Gamma amino butyric acid is a major inhibitory neurotransmitter in the central nervous system. In the present study we have investigated the alteration of GABA receptors in the brain stem of rats during pancreatic regeneration. Three groups of rats were used for the study: sham operated, 72 h and 7 days partially pancreatectomised. GABA was quantified by [(3)H]GABA receptor displacement method. GABA receptor kinetic parameters were studied by using the binding of [(3)H]GABA as ligand to the Triton X-100 treated membranes and displacement with unlabelled GABA. GABA(A) receptor activity was studied by using the [(3)H]bicuculline and displacement with unlabelled bicuculline. GABA content significantly decreased (P < 0.001) in the brain stem during the regeneration of pancreas. The high affinity GABA receptor binding showed a significant decrease in B(max) (P < 0.01) and K(d) (P < 0.05) in 72 h and 7 days after partial pancreatectomy. [(3)H]bicuculline binding showed a significant decrease in B(max) and K(d) (P < 0.001) in 72 h pancreatectomised rats when compared with sham where as B(max) and K(d) reversed to near sham after 7 days of pancreatectomy. The results suggest that GABA through GABA receptors in brain stem has a regulatory role during active regeneration of pancreas which will have immense clinical significance in the treatment of diabetes.