| dbo:abstract |
Xanomeline (LY-246,708; Lumeron, Memcor) is a small molecule muscarinic acetylcholine receptor agonist that was first synthesized in a collaboration between Eli Lilly and Novo Nordisk as an investigational therapeutic being studied for the treatment of central nervous system disorders. Its pharmacological action is mediated primarily through stimulation of central nervous system muscarinic M1 and M4 receptor subtypes. Xanomeline is currently being developed as a combination drug (Kar-XT; xanomeline + trospium) by Karuna Therapeutics. Trospium is a non-CNS penetrant non-selective muscarinic antagonist to quell peripheral muscarinic agonist-dependent side effects. Xanomeline’s mechanism of action is hypothesized to be via rebalancing key neurotransmitter circuits, including acetylcholine, dopamine, and glutamate, which are disrupted in schizophrenia and related diseases. (en) キサノメリン(Xanomeline)は、M1及びM4に選択性があるが、M5にも活性があることが知られているムスカリン性アセチルコリン受容体のアゴニストである。胃腸への副作用はあるものの、アルツハイマー病と統合失調症の両方、特に認知と陰性症状の両方について研究が行われているが、臨床的な副作用により中断率が高くなっている。これを除けば、キサノメリンは統合失調症の症状に効果をある程度効果を示す。また、ヒトにおいて、学習やワーキングメモリを改善する効果が示されている。 (ja) |
| dbo:casNumber |
131986-45-3 |
| dbo:chEMBL |
21536 |
| dbo:fdaUniiCode |
9ORI6L73CJ |
| dbo:kegg |
D06330 |
| dbo:pubchem |
60809 |
| dbo:thumbnail |
wiki-commons:Special:FilePath/Xanomeline.png?width=300 |
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| dbo:wikiPageWikiLink |
dbr:Schizophrenia dbr:Hydrogen_bond dbr:Betel dbr:Vedaclidine dbr:Neurotransmitter dbc:Tetrahydropyridines dbr:Sabcomeline dbr:Eli_Lilly dbr:Muscarinic_acetylcholine_receptor dbr:Muscarinic_acetylcholine_receptor_M1 dbr:Muscarinic_acetylcholine_receptor_M4 dbc:Muscarinic_agonists dbr:Acetylcholine dbr:Alvameline dbr:Novo_Nordisk dbr:Central_nervous_system dbr:KarXT dbr:Tazomeline dbr:Arecoline dbc:Thiadiazoles dbr:Dopamine dbr:Milameline dbr:Glutamate dbr:Trospium |
| dbp:atcPrefix |
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14 (xsd:integer) |
| dbp:casNumber |
131986 (xsd:integer) |
| dbp:chembl |
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| dbp:s |
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| dbp:smiles |
CCCCCCOC1=NSN=C1C2=CCCNC (en) |
| dbp:unii |
9 (xsd:integer) |
| dbp:wikiPageUsesTemplate |
dbt:Cite_journal dbt:Drugbox dbt:Reflist dbt:Short_description dbt:Fdacite dbt:Muscarinic_acetylcholine_receptor_modulators dbt:Anti-dementia_drugs |
| dcterms:subject |
dbc:Tetrahydropyridines dbc:Muscarinic_agonists dbc:Thiadiazoles |
| gold:hypernym |
dbr:Agonist |
| rdf:type |
owl:Thing dul:ChemicalObject dbo:ChemicalSubstance wikidata:Q8386 yago:WikicatMolecularFormulas yago:Abstraction100002137 yago:Base114618253 yago:Chemical114806838 yago:Communication100033020 yago:Compound114818238 yago:Formula106816935 yago:Material114580897 yago:Matter100020827 yago:Message106598915 yago:MolecularFormula106817173 yago:Part113809207 yago:PhysicalEntity100001930 yago:Pyridine114692510 yago:Relation100031921 dbo:Drug yago:Statement106722453 yago:Substance100019613 yago:WikicatPyridines umbel-rc:DrugProduct |
| rdfs:comment |
キサノメリン(Xanomeline)は、M1及びM4に選択性があるが、M5にも活性があることが知られているムスカリン性アセチルコリン受容体のアゴニストである。胃腸への副作用はあるものの、アルツハイマー病と統合失調症の両方、特に認知と陰性症状の両方について研究が行われているが、臨床的な副作用により中断率が高くなっている。これを除けば、キサノメリンは統合失調症の症状に効果をある程度効果を示す。また、ヒトにおいて、学習やワーキングメモリを改善する効果が示されている。 (ja) Xanomeline (LY-246,708; Lumeron, Memcor) is a small molecule muscarinic acetylcholine receptor agonist that was first synthesized in a collaboration between Eli Lilly and Novo Nordisk as an investigational therapeutic being studied for the treatment of central nervous system disorders. (en) |
| rdfs:label |
キサノメリン (ja) Xanomeline (en) |
| owl:sameAs |
freebase:Xanomeline yago-res:Xanomeline wikidata:Xanomeline dbpedia-fa:Xanomeline dbpedia-ja:Xanomeline dbpedia-sh:Xanomeline dbpedia-sr:Xanomeline https://global.dbpedia.org/id/4xD6J |
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wikipedia-en:Xanomeline?oldid=1120577679&ns=0 |
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wiki-commons:Special:FilePath/Xanomeline.png |
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wikipedia-en:Xanomeline |
| is dbo:wikiPageRedirects of |
dbr:C14H23N3OS dbr:LY-246,708 dbr:LY-246708 dbr:LY246,708 dbr:LY246708 dbr:Lumeron dbr:Memcor |
| is dbo:wikiPageWikiLink of |
dbr:List_of_investigational_antipsychotics dbr:Sabcomeline dbr:Muscarinic_acetylcholine_receptor_M1 dbr:Muscarinic_acetylcholine_receptor_M5 dbr:Muscarinic_agonist dbr:C14H23N3OS dbr:Alvameline dbr:KarXT dbr:Tazomeline dbr:Acetylcholine_receptor dbr:Milameline dbr:Flavin-containing_monooxygenase dbr:Flavin-containing_monooxygenase_3 dbr:List_of_drugs:_X dbr:LY-246,708 dbr:LY-246708 dbr:LY246,708 dbr:LY246708 dbr:Lumeron dbr:Memcor |
| is foaf:primaryTopic of |
wikipedia-en:Xanomeline |
