Regulate a family of transmembrane chloride channels such that binding of GABA or its analogs permits increased chloride influx, membrane hyperpolarization, and inhibition of postsynaptic electrical activity.

(receptors, gaba) Cell-surface proteins that bind GAMMA-AMINOBUTYRIC ACID with high affinity and trigger changes that influence the behavior of cells. GABA-A receptors control chloride channels formed by the receptor complex itself. They are blocked by bicuculline and usually have modulatory sites sensitive to benzodiazepines and barbiturates. GABA-B receptors act through G-proteins on several effector systems, are insensitive to bicuculline, and have a high affinity for L-baclofen.