Inhibition of neuronal GABA uptake and glial β-alanine uptake by synthetic GABA analogues

Thirty three synthetic analogues of GABA were tested for their ability to act as inhibitors of neuronal or glial uptake sites for GABA and β-alanine, using ³H]GABA uptake by synaptosome preparations from rat cerebral cortex, and ³H]β-alanine uptake by cortical slices as test systems for neuronal and glial uptake sites, respectively. The results confirm that both uptake processes favour a substantially folded conformation. Neuronal uptake sites were significantly inhibited by analogues with long alkyl side chain substituents, such as dodecyl GABA-amide which was of comparable potency to GABA.