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

European Journal of Pharmacology
P Placheta, M Karobath

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.

References

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Citations

Aug 11, 1981·Molecular and Cellular Biochemistry·P Krogsgaard-Larsen, E Falch
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