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pubmed-article:1331456pubmed:abstractTextTen 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.lld:pubmed
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pubmed-article:1331456pubmed:articleTitleCondensation of muscimol or thiomuscimol with aminopyridazines yields GABA-A antagonists.lld:pubmed
pubmed-article:1331456pubmed:affiliationCentre de Neurochimie du CNRS, Strasbourg, France.lld:pubmed
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