GABA-B Receptor Antagonists Small Molecules and Peptides

GABA_B receptors are GPCRs composed of seven transmembrane domains and a large extracellular N-terminal, and are responsible for mediating the inhibitory effects of GABA, alongside ionotropic GABA_A and GABA_A-ρ receptors. They are composed of 850 - 960 amino acids, and are most similar in structure to metabotropic glutamate receptors (mGluRs).

These receptors are heterodimers of GABA_B1 and GABA_B2 subunits. The GABA_B1 subunit hosts the binding site for GABA and other ligands, while the GABA_B2...