ArticleBritish journal of pharmacology2000
Isolation of the serotoninergic 5-HT4(e) receptor from human heart and comparative analysis of its pharmacological profile in C6-glial and CHO cell lines.
Article in British journal of pharmacology, 2000. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 68 citations in OpenAlex.
- Serotonergic Psychedelics Rapidly Modulate Evoked Glutamate Release in Cultured Cortical Neurons.Journal of neurochemistry · 2025Article
- Cardiac Roles of Serotonin (5-HT) and 5-HT-Receptors in Health and Disease.International journal of molecular sciences · 2023Review
- New characterization of dihydroergotamine receptor pharmacology in the context of migraine: utilization of a β-arrestin recruitment assay.Frontiers in neurology · 2023Article
- Distribution of 5-HT3, 5-HT4, and 5-HT7 Receptors Along the Human Colon.Journal of neurogastroenterology and motility · 2015Article
- Article
- The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptors.British journal of pharmacology · 2013Article
- 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
- Pharmacology and metabolism of renzapride : a novel therapeutic agent for the potential treatment of irritable bowel syndrome.Drugs in R&D · 2008Article
- Human 5-HT(4) and 5-HT(7) receptor splice variants: are they important?Current neuropharmacology · 2007Article
- Immunomodulation by maternal autoantibodies of the fetal serotoninergic 5-HT4 receptor and its consequences in early BALB/c mouse embryonic development.BMC developmental biology · 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
- Functional studies of the 5'-untranslated region of human 5-HT4 receptor mRNA.The Biochemical journal · 2005Article
- New insights into the human 5-HT4 receptor binding site: exploration of a hydrophobic pocket.British journal of pharmacology · 2004Article
- Functional serotonin 5-HT4 receptors in porcine and human ventricular myocardium with increased 5-HT4 mRNA in heart failure.Naunyn-Schmiedeberg's archives of pharmacology · 2004Article
- Cloning, pharmacological characterisation and tissue distribution of a novel 5-HT4 receptor splice variant, 5-HT4(i).Naunyn-Schmiedeberg's archives of pharmacology · 2004Article
- Characterization of human 5-HT4(d) receptor desensitization in CHO cells.British journal of pharmacology · 2003Article
- Pharmacological characterization of the human 5-HT(4(d)) receptor splice variant stably expressed in Chinese hamster ovary cells.British journal of pharmacology · 2000Article
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Authors and funding
12 authors at 6 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
RT - PCR technique was used to clone the human 5-HT(4(e)) receptor (h5-HT(4(e))) from heart atrium. We showed that this h5-HT(4(e)) receptor splice variant is restricted to brain and heart atrium. Recombinant h5-HT(4(e)) receptor was stably expressed in CHO and C6-glial cell lines at 347 and 88 fmol mg(-1) protein, respectively. Expression of h5-HT(4(e)) receptors at the cell membrane was confirmed by immunoblotting. The receptor binding profile, determined by competition with [(3)H]-GR113808 of a number of 5-HT(4) ligands, was consistent with that previously reported for other 5-HT(4) receptor isoforms. Surprisingly, we found that the rank order of potencies (EC(50)) of 5-HT(4) agonists obtained from adenylyl cyclase functional assays was inversely correlated to their rank order of affinities (K(i)) obtained from binding assays. Furthermore, EC(50) values for 5-HT, renzapride and cisapride were 2 fold lower in C6-glial cells than in CHO cells. ML10302 and renzapride behaved like partial agonists on the h5-HT(4(e)) receptor. These results are in agreement with the reported low efficacy of the these two compounds on L-type Ca(2+) currents and myocyte contractility in human atrium. A constitutive activity of the h5-HT(4(e)) receptor was observed in CHO cells in the absence of any 5-HT(4) ligand and two 5-HT(4) antagonists, GR113808 and ML10375, behaved as inverse agonists. These data show that the h5-HT(4(e)) receptor has a pharmacological profile which is close to the native h5-HT(4) receptor in human atrium with a functional potency which is dependent on the cellular context in which the receptor is expressed.
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