BD1008 (original) (raw)
BD1008 or N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-1-pyrrolidineethanamine is a selective sigma receptor antagonist, with a reported binding affinity of Ki = 2 ± 1 nM for the sigma-1 receptor and 4 times selectivity over the sigma-2 receptor. Consistent with other reported sigma receptor antagonists, pretreating Swiss Webster mice with BD1008 significantly attenuates the behavioral toxicity of cocaine, and may be potentially useful in the development of antidotes for the treatment of cocaine overdose.
| Property | Value |
|---|---|
| dbo:abstract | BD1008 or N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-1-pyrrolidineethanamine is a selective sigma receptor antagonist, with a reported binding affinity of Ki = 2 ± 1 nM for the sigma-1 receptor and 4 times selectivity over the sigma-2 receptor. Consistent with other reported sigma receptor antagonists, pretreating Swiss Webster mice with BD1008 significantly attenuates the behavioral toxicity of cocaine, and may be potentially useful in the development of antidotes for the treatment of cocaine overdose. (en) BD1008 o N-[2-(3,4-dichlorophenyl)etilo]-N-metilo-1-pyrrolidineethanamine es un antagonista selectivo del receptor sigma, con una afinidad de unión informada de Ki = 2 ± 1 nM por el receptor sigma-1 y 4 veces la selectividad sobre el receptor sigma-2. De acuerdo con otros antagonistas del receptor sigma informados, el pretratamiento de ratones Swiss Webster con BD1008 atenúa significativamente la toxicidad conductual de la cocaína y puede ser potencialmente útil en el desarrollo de antídotos para el tratamiento de la sobredosis de cocaína. (es) |
| dbo:casNumber | 138356-08-8 |
| dbo:fdaUniiCode | JCY43QE7FQ |
| dbo:pubchem | 126388 |
| dbo:thumbnail | wiki-commons:Special:FilePath/BD1008.png?width=300 |
| dbo:wikiPageID | 36175312 (xsd:integer) |
| dbo:wikiPageLength | 3680 (xsd:nonNegativeInteger) |
| dbo:wikiPageRevisionID | 1108866124 (xsd:integer) |
| dbo:wikiPageWikiLink | dbr:Antagonist dbr:Binding_affinity dbc:Chloroarenes dbc:Pyrrolidines dbr:LR132 dbr:BD1031 dbr:Sigma_receptor dbr:Sigma-2_receptor dbr:Sigma-1_receptor |
| dbp:c | 15 (xsd:integer) |
| dbp:casNumber | 138356 (xsd:integer) |
| dbp:chemspiderid | 112324 (xsd:integer) |
| dbp:cl | 2 (xsd:integer) |
| dbp:h | 22 (xsd:integer) |
| dbp:iupacName | N-[2-ethyl]-N-methyl-1-pyrrolidineethanamine (en) |
| dbp:n | 2 (xsd:integer) |
| dbp:pubchem | 126388 (xsd:integer) |
| dbp:smiles | CNCCN2CCCC2 (en) |
| dbp:stdinchi | 1 (xsd:integer) |
| dbp:stdinchikey | ASGIQUHBAVIOTI-UHFFFAOYSA-N (en) |
| dbp:unii | JCY43QE7FQ (en) |
| dbp:wikiPageUsesTemplate | dbt:Drugbox dbt:Reflist dbt:Cascite dbt:Fdacite dbt:Sigma_receptor_modulators |
| dcterms:subject | dbc:Chloroarenes dbc:Pyrrolidines |
| gold:hypernym | dbr:Antagonist |
| rdf:type | owl:Thing dul:ChemicalObject dbo:ChemicalSubstance wikidata:Q8386 dbo:Drug |
| rdfs:comment | BD1008 or N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-1-pyrrolidineethanamine is a selective sigma receptor antagonist, with a reported binding affinity of Ki = 2 ± 1 nM for the sigma-1 receptor and 4 times selectivity over the sigma-2 receptor. Consistent with other reported sigma receptor antagonists, pretreating Swiss Webster mice with BD1008 significantly attenuates the behavioral toxicity of cocaine, and may be potentially useful in the development of antidotes for the treatment of cocaine overdose. (en) BD1008 o N-[2-(3,4-dichlorophenyl)etilo]-N-metilo-1-pyrrolidineethanamine es un antagonista selectivo del receptor sigma, con una afinidad de unión informada de Ki = 2 ± 1 nM por el receptor sigma-1 y 4 veces la selectividad sobre el receptor sigma-2. De acuerdo con otros antagonistas del receptor sigma informados, el pretratamiento de ratones Swiss Webster con BD1008 atenúa significativamente la toxicidad conductual de la cocaína y puede ser potencialmente útil en el desarrollo de antídotos para el tratamiento de la sobredosis de cocaína. (es) |
| rdfs:label | BD1008 (en) BD1008 (es) |
| owl:sameAs | freebase:BD1008 wikidata:BD1008 dbpedia-es:BD1008 dbpedia-sh:BD1008 dbpedia-sr:BD1008 https://global.dbpedia.org/id/JMBU |
| prov:wasDerivedFrom | wikipedia-en:BD1008?oldid=1108866124&ns=0 |
| foaf:depiction | wiki-commons:Special:FilePath/BD1008.png |
| foaf:isPrimaryTopicOf | wikipedia-en:BD1008 |
| is dbo:wikiPageRedirects of | dbr:BD-1008 dbr:C15H22Cl2N2 |
| is dbo:wikiPageWikiLink of | dbr:BD-1008 dbr:BD1067 dbr:C15H22Cl2N2 dbr:LR132 dbr:BD1018 dbr:BD1031 dbr:BD1052 dbr:BD1060 dbr:BD1063 dbr:Sigma_receptor |
| is foaf:primaryTopic of | wikipedia-en:BD1008 |
