A. Hanna-Elias, D.T. Manallack, I. Berque-Bestel, H.R. Irving, I.M. Coupar and M.N. Iskander Pages 2775 - 2787 ( 13 )
For the development of novel 5-HT4 receptor ligands we have designed and synthesized two series of 5- methoxytryptamine derivatives varying the substitution on the primary amine. Their biological activities were evaluated in a receptor binding assay where a subset of compounds showed comparable potency to the agonists serotonin and 5- methoxytryptamine. Structure-activity analyses have highlighted promising avenues for further synthetic work and binding modes were proposed by docking these compounds into a homology model of the 5-HT4 receptor.
5-HT4 ligands,serotonin,tryptamine,5-HT4 receptor,medicinal chemistry
, , , , , Medicinal Chemistry and Drug Action, Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, Vic. 3053, Australia.