ArticleBritish journal of pharmacology2003
Characterization of human 5-HT4(d) receptor desensitization in CHO cells.
Article in British journal of pharmacology, 2003. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed, 34 citations in OpenAlex.
- Review
- Desensitization of the human 5-HTNaunyn-Schmiedeberg's archives of pharmacology · 2017Article
- Distribution of 5-HT3, 5-HT4, and 5-HT7 Receptors Along the Human Colon.Journal of neurogastroenterology and motility · 2015Article
- Selective desensitization of the 5-HT4 receptor-mediated response in pig atrium but not in stomach.British journal of pharmacology · 2009Article
- The in vitro pharmacological profile of TD-5108, a selective 5-HT(4) receptor agonist with high intrinsic activity.Naunyn-Schmiedeberg's archives of pharmacology · 2008Article
- Serotonin pharmacology in the gastrointestinal tract: a review.Naunyn-Schmiedeberg's archives of pharmacology · 2008Review
- Human 5-HT(4) and 5-HT(7) receptor splice variants: are they important?Current neuropharmacology · 2007Article
- A comparison of the pharmacological properties of guinea-pig and human recombinant 5-HT4 receptors.British journal of pharmacology · 2007Article
- Porcine left atrial and sinoatrial 5-HT(4) receptor-induced responses: fading of the response and influence of development.British journal of pharmacology · 2006Article
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Authors and funding
3 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1 Serotonin 5-HT(4) 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-HT(4) receptors stably expressed in CHO cells, with a special emphasis on the h5-HT(4(d)) isoform. 2 Exposure of h5-HT(4(d)) and h5-HT(4(e)) receptors to 1 micro M 5-HT induced a rapid desensitization of the adenylyl cyclase response. The h5-HT(4(d)) receptor desensitized with a faster rate (t(1/2)<5 min) than the h5-HT(4(e)) receptor (t(1/2)=15 min) and after 10 min 5-HT treatment cAMP production was reduced by approximately 70%. 3 5-HT-induced h5-HT(4(d)) receptor desensitization was mimicked by 8-Bromo-cAMP, a cAMP analogue, and was inhibited by [n-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulphonamide, 2HCl] (H-89), an inhibitor of cAMP-dependent protein kinase (PKA). Inhibitors of endocytosis (sucrose, 0.45 M and concanavaline A, 0.25 mg ml(-1)) partially reversed the h5-HT(4(d)) receptor desensitization process. 4 Given the prominent role of PKA in agonist-induced desensitization, we mutated the four putative PKA phosphorylation sites present in the third intracellular loop (Ser242, Thr253, Thr255) and the C terminal tail (Ser338) of the h5-HT(4(d)) receptor. Surprisingly, mutated receptors in which either one or all four putative phosphorylation sites were substituted to alanine did not impair receptor desensitization suggesting that PKA might act on nonconsensus sites. 5 Altogether, our data demonstrate that the C-terminal tail of h5-HT(4) receptors may influence the rate of agonist-induced desensitization and we provide evidence for a major role of PKA in h5-HT(4(d)) receptor desensitization.
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