Inhibition of [3H]GABA Binding to Postsynaptic Receptors in Human Cerebellar Synaptic Membranes by Carboxyl and Amino Derivatives of GABA

Abstract

Synthetic analog [50] of GABA were tested for their ability to interact with GABA receptors, using [3] GABA binding to human cerebellar membranes as an in vitro model. The most active compounds were aliphatic and heterocyclic aminosulfonic acids. Compounds with highly substituted N atoms were only weakly active unless a long alkyl chain, which can interact with the postsynaptic membrane, was present. A pyramidal N atom is probably favored for binding of GABA analogs to human cerebellar membranes.