Levallorphan

CHEMBL1254682 Phase 4 Approved Small molecule

Half-Life

—

Bioavailability

—

Protein Binding

—

Molecular Weight

283.4 g/mol

LogP

3.5

Phase

4

This opioid antagonist reverses the effects of opioid medications, particularly respiratory depression caused by opioid overdose. It was historically used to counteract narcotic-induced breathing problems but has largely been replaced by more selective agents.

Molecular Weight

283.4000 g/mol

LogP

3.50

TPSA

23.50 Å²

Lipinski RO5

Pass

Mechanism of Action

Binds to mu (μ), kappa (κ), and/or delta (δ) opioid receptors in the central and peripheral nervous system, mimicking endogenous endorphins. Activation of these G-protein-coupled receptors inhibits pain signal transmission and modulates the emotional response to pain.

Pharmacokinetics (PK)

Pharmacodynamics (PD)

Mechanism

Binds to mu (μ), kappa (κ), and/or delta (δ) opioid receptors in the central and peripheral nervous system, mimicking endogenous endorphins. Activation of these G-protein-coupled receptors inhibits pain signal transmission …

2D Structure

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SMILES

C=CCN1CC[C@]23CCCC[C@H]2[C@H]1Cc1ccc(O)cc13

InChI

InChI=1S/C19H25NO/c1-2-10-20-11-9-19-8-4-3-5-16(19)18(20)12-14-6-7-15(21)13-17(14)19/h2,6-7,13,16,18,21H,1,3-5,8-12H2/t16-,18+,19+/m0/s1

Molecular Formula

C19H25NO

HBD / HBA

1 / 2

Rotatable Bonds

2

Heavy Atoms

21

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

This opioid antagonist reverses the effects of opioid medications, particularly respiratory depression caused by opioid overdose. It was historically used to counteract narcotic-induced breathing problems but has largely been replaced by more selective agents.

Binds to mu (μ), kappa (κ), and/or delta (δ) opioid receptors in the central and peripheral nervous system, mimicking endogenous endorphins. Activation of these G-protein-coupled receptors inhibits pain signal transmission and modulates the emotional response to pain.

Yes, Levallorphan 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). CHEMBL1254682. Open-access bioactivity database.
PubChem — National Center for Biotechnology Information (NCBI). CID 5359371. Chemical information database.

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

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Structure

Quick Data

Formula: C19H25NO

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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.