Summary
Because tryptamine derivatives typically bind at multiple populations of 5-HT receptors, they are not normally considered as templates for the design of site-selective serotonergic agents. Taking advantage of the proposal that 5-HT3 receptors are ligand-gated ion channel receptors, and that such receptors usually accept positively charged ligands, we synthesized and evaluated the N,N,N-trimethyl quaternary amine analog of serotonin (5HTQ), 5-HTQ binds at 5-HT3 receptors with ten times the affinity of 5-HT and displays considerable selectivity relative to the other populations of 5-HT receptors. Although 5-HTQ may not readily penetrate the blood-brain barrier, limiting its application for in vivo investigations, it should be useful for in vitro studies.
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© 1991 Birkhäuser Verlag Basel/Switzerland
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Glennon, R.A., Peroutka, S.J., Dukat, M. (1991). Binding Characteristics of a Quaternary Amine Analog of Serotonin: 5-HTQ. In: Fozard, J.R., Saxena, P.R. (eds) Serotonin: Molecular Biology, Receptors and Functional Effects. Birkhäuser Basel. https://doi.org/10.1007/978-3-0348-7259-1_17
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DOI: https://doi.org/10.1007/978-3-0348-7259-1_17
Publisher Name: Birkhäuser Basel
Print ISBN: 978-3-0348-7261-4
Online ISBN: 978-3-0348-7259-1
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