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Synthesis and Preliminary Screening of Novel Tryptamines as 5-HT4 Receptor Ligands

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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.
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Keywords: 5-HT4 ligands; 5-HT4 receptor; medicinal chemistry; serotonin; tryptamine

Document Type: Research Article

Affiliations: Medicinal Chemistry and Drug Action, Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, Vic. 3053, Australia.

Publication date: 2010-09-01

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