Characterization of human 5‐HT4(d) receptor desensitization in CHO cells

• Published in: British journal of pharmacology 2003-02, Vol.138 (3), p.445-452
• Main Authors: Mialet, Jeanne, Fischmeister, Rodolphe, Lezoualc'h, Frank
• Format: Article
• Language: English
• Subjects: adenylyl cyclase; Animals; Biological and medical sciences; Cell receptors; Cell structures and functions; CHO Cells; Cricetinae; cyclic AMP; Cyclic AMP - biosynthesis; Cyclic AMP-Dependent Protein Kinases - antagonists & inhibitors; desensitization; Enzyme Inhibitors - pharmacology; Fundamental and applied biological sciences. Psychology; G protein‐coupled receptor kinase; G‐protein‐coupled receptors; Humans; Molecular and cellular biology; Monoamines receptors (catecholamine, serotonine, histamine, acetylcholine); Mutagenesis, Site-Directed; Protein Isoforms - drug effects; Protein Isoforms - genetics; Protein Isoforms - physiology; protein kinase A; Radioimmunoassay; Receptors, Serotonin - drug effects; Receptors, Serotonin - genetics; Receptors, Serotonin - physiology; Receptors, Serotonin, 5-HT4; Serotonin Receptor Agonists - pharmacology; serotoninergic receptors; Signal Transduction - physiology; Time Factors
• ISSN: 0007-1188; 1476-5381
• DOI: 10.1038/sj.bjp.0705061

Serotonin 5‐HT4 receptor isoforms differ in their C‐terminal tail and yet little is known about their regulation. In this study, we investigated the desensitization of two human 5‐HT4 receptors stably expressed in CHO cells, with a special emphasis on the h5‐HT4(d) isoform. Exposure of h5‐HT4(d) and h5‐HT4(e) receptors to 1 μM 5‐HT induced a rapid desensitization of the adenylyl cyclase response. The h5‐HT4(d) receptor desensitized with a faster rate (t1/2