The aim of the present study was to determine the 5-HT receptor subtypes involved in the serotonin-induced inhibition of L-leucine absorption across rabbit jejunum in vitro. A number of agonists and antagonists were used to characterize the receptors through which serotonin inhibits this absorption. The results show that 2.5x10(-6) M 5-HT inhibits the amino acid absorption by about 20%. The 5-HT receptor agonists, alpha-methyl-5-HT (5-HT2), 2-methyl-5-HT (5-HT3) and zacopride (5-HT4) at concentrations 2.5x10(-6) and 2.5x10(-5) M produced 10-30% inhibition on L-leucine intestinal absorption. 5-carboxyamidotryptamine (5-HT1) did not produce any inhibition. The 5-HT antagonists, GR 113808A (5-HT4) at 2.5x10(-6) M and ritanserin (5-HT2) and ondansetron (5-HT3) at 2.5x10(-5) M completely blocked the effect of 5-HT. However, methiothepin (5-HT1) did not produce any effect on serotonin action in the intestinal absorption of amino acid. It can be concluded that 5-HT2, 5-HT3 and 5-HT4 receptors could mediate inhibition of L-leucine absorption across rabbit jejunum.