Inhibition of neuronal GABA uptake and glial β-alanine uptake by synthetic GABA analogues |
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Authors: | Robin J Breckenridge Sydney H Nicholson Alan J Nicol Colin J Suckling Beatrice Leigh Leslie Iversen |
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Institution: | Department of Pure and Applied Chemistry, University of Strathclyde, Glasgow, U.K.;M.R.C. Neurochemical Pharmacology Unit, Department of Pharmacology, University of Cambridge, U.K. |
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Abstract: | 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. |
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