BD1008 (original) (raw)

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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.

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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
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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
dct: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)
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