title: In vitro modulation by SQ 20009 and SQ 65396 of GABA receptor binding in rat CNS membranes.
abstract: SQ 20009 and SQ 65396, two new pyrazolopyridines with anxiolytic properties in animals, reversibly increased Na+-independent 3H-GABA binding to rat cerabral cortex membranes in vitro. This modulation was partially chloride dependent and sensitive to Triton-X 100. Kinetic analysis of 3H-muscimol binding revealed an increase of the apparent number of binding sites. The results are compatible with a functional association between Na+-independent GABA binding sites and the GABA/benzodiazepine receptor complex.
mesh_terms: D000818:Animals; D014151:Anti-Anxiety Agents / Q000494:pharmacology*; D001921:Brain / Q000187:drug effects / Q000378:metabolism*; D004974:Etazolate / Q000494:pharmacology*; D066298:In Vitro Techniques; D007700:Kinetics; D008566:Membranes / Q000378:metabolism; D009118:Muscimol / Q000378:metabolism; D009419:Nerve Tissue Proteins / Q000378:metabolism; D009539:Nicotinic Acids / Q000494:pharmacology*; D011720:Pyrazoles / Q000494:pharmacology*; D011725:Pyridines / Q000494:pharmacology*; D051381:Rats; D011956:Receptors, Cell Surface / Q000187:drug effects / Q000378:metabolism*; D005680:gamma-Aminobutyric Acid / Q000378:metabolism*
chemical_list: D014151:Anti-Anxiety Agents; D009419:Nerve Tissue Proteins; D009539:Nicotinic Acids; D011720:Pyrazoles; D011725:Pyridines; D011956:Receptors, Cell Surface; D009118:Muscimol; D005680:gamma-Aminobutyric Acid; C006315:cartazolate; D004974:Etazolate