Levallorphan

DB00504ApprovedSmall molecule

An opioid antagonist with properties similar to those of naloxone; in addition it also possesses some agonist properties. It should be used cautiously; levallorphan reverses severe opioid-induced respiratory depression but... (From Martindale, The Extra Pharmacopoeia, 30th ed, p683).

Mechanism: Levallorphan antagonizes opioid effects by competing for the same receptor sites. It binds to the opioid mu receptor and the nicotinic acetylcholine receptor alpha2/alpha3.
Curator reviewed
Primary indication: For the complete or partial reversal of narcotic depression, including respiratory depression, induced by opioids.Curator reviewed
Formula / weight: C₁₉H₂₅NO · 283.4079 g/mol (avg)
Code names: HSDB 2148 · Ro-1-7700

Resolves to

Compound

UNII353613BU4UCAS152-02-3ChEMBLCHEMBL1254682ChEBI6431PubChem5359371KEGGC07069

Clinical / RWD

RxNorm6370PharmGKBPA164749284

Structure

InChIKeyOZYUPQUCAUTOBP-QXAKKESOSA-NSMILES[H][C@@]12CCCC[C@@]11CCN(CC=C)[C@@H]2CC2=C1C=C(O)C=C2

Targets

P41145OPRK1P35372OPRM1Q15822CHRNA2

What you can answer from here — as of September 12, 2026

3Protein targetsEach mapped to UniProt, with action and pharmacological action

Listed above

54Drug interactionsStructured to mechanism, not free text

10+ReferencesStructured and connected to the statements they support

Which drugs share a target with Levallorphan, and which of those have an active Phase 3 trial?

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