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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
5
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pubmed:dateCreated |
1989-6-6
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pubmed:abstractText |
A series of 6,9-disubstituted purines were tested for their ability to bind to the benzodiazepine receptor in rat brain tissue. One of the most active compounds was 9-(3-aminobenzyl)-6-(dimethylamino)-9H-purine (44) with an IC50 = 0.9 microM, which was only 4.5-fold higher than the IC50 for chlordiazepoxide. Substitution of a 3-aminobenzyl or 3-hydroxybenzyl group at the 9-position of 6-(dimethylamino)purine led to over a 50-fold increase in receptor affinity. Compound 44 did not exhibit significant anxiolytic activity, nor did anticonvulsant activity correlate with relative receptor binding affinity.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
May
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
32
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1020-4
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pubmed:dateRevised |
2003-11-14
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pubmed:meshHeading |
pubmed-meshheading:2540330-Animals,
pubmed-meshheading:2540330-Anticonvulsants,
pubmed-meshheading:2540330-Conflict (Psychology),
pubmed-meshheading:2540330-Diazepam,
pubmed-meshheading:2540330-Female,
pubmed-meshheading:2540330-Purines,
pubmed-meshheading:2540330-Rats,
pubmed-meshheading:2540330-Receptors, GABA-A,
pubmed-meshheading:2540330-Structure-Activity Relationship
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pubmed:year |
1989
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pubmed:articleTitle |
Benzodiazepine receptor binding activity of 6,9-disubstituted purines.
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pubmed:affiliation |
Division of Organic Chemistry, Burroughs Wellcome Co., Research Triangle Park, North Carolina 27709.
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pubmed:publicationType |
Journal Article
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