Allosteric Modulation of the Human 5-HT7A Receptor by Lipidic Amphipathic Compounds

Human 5-HT 7A receptors positively modulated adenylyl cyclases via G s subtypes of G proteins in human embryonic kidney 293 cells, and bound 5-hydroxytryptamine (HT) with high and low affinity ( K I values of 1.5 ± 0.3 and 93 ± 4 nM). More than 60% of 5-HT 7A receptors, however, displayed the high...

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Bibliographic Details
Published in:Molecular pharmacology 2001-12, Vol.60 (6), p.1349-1355
Main Authors: Alberts, Glen L., Chio, Christopher L., Im, Wha Bin
Format: Article
Language:English
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Summary:Human 5-HT 7A receptors positively modulated adenylyl cyclases via G s subtypes of G proteins in human embryonic kidney 293 cells, and bound 5-hydroxytryptamine (HT) with high and low affinity ( K I values of 1.5 ± 0.3 and 93 ± 4 nM). More than 60% of 5-HT 7A receptors, however, displayed the high-affinity 5-HT binding with no sensitivity to 5′-guanylylimidodiphosphate. In this study, we found that select amphipathic agents affected the high-affinity 5-HT binding to 5-HT 7A . Oleic acid at low concentrations (
ISSN:0026-895X
1521-0111
DOI:10.1124/mol.60.6.1349