rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
1
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pubmed:dateCreated |
1994-4-28
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pubmed:abstractText |
The selectivity of N,N-dipropyl-2-[4-methoxy-3-(2-phenylethoxy)phenyl]-ethylamine monohydrochloride (NE-100) for sigma 1 and sigma 2 binding sites was studied by means of binding of [3H](+)-pentazocine and [3H]1,3-di-o-tolylguanidine ([3H]DTG) in guinea pig brain. NE-100 inhibited [3H](+)-pentazocine binding to sigma 1 binding sites potently with an IC50 value of 1.54 +/- 0.26 nM while it had a weak effect on [3H]DTG binding to sigma 2 binding sites. The inhibitory effect of NE-100 on [3H](+)-pentazocine was 55 times more potent than that on [3H]DTG binding. These results suggest that NE-100 is a potent and selective ligand for sigma 1 binding sites.
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pubmed:language |
eng
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pubmed:journal |
|
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/1,3-ditolylguanidine,
http://linkedlifedata.com/resource/pubmed/chemical/Anisoles,
http://linkedlifedata.com/resource/pubmed/chemical/Guanidines,
http://linkedlifedata.com/resource/pubmed/chemical/Ligands,
http://linkedlifedata.com/resource/pubmed/chemical/N,N-dipropyl-2-(4-methoxy-3-(2-pheny...,
http://linkedlifedata.com/resource/pubmed/chemical/Pentazocine,
http://linkedlifedata.com/resource/pubmed/chemical/Propylamines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, sigma
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pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
0014-2999
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pubmed:author |
|
pubmed:issnType |
Print
|
pubmed:day |
4
|
pubmed:volume |
251
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pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
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pubmed:pagination |
R1-2
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:8137864-Animals,
pubmed-meshheading:8137864-Anisoles,
pubmed-meshheading:8137864-Binding, Competitive,
pubmed-meshheading:8137864-Brain,
pubmed-meshheading:8137864-Guanidines,
pubmed-meshheading:8137864-Guinea Pigs,
pubmed-meshheading:8137864-Ligands,
pubmed-meshheading:8137864-Pentazocine,
pubmed-meshheading:8137864-Propylamines,
pubmed-meshheading:8137864-Receptors, sigma
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pubmed:year |
1994
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pubmed:articleTitle |
NE-100, a novel potent sigma ligand, preferentially binds to sigma 1 binding sites in guinea pig brain.
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pubmed:affiliation |
Department of Pharmacology, Taisho Pharmaceutical Co. Ltd., Saitama, Japan.
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pubmed:publicationType |
Journal Article,
In Vitro
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