Tolazoline

CHEMBL770 Phase 4 Aprovado 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.

Peso Molecular

160,2200 g/mol

LogP

2,60

TPSA

24,40 Å²

Regra dos 5 de Lipinski

Aprovado

Áreas Terapêuticas

Hypertension

Mecanismo de Ação

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)

Mecanismo

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 …

Estrutura 2D

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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

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.

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.

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

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Estrutura

Dados Rápidos

Fórmula: C10H12N2
Sinônimos: 1

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Aviso Médico

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.