Recent studies have demonstrated that serotonin (5-hydroxytryptamine, 5-HT) may interact with either specific receptors or with a specific transporter that takes up 5-HT in the gastrointestinal tract. The purpose of the present work was to study the 5-HT interactions with brush border membrane from rabbit jejunum enterocytes. The results obtained showed that 5-HT did not seem to be transported by any specific system of transport in brush border membrane vesicles. Nevertheless, [3H]5-HT seemed to bind specifically to this membrane. The kinetic analysis indicated a saturable and dissociable specific binding with a dissociation constant K(D)=14x10(-9) M. The saturation studies with [3H]5-HT indicated the presence of one specific site in the brush border membrane. The results of displacement of [3H]5-HT specific binding from the brush border membrane showed that both unlabelled 5-HT and unlabelled GR113080 ([1-[(2-methyl sulphonyl) amino] ethyl-4-piperidinyl] methyl-1-methyl-1H-indole-3-carboxylate), a specific competitive antagonist of 5-HT(4) receptors, inhibited the specific binding of [3H]5-HT to this membrane.