The amino acid γ-aminobutyric acid (GABA) is an inhibitory neurotransmitter that acts through two families of heteromeric ligand-gated ion channels, GABAA and GABAC, and a G protein-coupled receptor, GABAB. CGP 35348 is a selective, brain-accessible GABAB receptor antagonist (IC50 = 34 μM). It blocks the action of the GABAB-selective agonist baclofen at postsynaptic sites but not at presynaptic receptors. CGP 35348 prevents baclofen-induced antinociception and muscle relaxation in mice and rats. It is commonly used to investigate the role of GABAB activation in neurological signaling.
