Inhibition of high-affinity synaptosomal uptake of gamma-aminobutyric acid by a bicyclo-heptane derivative.
EGYT 3886 (dia(-)2-phenyl-2-(dimethylamino-ethoxy) - 1R - 1,7,7-trimethyl-bicyclo[2.2.1.]heptane hemifumarate) exhibiting anxiolytic and anticonvulsant properties is inactive on various binding sites of the GABAA (gamma-aminobutyric acid A) receptor/chloride ionophore complex, but is an effective inhibitor of high-affinity synaptosomal 3H-GABA uptake.
Kovács
I
I
Central Research Institute for Chemistry, Hungarian Academy of Sciences, Budapest.
Maksay
G
G
Simonyi
M
M
D000818:Animals; D000927:Anticonvulsants / Q000494:pharmacology*; D001643:Bridged Bicyclo Compounds / Q000378:metabolism / Q000494:pharmacology*; D019086:Bridged Bicyclo Compounds, Heterocyclic; D001952:Bridged-Ring Compounds / Q000494:pharmacology*; D001892:Camphanes; D002243:Carbolines / Q000378:metabolism; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism; D003975:Diazepam / Q000378:metabolism; D005442:Flumazenil / Q000378:metabolism; D066298:In Vitro Techniques; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D013570:Synaptic Membranes / Q000187:drug effects / Q000378:metabolism; D013574:Synaptosomes / Q000378:metabolism*; D005680:gamma-Aminobutyric Acid / Q000378:metabolism*
D000927:Anticonvulsants; D001643:Bridged Bicyclo Compounds; D019086:Bridged Bicyclo Compounds, Heterocyclic; D001952:Bridged-Ring Compounds; D001892:Camphanes; D002243:Carbolines; D005442:Flumazenil; D005680:gamma-Aminobutyric Acid; C046308:tert-butylbicyclo-2-benzoate; C036150:beta-carboline-3-carboxylic acid methyl ester; C060555:deramciclane; D003975:Diazepam