Tolazoline
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.
Peso Molecular
160,2200 g/mol
LogP
2,60
TPSA
24,40 Ų
Regra dos 5 de Lipinski
Aprovado
Mecanismo de Ação
Competitively binds to its target receptor without activating it, blocking the natural ligand from binding and preventing receptor-mediated signaling.
Pharmacokinetics (PK)
Pharmacodynamics (PD)
Competitively binds to its target receptor without activating it, blocking the natural ligand from binding and preventing receptor-mediated signaling.
Estrutura 2D
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
Ligações Rotacionáveis
2
Átomos Pesados
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.
Perguntas frequentes
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
- 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.
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