Abstract: OBJECTIVE To observe the antianxiety effects of the baicalin bind the g-aminobutyric acid(GABA) receptor. METHODS By radioactive-labeled GABA receptor binding assay and the elevated plus-maze test and hole-board test, the study observed the relationship of the baicalin with GABA receptor and the animal behaviour changes after administrated with baicalin. RESULTS The GABA receptor binding assay showed that the baicalin inhibited 50% GABA receptor benzodiazepine’s site(IC₅₀) which was (117.62±8.50)μmol·L^-1 and K_i value was (77.10±4.79)μmol·L^-1. The baicalin increased the number, time spent, percentage at open arm entries of elevated plus-maze, decreased the number of head-dips and rears at the hole-board test. These changes had a significant relationship with baicalin dosage and was blocked by GABA receptor antagonist Ro 15-1788. CONCLUSION The baicalin is a ligand of GABA binding site and it has some effect of anti-anxiety disorders.