Literature DB >> 2854054

Structure and functional expression of cloned rat serotonin 5HT-2 receptor.

D B Pritchett1, A W Bach, M Wozny, O Taleb, R Dal Toso, J C Shih, P H Seeburg.   

Abstract

A complementary DNA (cDNA) encoding a serotonin receptor with 51% sequence identity to the 5HT-1C subtype was isolated from a rat brain cDNA library by homology screening. Transient expression of the cloned cDNA in mammalian cells was used to establish the pharmacological profile of the encoded receptor polypeptide. Membranes from transfected cells showed high-affinity binding of the serotonin antagonists spiperone, ketanserin and mianserin, low affinity for haloperidol (a dopamine D2 receptor antagonist), 8-OH-DPAT as well as MDL-72222 and no detectable binding of [3H]serotonin. This profile is consonant with the 5HT-2 subtype of serotonin receptors. In agreement with this assignment, serotonin increased the intracellular Ca2+ concentration and activated phosphoinositide hydrolysis in transfected mammalian cells. The agonist also elicited a current flow, blocked by spiperone, in Xenopus oocytes injected with in vitro synthesized RNA containing the cloned nucleotide sequences.

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Year:  1988        PMID: 2854054      PMCID: PMC455123          DOI: 10.1002/j.1460-2075.1988.tb03308.x

Source DB:  PubMed          Journal:  EMBO J        ISSN: 0261-4189            Impact factor:   11.598


  32 in total

1.  Differential regulation of PI hydrolysis and adenylyl cyclase by muscarinic receptor subtypes.

Authors:  E G Peralta; A Ashkenazi; J W Winslow; J Ramachandran; D J Capon
Journal:  Nature       Date:  1988-08-04       Impact factor: 49.962

Review 2.  Molecular pharmacology and biology of 5-HT1C receptors.

Authors:  D Hoyer
Journal:  Trends Pharmacol Sci       Date:  1988-03       Impact factor: 14.819

3.  Molecular characterization of a functional cDNA encoding the serotonin 1c receptor.

Authors:  D Julius; A B MacDermott; R Axel; T M Jessell
Journal:  Science       Date:  1988-07-29       Impact factor: 47.728

4.  Receptor binding profile of R 41 468, a novel antagonist at 5-HT2 receptors.

Authors:  J E Leysen; F Awouters; L Kennis; P M Laduron; J Vandenberk; P A Janssen
Journal:  Life Sci       Date:  1981-03-02       Impact factor: 5.037

5.  [3H]Ketanserin (R 41 468), a selective 3H-ligand for serotonin2 receptor binding sites. Binding properties, brain distribution, and functional role.

Authors:  J E Leysen; C J Niemegeers; J M Van Nueten; P M Laduron
Journal:  Mol Pharmacol       Date:  1982-03       Impact factor: 4.436

6.  Ultrasonic vocalisations facilitate sexual behaviour of female rats.

Authors:  T K McIntosh; R J Barfield; L A Geyer
Journal:  Nature       Date:  1978-03-09       Impact factor: 49.962

7.  The genomic clone G-21 which resembles a beta-adrenergic receptor sequence encodes the 5-HT1A receptor.

Authors:  A Fargin; J R Raymond; M J Lohse; B K Kobilka; M G Caron; R J Lefkowitz
Journal:  Nature       Date:  1988-09-22       Impact factor: 49.962

8.  Cloning and expression of the human and rat m5 muscarinic acetylcholine receptor genes.

Authors:  T I Bonner; A C Young; M R Brann; N J Buckley
Journal:  Neuron       Date:  1988-07       Impact factor: 17.173

9.  DNA sequencing with chain-terminating inhibitors.

Authors:  F Sanger; S Nicklen; A R Coulson
Journal:  Proc Natl Acad Sci U S A       Date:  1977-12       Impact factor: 11.205

10.  High efficiency DNA-mediated transformation of primate cells.

Authors:  C Gorman; R Padmanabhan; B H Howard
Journal:  Science       Date:  1983-08-05       Impact factor: 47.728

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  65 in total

1.  "5-HT1R" or 5-HT1D sites? Evidence for 5-HT1D binding sites in rabbit brain.

Authors:  D Hoyer; H Lery; C Waeber; A T Bruinvels; J Nozulak; J M Palacios
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1992-09       Impact factor: 3.000

2.  Molecular structural basis of ligand selectivity for 5-HT2 versus 5-HT1C cortical receptors.

Authors:  P A Pierce; J Y Kim; S J Peroutka
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1992-07       Impact factor: 3.000

Review 3.  In vitro mutagenesis and the search for structure-function relationships among G protein-coupled receptors.

Authors:  T M Savarese; C M Fraser
Journal:  Biochem J       Date:  1992-04-01       Impact factor: 3.857

4.  Agonist/antagonist interactions with cloned human 5-HT1A receptors: variations in intrinsic activity studied in transfected HeLa cells.

Authors:  H W Boddeke; A Fargin; J R Raymond; P Schoeffter; D Hoyer
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1992-03       Impact factor: 3.000

Review 5.  The serotonin 5-HT1D receptor: a progress review.

Authors:  C Waeber; P Schoeffter; D Hoyer; J M Palacios
Journal:  Neurochem Res       Date:  1990-06       Impact factor: 3.996

Review 6.  Use of Xenopus oocytes for the functional expression of plasma membrane proteins.

Authors:  E Sigel
Journal:  J Membr Biol       Date:  1990-09       Impact factor: 1.843

Review 7.  The 5-HT1A receptor: an overview of recent advances.

Authors:  S el Mestikawy; A Fargin; J R Raymond; H Gozlan; M Hnatowich
Journal:  Neurochem Res       Date:  1991-01       Impact factor: 3.996

8.  RTA, a candidate G protein-coupled receptor: cloning, sequencing, and tissue distribution.

Authors:  P C Ross; R A Figler; M H Corjay; C M Barber; N Adam; D R Harcus; K R Lynch
Journal:  Proc Natl Acad Sci U S A       Date:  1990-04       Impact factor: 11.205

9.  The gastrointestinal prokinetic benzamide derivatives are agonists at the non-classical 5-HT receptor (5-HT4) positively coupled to adenylate cyclase in neurons.

Authors:  A Dumuis; M Sebben; J Bockaert
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1989-10       Impact factor: 3.000

10.  Two members of a distinct subfamily of 5-hydroxytryptamine receptors differentially expressed in rat brain.

Authors:  M G Erlander; T W Lovenberg; B M Baron; L de Lecea; P E Danielson; M Racke; A L Slone; B W Siegel; P E Foye; K Cannon
Journal:  Proc Natl Acad Sci U S A       Date:  1993-04-15       Impact factor: 11.205

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