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Título

Cloning and characterization of a novel human 5-HT4 receptor variant that lacks the alternatively spliced carboxy terminal exon. RT-PCR distribution in human brain and periphery of multiple 5-HT4 receptor variants

Autor Vilaró, Maria Teresa ; Doménech, Teresa; Palacios, José M.; Mengod Los Arcos, Guadalupe
Palabras clave Receptor constitutive activity
C-terminal splice variants
[3H]GR 113808
Human brain distribution
5-HT4 receptors
Fecha de publicación 31-oct-2001
EditorPergamon Press
Citación Neuropharmacology 42(1): 60-73 (2002)
ResumenWe have cloned a novel C-terminal splice variant of serotonin 5-HT4 receptors from human hippocampus. The deduced protein extends only one aminoacid past the splicing point. We propose to call the novel variant h5-HT4(n) since it contains none of the C-terminal exons alternatively spliced in other variants. The pharmacological profile of h5-HT4(n) stably expressed in HeLa cells is in agreement with other reported variants. Stably transfected cells showed increased basal levels of intracellular cAMP in absence of agonist, indicating constitutive activity of the expressed receptors. 5-HT induced robust increases of intracellular cAMP. The 5-HT4 receptor antagonist GR 113808 blocked the effects of 5-HT and brought intracellular cAMP below basal constitutive levels, indicating inverse agonism of this compound in this system. The RT-PCR distribution of all known human C-terminal splice variants in human brain regions and periphery showed complex patterns of variant expression, with the novel variant h5-HT4(n) being widely and abundantly expressed. © 2002 Elsevier Science Ltd. All rights reserved.
Versión del editorhttp://dx.doi.org/10.1016/S0028-3908(01)00154-X
URI http://hdl.handle.net/10261/112650
DOI10.1016/S0028-3908(01)00154-X
Identificadoresdoi: 10.1016/S0028-3908(01)00154-X
issn: 0028-3908
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