Bitolterol

CHEMBL1201295 Phase 4 Approved Small molecule
Half-Life
Bioavailability
Protein Binding
Molecular Weight
461.5 g/mol
LogP
5.2
Phase
4

A beta-2 adrenergic agonist bronchodilator that was used to treat and prevent bronchospasm in asthma and chronic obstructive pulmonary disease. It is a prodrug that is converted to the active compound colterol in the body. It was withdrawn from the market and replaced by other bronchodilators.

Molecular Weight

461.5000 g/mol

LogP

5.20

TPSA

84.90 Ų

Lipinski RO5

Pass

Mechanism of Action

Activates beta-2 adrenergic receptors on bronchial smooth muscle, stimulating adenylyl cyclase and increasing intracellular cAMP. This relaxes airway smooth muscle and produces bronchodilation.

Pharmacokinetics (PK)

Pharmacodynamics (PD)

Mechanism

Activates beta-2 adrenergic receptors on bronchial smooth muscle, stimulating adenylyl cyclase and increasing intracellular cAMP. This relaxes airway smooth muscle and produces bronchodilation.

2D Structure

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SMILES

Cc1ccc(C(=O)Oc2ccc(C(O)CNC(C)(C)C)cc2OC(=O)c2ccc(C)cc2)cc1

InChI

InChI=1S/C28H31NO5/c1-18-6-10-20(11-7-18)26(31)33-24-15-14-22(23(30)17-29-28(3,4)5)16-25(24)34-27(32)21-12-8-19(2)9-13-21/h6-16,23,29-30H,17H2,1-5H3

Molecular Formula

C28H31NO5

HBD / HBA

2 / 6

Rotatable Bonds

10

Heavy Atoms

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.

Frequently Asked Questions

A beta-2 adrenergic agonist bronchodilator that was used to treat and prevent bronchospasm in asthma and chronic obstructive pulmonary disease. It is a prodrug that is converted to the active compound colterol in the body. It was withdrawn from the market and replaced by other bronchodilators.

Activates beta-2 adrenergic receptors on bronchial smooth muscle, stimulating adenylyl cyclase and increasing intracellular cAMP. This relaxes airway smooth muscle and produces bronchodilation.

Yes, Bitolterol 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). CHEMBL1201295. Open-access bioactivity database.
  • PubChem — National Center for Biotechnology Information (NCBI). CID 35330. Chemical information database.

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

Medical Disclaimer

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.