diprenorphine
Sign in to saveAlso known as Diprenorfin
Diprenorphine (brand name Revivon; former developmental code name M5050), also known as diprenorfin, is a non-selective, high-affinity, weak partial agonist of the μ- (MOR), κ- (KOR), and δ-opioid receptor (DOR) (with equal affinity) which is used in veterinary medicine as an opioid antagonist. It is used to reverse the effects of super-potent opioid analgesics such as etorphine and carfentanil that are used for tranquilizing large animals. The drug is not approved for use in humans.
Research
765 papers- [6-O-methyl-(11)C]Diprenorphine.2004
- Influence of pediatric vaccines on amygdala growth and opioid ligand binding in rhesus macaque infants: A pilot study.Acta neurobiologiae experimentalis · 2010
- Delta Opioid Receptor-Mediated Antidepressant-Like Effects of Diprenorphine in Mice.The Journal of pharmacology and experimental therapeutics · 2023
- 6-O-(2-[(18)F]Fluoroethyl)-6-O-Desmethyl-Diprenorphine ([(18)F]FE-DPN) Preferentially Binds to Mu Opioid Receptors In Vivo.Molecular imaging and biology · 2023
- Diprenorphine as a stimulus in drug discrimination learning.Pharmacology, biochemistry, and behavior · 1992
via PubMed
Wikidata facts
- Mass
- 425.256609
Show 3 more facts
- chemical formula
- C₂₆H₃₅NO₄
- canonical SMILES
- CC(C)(C1CC23CCC1(C4C25CCN(C3CC6=C5C(=C(C=C6)O)O4)CC7CC7)OC)O
- isomeric SMILES
- CC(C)([C@H]1C[C@@]23CC[C@@]1([C@H]4[C@@]25CCN([C@@H]3CC6=C5C(=C(C=C6)O)O4)CC7CC7)OC)O
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Article
1 sectionsContents
- References
Diprenorphine (brand name Revivon; former developmental code name M5050), also known as diprenorfin, is a non-selective, high-affinity, weak partial agonist of the μ- (MOR), κ- (KOR), and δ-opioid receptor (DOR) (with equal affinity) which is used in veterinary medicine as an opioid antagonist. It is used to reverse the effects of super-potent opioid analgesics such as etorphine and carfentanil that are used for tranquilizing large animals. The drug is not approved for use in humans.
Diprenorphine is the strongest opioid antagonist that is commercially available (some 100 times more potent than nalorphine), and is used for reversing the effects of very strong opioids for which the binding affinity is so high that naloxone does not effectively or reliably reverse the narcotic effects. These super-potent opioids, with the single exception of buprenorphine (which has an improved safety-profile due to its partial agonism character), are not used in humans because the dose for a human is so small that it would be difficult to measure properly , so there is an excessive risk of overdose leading to fatal respiratory depression. However conventional opioid derivatives are not strong enough to rapidly tranquilize large animals, like elephants and rhinos, so drugs such as etorphine and carfentanil are available for this purpose.