Abstract
Studies using HeLa cells expressing 5-HT 7 receptors showed that detergent resistant membranous lipid rafts purified by sucrose gradient centrifugation contained 5-HT 7 receptors and caveolin-1. Caveolin-1 siRNA-mediated knockdown or serotonin (5-HT) treatment caused significant reductions of maximum [ 3H]5-HT binding to 5-HT 7 receptors and total immunoreactivity of membranous 5-HT 7 receptors in intact cells. Co-treatment with 5-HT, caveolin-1 siRNA and methyl-β-cyclodextrin had no additive effects on reducing maximum binding of [ 3H]5-HT to 5-HT 7 receptors. 5-HT-mediated reduction of [ 3H]5-HT binding to 5-HT 7 receptors was counteracted by genistein, but not by sucrose. Caveolin-1, specifically localized in cholesterol-enriched lipid rafts, appears to regulate constitutive and agonist-stimulated cell surface levels of 5-HT 7 receptors via a clathrin-independent mechanism.
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