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Statements

Subject Item
dbr:Oxilorphan
rdf:type
umbel-rc:DrugProduct yago:Relation100031921 dbo:ChemicalSubstance yago:Abstraction100002137 yago:WikicatAlcohols yago:Alcohol107884567 n14:ChemicalObject yago:Substance100019613 yago:Substance100020090 yago:Matter100020827 yago:Agent114778436 wikidata:Q8386 yago:OrganicCompound114727670 yago:DrugOfAbuse103248958 yago:PhysicalEntity100001930 yago:Drug103247620 yago:Chemical114806838 yago:Beverage107881800 yago:CausalAgent100007347 yago:WikicatPhenols yago:Fluid114939900 yago:Liquid114940386 yago:Material114580897 owl:Thing yago:Phenol114989545 yago:Part113809207 dbo:Drug yago:Compound114818238 yago:Food100021265
rdfs:label
Oxilorphan
rdfs:comment
Oxilorphan (INN, USAN) (developmental code name L-BC-2605) is an opioid antagonist of the morphinan family that was never marketed. It acts as a μ-opioid receptor (MOR) antagonist but a κ-opioid receptor (KOR) partial agonist, and has similar effects to naloxone and around the same potency as an MOR antagonist. Oxilorphan has some weak partial agonist actions at the MOR (with miosis, nausea, dizziness, and some euphoria observed) and can produce hallucinogenic/dissociative effects at sufficient doses, indicative of KOR activation. It was trialed for the treatment of opioid addiction, but was not developed commercially. The KOR agonist effects of oxilorphan are associated with dysphoria, which combined with its hallucinogenic effects, serve to limit its clinical usefulness; indeed, many pat
foaf:depiction
n8:Oxilorphan.svg
dcterms:subject
dbc:Phenols dbc:Morphinans dbc:Analgesics dbc:Synthetic_opioids dbc:Mu-opioid_receptor_antagonists dbc:Antidotes dbc:Kappa-opioid_receptor_agonists dbc:Dissociative_drugs dbc:Mu-opioid_receptor_agonists dbc:Tertiary_alcohols
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dbo:wikiPageRevisionID
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dbo:wikiPageWikiLink
dbr:Levomethorphan dbc:Phenols dbc:Morphinans dbr:Morphinan dbr:Dissociative dbc:Analgesics dbc:Synthetic_opioids dbr:Kappa_opioid_receptor dbr:Miosis dbc:Mu-opioid_receptor_antagonists dbr:Proxorphan dbr:Ketorfanol dbr:Dysphoria dbr:Butorphanol dbr:Dizziness dbc:Antidotes dbr:Mu_opioid_receptor dbr:Xorphanol dbr:Nausea dbr:Euphoria dbr:Opioid_antagonist dbr:International_Nonproprietary_Name dbc:Kappa-opioid_receptor_agonists dbc:Dissociative_drugs dbr:Levallorphan dbr:United_States_Adopted_Name dbc:Mu-opioid_receptor_agonists dbr:Cyclorphan dbr:Partial_agonist dbr:Receptor_antagonist dbr:Levorphanol dbr:Opioid_addiction dbr:Naloxone dbr:Nalbuphine dbr:Hallucinogen dbc:Tertiary_alcohols
owl:sameAs
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dbo:thumbnail
n8:Oxilorphan.svg?width=300
dbp:atcPrefix
None
dbp:c
20
dbp:casNumber
42281
dbp:chemspiderid
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dbp:h
27
dbp:iupacName
-17
dbp:kegg
D05299
dbp:n
1
dbp:o
2
dbp:pubchem
5361090
dbp:smiles
Oc3ccc4C[C@H]1NCC5CC5
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1
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140
dbo:abstract
Oxilorphan (INN, USAN) (developmental code name L-BC-2605) is an opioid antagonist of the morphinan family that was never marketed. It acts as a μ-opioid receptor (MOR) antagonist but a κ-opioid receptor (KOR) partial agonist, and has similar effects to naloxone and around the same potency as an MOR antagonist. Oxilorphan has some weak partial agonist actions at the MOR (with miosis, nausea, dizziness, and some euphoria observed) and can produce hallucinogenic/dissociative effects at sufficient doses, indicative of KOR activation. It was trialed for the treatment of opioid addiction, but was not developed commercially. The KOR agonist effects of oxilorphan are associated with dysphoria, which combined with its hallucinogenic effects, serve to limit its clinical usefulness; indeed, many patients who experienced these side effects refused to take additional doses in clinical trials.
gold:hypernym
dbr:Antagonist
prov:wasDerivedFrom
wikipedia-en:Oxilorphan?oldid=1051579244&ns=0
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5130
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42281-59-4
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dbo:kegg
D05299
dbo:pubchem
5361090
foaf:isPrimaryTopicOf
wikipedia-en:Oxilorphan