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Merck

Synthesis and preliminary screening of novel tryptamines as 5-HT4 receptor ligands.

Current medicinal chemistry (2010-07-01)
A Hanna-Elias, D T Manallack, I Berque-Bestel, H R Irving, I M Coupar, M N Iskander
RESUMO

For the development of novel 5-HT(4) 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-HT(4) receptor.

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Sigma-Aldrich
5-Methoxytryptamine, 97%