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5-HT5B Receptor

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René Hen – One of the best experts on this subject based on the ideXlab platform.

  • Human 5-HT5 Receptors: the 5-HT5A Receptor is functional but the 5-HT5B Receptor was lost during mammalian evolution
    European journal of pharmacology, 2001
    Co-Authors: Régis Grailhe, Gregg W. Grabtree, René Hen

    Abstract:

    Abstract We have isolated from a human genomic library the human 5-hydroxytryptamine 5-HT 5A and 5-HT 5B genes. The human 5-HT 5A gene encodes a protein with similar characteristics to its mouse homologue. When expressed in monkey COS-7 cells, the human 5-HT 5A Receptor displayed a high affinity for tritiated 5-carbamidotryptamine ([ 3 H]5-CT; K D =2.8 nM) and iodinated lysergic acid diethylamide ([ 125 I]LSD; K D =187 pM). These binding sites displayed the following displacement profile: Ergotamine>Methiothepin>5-CT, Ritanserin>5-HT. Reverse transcriptase polymerase chain reaction (RT-PCR) experiments revealed the presence of human 5-HT 5A mRNA in the central nervous system but not in peripheral organs. When expressed in Xenopus oocytes, the 5-HT 5A Receptor was able to couple to the inwardly rectifying K + channel, GIRK 1 . In contrast to the human 5-HT 5A gene and the mouse 5-HT 5B gene, the human 5-HT 5B gene does not encode a functional protein because its coding sequence is interrupted by stop codons. Our results suggest, therefore, that the 5-HT 5B Receptor has been lost during evolution after the divergence between rodents and primates. The 5-HT 5B Receptor is the first example of a brain-specific protein that is absent in human.

  • Mouse 5-hydroxytryptamine5A and 5-hydroxytryptamine5B Receptors define a new family of serotonin Receptors: cloning, functional expression, and chromosomal localization.
    Molecular pharmacology, 1993
    Co-Authors: H Matthes, Ursula Boschert, Nourdine Amlaiky, R. Grailhe, Jean-luc Plassat, Françoise Muscatelli, Marie Geneviève Mattei, René Hen

    Abstract:

    Serotonin [5-hydroxytryptamine (5-HT)] is a neuromodulator that mediates a wide range of physiological functions by activating multiple Receptors. Using a strategy based on amino acid sequence homology between 5-HT Receptors that interact with guanine nucleotide-binding proteins, we have isolated from a mouse brain library a cDNA encoding a new serotonin Receptor. Amino acid sequence comparisons revealed that this Receptor was a close relative of the previously identified 5-HT5 Receptor but was distant from all other 5-HT Receptor subtypes; we therefore named it 5-HT5B. When expressed in COS-7 cells, the 5-HT5B Receptor displayed a high affinity for the serotonergic radioligand 125I-lysergic acid diethylamide. Its pharmacological profile was distinct from that of all classic 5-HT Receptor subtypes. However, the high affinity of the 5-HT5B Receptor for 5-carboxamidotryptamine and its low affinity for sumatriptan indicated that it might correspond to recently described 5-HT1D-like binding sites that were labeled with [3H]5-carboxamidotryptamine and insensitive to sumatriptan. In situ hybridization experiments revealed that the 5-HT5B mRNA was expressed predominantly in the habenula and in the CA1 field of the hippocampus. We also determined the chromosomal localization of the 5-HT5A and 5-HT5B genes and of their human counterparts. The 5-HT5A gene colocalized with the mouse mutation reeler and the human mutation holoprosencephaly type 3, which both result in abnormal brain development, raising the possibility that the 5-HT5A Receptor plays a role in brain development.

Mark M. Voigt – One of the best experts on this subject based on the ideXlab platform.

  • Cloning and characterization of the rat 5-HT5B Receptor : evidence that the 5-HT5B Receptor couples to a G protein in mammalian cell membranes
    FEBS letters, 1993
    Co-Authors: William Wisden, Eric M. Parker, Cathy D. Mahle, Darcy A. Grisel, Henry P. Nowak, Frank D. Yocca, Christian C. Felder, Peter H. Seeburg, Mark M. Voigt

    Abstract:

    A gene encoding a novel G protein-coupled 5-hydroxytryptamine (5-HT) Receptor, termed 5-HT5B, was cloned. The ligand binding profile of this Receptor is distinct from that of other cloned 5-HT Receptors. The 5-HT5B Receptor couples to a G protein in COS1 cell membranes; however, activation of the 5-HT5B Receptor does not appear to alter either cAMP accumulation or phosphoinositide turnover in a variety of fibroblast cell lines. In the rat brain, 5-HT5B gene expression occurs predominantly in the medial habenulae and hippocampal CA1 cells of the adult. Little expression is seen during embryonic development.

William Wisden – One of the best experts on this subject based on the ideXlab platform.

  • Cloning and characterization of the rat 5-HT5B Receptor : evidence that the 5-HT5B Receptor couples to a G protein in mammalian cell membranes
    FEBS letters, 1993
    Co-Authors: William Wisden, Eric M. Parker, Cathy D. Mahle, Darcy A. Grisel, Henry P. Nowak, Frank D. Yocca, Christian C. Felder, Peter H. Seeburg, Mark M. Voigt

    Abstract:

    A gene encoding a novel G protein-coupled 5-hydroxytryptamine (5-HT) Receptor, termed 5-HT5B, was cloned. The ligand binding profile of this Receptor is distinct from that of other cloned 5-HT Receptors. The 5-HT5B Receptor couples to a G protein in COS1 cell membranes; however, activation of the 5-HT5B Receptor does not appear to alter either cAMP accumulation or phosphoinositide turnover in a variety of fibroblast cell lines. In the rat brain, 5-HT5B gene expression occurs predominantly in the medial habenulae and hippocampal CA1 cells of the adult. Little expression is seen during embryonic development.