Butorphanol is an opioid agonist-antagonist used to treat moderate to severe pain. A synthetic morphinan analgesic with narcotic antagonist action.
- Mechanism
- Curator reviewed
The exact mechanism of action is unknown, but is believed to interact with an opiate receptor site in the CNS (probably in or associated with the limbic system). The opiate antagonistic effect may result from competitive inhibition at the opiate receptor, but may also be a result of other mechanisms. Butorphanol is believed to have both partial agonism and partial antagonism at the μ-opioid receptor, as well as partial agonist and antagonist activity at the κ-opioid receptor.
- Primary indication
- For the relief of moderate to severe pain.Curator reviewed · 3 structured indications
- Formula / weight
- C21H29NO2 · 327.4605 g/mol (avg)
- First approval
- Canada, 2001 · United States, 1996
- Code names
- BC-2627 · LEVO-BC-2627
- Brand names
Resolves to
IFKLAQQSCNILHL-QHAWAJNXSA-NSMILES[H][C@@]12CC3=C(C=C(O)C=C3)[C@]3(CCCC[C@@]13O)CCN2CC1CCC1What you can answer from here — as of September 23, 2026
Which drugs share a target with Butorphanol, and which of those have an active Phase 3 trial?
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