Quantitative structure-activity relationship study on tetrahydro-β-carboline antagonists of the serotonin 2B (5HT2B) contractile receptor in the rat stomach fundus

The antagonist actions of three sub-series of tetrahydro-beta-carbolines at the serotonin 2B (5HT(2B)) contractile receptor in the rat stomach fundus are analyzed in relation to the physicochemical properties of the molecules. Significant correlations are obtained between the 5HT(2B) receptor antagonist affinity and the hydrophobic, steric, electronic, hydrogen bond acceptor and some indicator variables of substituents. Based on these findings, the mode of actions of these congeneric series and future strategy to synthesize more potential compounds are discussed.