an effect unrelated to the intended indication. Inhaled nitric oxide has largely replaced it, being selective for the pulmonary circulation and better tolerated, whereas tolazoline acts on the systemic vasculature as well. The molecule is small, C10H12N2 at about 160.2 g/mol, with development through the final clinical phase.

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.

Khối lượng phân tử

160,2200 g/mol

LogP

2,60

TPSA

24,40 Ų

Lipinski RO5

Đạt

Lĩnh vực điều trị

Hypertension

Cơ chế tác dụng

A competitive, non-selective alpha-adrenergic receptor antagonist that also relaxes vascular smooth muscle directly and has histamine H1 agonist and cholinomimetic activity. Alpha blockade together with direct vasodilation lowers pulmonary and systemic vascular resistance.

Pharmacokinetics (PK)

Pharmacodynamics (PD)

Cơ chế

A competitive, non-selective alpha-adrenergic receptor antagonist that also relaxes vascular smooth muscle directly and has histamine H1 agonist and cholinomimetic activity. Alpha blockade together with direct vasodilation lowers pulmonary and …

Cấu trúc 2D

SVG PNG

Cite this structure


                        

                            
                            
                        

                    

                


                
                

                    

                    

                        
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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

                    

                    
                    

                        
Liên kết có thể quay

                        
2

                    

                    
                    
                    

                        
Nguyên tử nặng

                        
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.

    



                
            


            
            
            

                
Câu hỏi thường gặp

                

                    
                    

                        
                        

                            
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.

                        

                    

                    

                    

                    
                    

                        
                        

                            
A competitive, non-selective alpha-adrenergic receptor antagonist that also relaxes vascular smooth muscle directly and has histamine H1 agonist and cholinomimetic activity. Alpha blockade together with direct vasodilation lowers pulmonary and systemic vascular resistance.

                        

                    

                    

                    

                    

                        
                        

                            
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.
            
        
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Data aggregated from publicly available pharmacological databases. Last updated 2026-08-20.




        


        
        
    


    



    
Tuyên bố miễn trách y tế

    

        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.