GSK-189254 (original) (raw)
GSK-189,254 is a potent and selective H3 histamine receptor inverse agonist developed by GlaxoSmithKline. It has subnanomolar affinity for the H3 receptor (Ki = 0.2nM) and selectivity of over 10,000x for H3 over other histamine receptor subtypes. Animal studies have shown it to possess not only stimulant and nootropic effects, but also analgesic action suggesting a role for H3 receptors in pain processing in the spinal cord. GSK-189,254 and several other related drugs are currently being investigated as a treatment for Alzheimer's disease and other forms of dementia, as well as possible use in the treatment of conditions such as narcolepsy, or neuropathic pain which do not respond well to conventional analgesic drugs.
| Property | Value |
|---|---|
| dbo:abstract | GSK-189,254 is a potent and selective H3 histamine receptor inverse agonist developed by GlaxoSmithKline. It has subnanomolar affinity for the H3 receptor (Ki = 0.2nM) and selectivity of over 10,000x for H3 over other histamine receptor subtypes. Animal studies have shown it to possess not only stimulant and nootropic effects, but also analgesic action suggesting a role for H3 receptors in pain processing in the spinal cord. GSK-189,254 and several other related drugs are currently being investigated as a treatment for Alzheimer's disease and other forms of dementia, as well as possible use in the treatment of conditions such as narcolepsy, or neuropathic pain which do not respond well to conventional analgesic drugs. (en) |
| dbo:casNumber | 720690-73-3 |
| dbo:chEMBL | 517140 |
| dbo:fdaUniiCode | 5T4TX6CO53 |
| dbo:pubchem | 9798547 |
| dbo:thumbnail | wiki-commons:Special:FilePath/GSK-189,254.svg?width=300 |
| dbo:wikiPageID | 19209465 (xsd:integer) |
| dbo:wikiPageLength | 5538 (xsd:nonNegativeInteger) |
| dbo:wikiPageRevisionID | 1102283405 (xsd:integer) |
| dbo:wikiPageWikiLink | dbr:Dementia dbc:GSK_plc_brands dbc:Phenol_ethers dbr:Neuropathic_pain dbr:GlaxoSmithKline dbc:Cyclobutyl_compounds dbr:Stimulant dbc:Benzazepanes dbc:H3_receptor_antagonists dbr:Dissociation_constant dbr:Analgesic dbc:Carboxamides dbc:Nootropics dbr:Alzheimer's_disease dbr:Nootropic dbr:Histamine_H3_receptor dbc:Pyridines dbr:Inverse_agonist dbr:Narcolepsy |
| dbp:c | 21 (xsd:integer) |
| dbp:casNumber | 720690 (xsd:integer) |
| dbp:chembl | 517140 (xsd:integer) |
| dbp:chemspiderid | 7974313 (xsd:integer) |
| dbp:h | 25 (xsd:integer) |
| dbp:iupacName | 6 (xsd:integer) |
| dbp:n | 3 (xsd:integer) |
| dbp:o | 2 (xsd:integer) |
| dbp:pubchem | 9798547 (xsd:integer) |
| dbp:smiles | c4cc1CCNCCc1cc4Ocncc2CNC (en) |
| dbp:stdinchi | 1 (xsd:integer) |
| dbp:stdinchikey | WROHEWWOCPRMIA-UHFFFAOYSA-N (en) |
| dbp:unii | 5 (xsd:integer) |
| dbp:verifiedfields | changed (en) |
| dbp:verifiedrevid | 449551934 (xsd:integer) |
| dbp:watchedfields | changed (en) |
| dbp:width | 240 (xsd:integer) |
| dbp:wikiPageUsesTemplate | dbt:Drugbox dbt:Reflist dbt:Short_description dbt:Cascite dbt:Chemspidercite dbt:Ebicite dbt:Fdacite dbt:Stdinchicite dbt:Histaminergics |
| dct:subject | dbc:GSK_plc_brands dbc:Phenol_ethers dbc:Cyclobutyl_compounds dbc:Benzazepanes dbc:H3_receptor_antagonists dbc:Carboxamides dbc:Nootropics dbc:Pyridines |
| rdf:type | owl:Thing dul:ChemicalObject dbo:ChemicalSubstance wikidata:Q8386 dbo:Drug |
| rdfs:comment | GSK-189,254 is a potent and selective H3 histamine receptor inverse agonist developed by GlaxoSmithKline. It has subnanomolar affinity for the H3 receptor (Ki = 0.2nM) and selectivity of over 10,000x for H3 over other histamine receptor subtypes. Animal studies have shown it to possess not only stimulant and nootropic effects, but also analgesic action suggesting a role for H3 receptors in pain processing in the spinal cord. GSK-189,254 and several other related drugs are currently being investigated as a treatment for Alzheimer's disease and other forms of dementia, as well as possible use in the treatment of conditions such as narcolepsy, or neuropathic pain which do not respond well to conventional analgesic drugs. (en) |
| rdfs:label | GSK-189254 (en) |
| owl:sameAs | wikidata:GSK-189254 dbpedia-sh:GSK-189254 dbpedia-sr:GSK-189254 https://global.dbpedia.org/id/4jcD1 |
| prov:wasDerivedFrom | wikipedia-en:GSK-189254?oldid=1102283405&ns=0 |
| foaf:depiction | wiki-commons:Special:FilePath/GSK-189,254.svg |
| foaf:isPrimaryTopicOf | wikipedia-en:GSK-189254 |
| is dbo:wikiPageRedirects of | dbr:GSK-189,254 dbr:C21H25N3O2 |
| is dbo:wikiPageWikiLink of | dbr:SCHEMBL5334361 dbr:GSK-189,254 dbr:C21H25N3O2 |
| is foaf:primaryTopic of | wikipedia-en:GSK-189254 |
