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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
22
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pubmed:dateCreated |
1992-12-1
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pubmed:abstractText |
Ten analogs of muscimol and thiomuscimol in which the amino function was delocalized in an amidinic system were prepared by N2 alkylation of 6-aryl-3-aminopyridazines with (chloromethyl)isoxazole or (chloromethyl)isothiazole derivatives. These muscimol and thiomuscimol derivatives show potent binding properties for GABA-A receptors (they displace [3H]GABA and [3H]gabazine) and provoke convulsions after iv injections. They fit well with the model pharmacophore proposed by our group for the GABA-A antagonists and show similar structure-activity profiles to that of the pyridazinyl-GABAs.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Oct
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pubmed:issn |
0022-2623
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
30
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pubmed:volume |
35
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4092-7
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:1331456-Animals,
pubmed-meshheading:1331456-Binding, Competitive,
pubmed-meshheading:1331456-Convulsants,
pubmed-meshheading:1331456-Female,
pubmed-meshheading:1331456-GABA-A Receptor Antagonists,
pubmed-meshheading:1331456-Mice,
pubmed-meshheading:1331456-Models, Molecular,
pubmed-meshheading:1331456-Molecular Conformation,
pubmed-meshheading:1331456-Muscimol,
pubmed-meshheading:1331456-Pyridazines,
pubmed-meshheading:1331456-Radioligand Assay,
pubmed-meshheading:1331456-Rats,
pubmed-meshheading:1331456-Receptors, GABA-A,
pubmed-meshheading:1331456-Structure-Activity Relationship
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pubmed:year |
1992
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pubmed:articleTitle |
Condensation of muscimol or thiomuscimol with aminopyridazines yields GABA-A antagonists.
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pubmed:affiliation |
Centre de Neurochimie du CNRS, Strasbourg, France.
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pubmed:publicationType |
Journal Article,
In Vitro
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