In vitro modulation by SQ 20009 and SQ 65396 of GABA receptor binding in rat CNS membranes.
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.
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*
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