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Cloning, Expression, and Pharmacology of Four Human 5‐Hydroxytryptamine4 Receptor Isoforms Produced by Alternative Splicing in the Carboxyl Terminus
Abstract: We report here the molecular cloning of three new splice variants of the human serotonin 5‐hydroxytryptamine4 (h5‐HT4) receptor, which we named h5‐HT4(b), h5‐HT4(c), and h5‐HT4(d). TheExpand
Molecular and functional characterization of a 5‐HT4 receptor cloned from human atrium
5‐Hydroxytryptamine (5‐HT) has been shown to exert positive inotropic, chronotropic, and lusitropic effects and to stimulate the L‐type calcium channel current (I Ca) in human atrial tissue throughExpand
Exploration of the ligand binding site of the human 5‐HT4 receptor by site‐directed mutagenesis and molecular modeling
Among the five human 5‐HT4 (h5‐HT4) receptor isoforms, the h5‐HT4(a) receptor was studied with a particular emphasis on the molecular interactions involved in ligand binding. For this purpose, weExpand
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
RT–PCR technique was used to clone the human 5‐HT4(e) receptor (h5‐HT4(e)) from heart atrium. We showed that this h5‐HT4(e) receptor splice variant is restricted to brain and heart atrium.Expand
Prucalopride and donepezil act synergistically to reverse scopolamine-induced memory deficit in C57Bl/6j mice
It is known that 5-HT(4) receptor agonists increase sAPPalpha levels in the cortex and hippocampus of mice as well as in a model of Alzheimer's disease (AD). As sAPPalpha is thought to haveExpand
The 5‐HT4 receptor antagonist ML10375 inhibits the constitutive activity of human 5‐HT4(c) receptor
Transient expression in COS‐7 cells of the recombinant human 5‐hydroxytryptamine (5‐HT) h5‐HT4(c) receptor isoform led to constitutive activity of the receptor. The 5‐HT4 receptor antagonistExpand
5‐HT4 receptor agonists increase sAPPα levels in the cortex and hippocampus of male C57BL/6j mice
A strategy to treat Alzheimer's disease (AD) is to increase the soluble form of amyloid precursor protein (sAPPα), a promnesic protein, in the brain. Because strong evidence supports beneficialExpand
Pharmacological characterization of the human 5‐HT4(d) receptor splice variant stably expressed in Chinese hamster ovary cells
The recently identified C‐terminal splice variant of the human 5‐HT4 receptor, the h5‐HT4(d) receptor, was stably expressed in a CHO cell line at 493±25 fmol mg−1 protein. We analysed itsExpand
Intestinal prokinesia by two esters of 4-amino-5-chloro-2- methoxybenzoic acid: involvement of 5-hydroxytryptamine-4 receptors and dissociation from cardiac effects in vivo.
In five fasting, conscious dogs, we compared the prokinetic action of two selective 5-hydroxytryptamine-4 (5-HT4) receptor agonists with low affinity for 5-HT3 receptors ML10302 (2-piperidinoethylExpand
PAPER 5-HT 4 receptor agonists increase sAPP a levels in the cortex and hippocampus of male C 57 BL / 6 j mice
EA3544, Sérotonine et Neuropharmacologie, Faculté de Pharmacie, Universite Paris-Sud, Châtenay-Malabry cedex, France; IFR-141, Faculté de Pharmacie, Université Paris-Sud, Châtenay-Malabry cedex,Expand