Repositioning Candidate Details
| Candidate ID: | R0242 |
| Source ID: | DB00844 |
| Source Type: | approved |
| Compound Type: | small molecule |
| Compound Name: | Nalbuphine |
| Synonyms: | |
| Molecular Formula: | C21H27NO4 |
| SMILES: | O[C@H]1CC[C@@]2(O)[C@H]3CC4=CC=C(O)C5=C4[C@@]2(CCN3CC2CCC2)[C@H]1O5 |
| Structure: |
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| DrugBank Description: | A narcotic used as a pain medication. It appears to be an agonist at kappa opioid receptors and an antagonist or partial agonist at mu opioid receptors. Nalbuphine is the only opioid analgesic that is not a controlled substance in the United States. |
| CAS Number: | 20594-83-6 |
| Molecular Weight: | 357.4434 |
| DrugBank Indication: | For the relief of moderate to severe pain. |
| DrugBank Pharmacology: | Nalbuphine is a synthetic opioid agonist-antagonist analgesic of the phenanthrene series. Nalbuphine's analgesic potency is essentially equivalent to that of [morphine] on a milligram basis. The opoioid antagonist activity of nalbuphine is about one-fourth to that of [nalorphine] and 10 times to that of [pentazocine]. Nalbuphine by itself has potent opioid antagonist activity at doses equal to or lower than its analgesic dose. When administered following or concurrent with mu agonist opioid analgesics (e.g., morphine, oxymorphone, fentanyl), nalbuphine may partially reverse or block opioid-induced respiratory depression from the mu agonist analgesic. Nalbuphine may precipitate withdrawal in patients dependent on opioid drugs. Nalbuphine should be used with caution in patients who have been receiving mu opioid analgesics on a regular basis. |
| DrugBank MoA: | 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. Nalbuphine is thought primarily to be a kappa agonist. It is also a partial mu antagonist analgesic, with some binding to the delta receptor and minimal agonist activity at the sigma receptor. |
| Targets: | Kappa-type opioid receptor; Mu-type opioid receptor; Delta-type opioid receptor |
| Inclusion Criteria: |
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