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Eur J Pharmacol. 2005 Jul 25;518(1):18-21.

Insulin induces internalization of the 5-HT2A receptor expressed in HEK293 cells.

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First Department of Pharmacology, School of Pharmaceutical Sciences, Kyushu University of Health and Welfare, Yoshino, Nobeoka 882-8508, Japan.


To visualize the 5-hydroxytryptamine2A (5-HT2A) receptor, we developed a 5-HT2A receptor fused with yellow fluorescent protein (5-HT2A-YFP) and expressed this receptor in HEK293 cells. In 5-HT2A-YFP-expressing cells, but not in YFP-expressing or non-expressing cells, 5-HT induced a transient increase in the intracellular Ca(2+) concentration (Ca(2+) transient) in the Fluo 3 assay, suggesting that 5-HT2A-YFP possesses a function similar to the wild-type 5-HT2A receptor. Interestingly, not only 5-HT but also insulin induced the internalization of 5-HT2A-YFP. Insulin also inhibited the 5-HT-induced Ca(2+) transient. Genistein, an inhibitor of tyrosine kinase, blocked these insulin effects. Our results provide the first evidence that insulin receptor signaling via tyrosine kinase activation induces internalization of the plasma membrane 5-HT2A receptor, and demonstrate crosstalk between the 5-HT2A receptor and the insulin receptor.

[Indexed for MEDLINE]

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