SB-205384 (original) (raw)

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SB-205384 is an anxiolytic drug. It has similar effects to benzodiazepine drugs, but is structurally distinct and so is classed as a nonbenzodiazepine anxiolytic. SB-205384 is a GABAA positive allosteric modulator, which binds preferentially to α3, α5, and α6 subunit containing subtypes. It has a novel mechanism of action, prolonging the duration of GABA-mediated chloride flux but without increasing the intensity of the response, and this may give it an unusual pharmacological profile, with tests showing that it alters the firing of some populations of neurons while leaving others unaffected. Animal studies have shown it to produce both anxiolytic and anti-aggressive effects, but with little sedation or other behavioural changes.

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dbo:abstract SB-205384 is an anxiolytic drug. It has similar effects to benzodiazepine drugs, but is structurally distinct and so is classed as a nonbenzodiazepine anxiolytic. SB-205384 is a GABAA positive allosteric modulator, which binds preferentially to α3, α5, and α6 subunit containing subtypes. It has a novel mechanism of action, prolonging the duration of GABA-mediated chloride flux but without increasing the intensity of the response, and this may give it an unusual pharmacological profile, with tests showing that it alters the firing of some populations of neurons while leaving others unaffected. Animal studies have shown it to produce both anxiolytic and anti-aggressive effects, but with little sedation or other behavioural changes. (en)
dbo:casNumber 160296-13-9
dbo:pubchem 197690
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dbo:wikiPageWikiLink dbr:Benzodiazepine dbc:Alkyne_derivatives dbc:Carboxylate_esters dbc:GABAA_receptor_positive_allosteric_modulators dbc:Secondary_alcohols dbr:Anxiolytic dbr:Positive_allosteric_modulator dbr:GABAA_receptor dbc:Anxiolytics dbr:Nonbenzodiazepine
dbp:c 17 (xsd:integer)
dbp:casNumber 160296 (xsd:integer)
dbp:chemspiderid 171116 (xsd:integer)
dbp:h 18 (xsd:integer)
dbp:iupacName But-2-ynyl 4-amino-7-hydroxy-2-methyl-5,6,7,8-tetrahydro-[1]benzothiolo[3,2-e]pyridine-3-carboxylate (en)
dbp:legalUs Investigational New Drug (en)
dbp:n 2 (xsd:integer)
dbp:o 3 (xsd:integer)
dbp:pubchem 197690 (xsd:integer)
dbp:s 1 (xsd:integer)
dbp:smiles CC#CCOCc1cnc2sc3CCCCc3c2c1N (en)
dbp:stdinchi 1 (xsd:integer)
dbp:stdinchikey JDTZAGLGBRRCJT-UHFFFAOYSA-N (en)
dbp:verifiedfields changed (en)
dbp:verifiedrevid 399126895 (xsd:integer)
dbp:watchedfields changed (en)
dbp:width 250 (xsd:integer)
dbp:wikiPageUsesTemplate dbt:Drugbox dbt:GABAAR_PAMs dbt:Reflist dbt:Cascite dbt:Chemspidercite dbt:Drugbankcite dbt:Stdinchicite dbt:Anxiolytics dbt:Anxiolytic-stub
dct:subject dbc:Alkyne_derivatives dbc:Carboxylate_esters dbc:GABAA_receptor_positive_allosteric_modulators dbc:Secondary_alcohols dbc:Anxiolytics
rdf:type owl:Thing dul:ChemicalObject dbo:ChemicalSubstance wikidata:Q8386 dbo:Drug
rdfs:comment SB-205384 is an anxiolytic drug. It has similar effects to benzodiazepine drugs, but is structurally distinct and so is classed as a nonbenzodiazepine anxiolytic. SB-205384 is a GABAA positive allosteric modulator, which binds preferentially to α3, α5, and α6 subunit containing subtypes. It has a novel mechanism of action, prolonging the duration of GABA-mediated chloride flux but without increasing the intensity of the response, and this may give it an unusual pharmacological profile, with tests showing that it alters the firing of some populations of neurons while leaving others unaffected. Animal studies have shown it to produce both anxiolytic and anti-aggressive effects, but with little sedation or other behavioural changes. (en)
rdfs:label SB-205384 (en)
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