Possible Interaction: Gamma-Aminobutyric Acid and Gaboxadol

“Further analysis of α1(T47R)β2γ2 receptors revealed that the efficacy of the partial agonist THIP (4,5,6,7‐tetrahydroisoxazolo[5,4‐c]pyridine‐3‐ol) relative to GABA was impaired.”

“Concomitant intranigral injection of the GABA agonists muscimol and THIP , however, completely antagonized biting.”

“The substrate specificity of the high-affinity transporter was further studied and Gly-Sar, Leucine, gaboxadol , sarcosine, lysine, betaine, 5-hydroxythryptophan, proline and glycine reduced the GABA uptake to approximately 44-70% of the GABA uptake in the absence of inhibitor.”

“ Gaboxadol inhibition of the binding could be partially prevented by GABA.”

“The GABA agonists, muscimol, baclofen and THIP decreased the accumulation of GABA following inhibition of GABA-α-ketoglutaric acid aminotransferase byγ-acetylenic GABA (GAG) in both structures investigated.”

“Superfusion experiments on cells cultured under the different conditions demonstrated that the low affinity GABA receptors expressed after culturing in the presence of THIP or taurine mediated an inhibition by GABA of evoked transmitter release from the granule cells.”

“Treatment with THIP (15 mg/kg) was found to block the antinociceptive response to an inhibitor of the uptake of GABA , an inhibitor of GABA-transaminase, a direct-acting GABA receptor agonist and to a cholinesterase inhibitor.”

“GABA analogues such as muscimol, piperidine-4-sulphonic acid, homo-beta-proline, THIP , and isoguvacine were potent displacers of GABA binding to cultured granule cells, whereas nipecotic acid and guvacine had no effect.”

“Abstract: Depolarization‐induced release of [3H]γ‐aminobutyric acid ([3H]‐GABA) from preloaded slices of rat cerebral cortex was inhibited by muscimol and THIP in a dose‐dependent fashion.”

“ THIP , which has only minimal stimulatory effects on benzodiazepine (BZ) receptor binding, has been found to inhibit the stimulation induced by small concentrations (2 microM) of exogenous GABA.”