A novel rat serotonin (5-HT6) receptor: molecular cloning, localization and stimulation of cAMP accumulation.

  title={A novel rat serotonin (5-HT6) receptor: molecular cloning, localization and stimulation of cAMP accumulation.},
  author={M. Ruat and E. Traiffort and J. Arrang and J. Tardivel-Lacombe and J. D{\'i}az and R. Leurs and J. Schwartz},
  journal={Biochemical and biophysical research communications},
  volume={193 1},
Using a strategy based upon nucleotide sequence homology and starting from the sequence of the rat histamine H2 receptor (Ruat et al., Biochem. Biophys. Res. Commun. 1991, 179, 1470-1478), we have cloned a rat cDNA encoding a functional serotonin receptor (5-HT6). Its coding sequence corresponds to a glycoprotein of 436 amino acids displaying significant homology with other cloned monoaminergic receptors, e.g., various serotonin receptors. Genomic analysis of its gene indicated the presence of… Expand
5-HT4, 5-HT6, 5-HT7; molecular pharmacology of adenylate cyclase stimulating receptors
The most recent subset of receptors for serotonin to be cloned are those that couple to the stimulation of adenylate cyclase activity, and these subtypes, although sharing a common signal transduction pathway, are remarkably divergent in their amino acid sequences, distribution in the brain and pharmacological properties. Expand
Genomic organisation and functional expression of the gene encoding the human serotonin 5-HT2C receptor.
Membranes prepared from NIH 3T3 cells stably expressing the 5-HT2C receptor cDNA displayed a single population of high affinity sites for the antagonist [3H]mesulergine and binding by ligands indicated a pharmacological similarity of these binding sites with porcine and rat choroid plexus 5- HT2C receptors. Expand
Cloning, Characterization, and Chromosomal Localization of a Human 5‐HT6 Serotonin Receptor
Comparison of genomic and cDNA clones for the human 5‐HT6 receptor reveals an RsaI restriction fragment length polymorphism within the coding region, suggesting that these may be closely linked. Expand
Characterization of 5-ht6 receptor and expression of 5-ht6 mRNA in the rat brain during ontogenetic development
The hypothesis that 5-ht6 receptors may correspond to an important target for atypical antipsychotics and reveal an original pharmacological profile for this receptor is confirmed and its role in the early growth process involving the serotonergic system is suggested. Expand
Immuno-localization of serotonin 5-HT6 receptor-like material in the rat central nervous system
The relative abundance of 5-HT6 receptor-like immunoreactivity in extrapyramidal and limbic areas suggests that 5- HT6 receptors may participate in the serotoninergic control of motor function and mood-dependent behavior, respectively. Expand
Identification of a human 5-HT6 receptor variant produced by alternative splicing.
Experiments performed using a degenerate PCR approach from human caudate cDNA revealed a 5-HT6 receptor clone with a 289 bp deletion of the region coding for transmembrane IV through the third intracellular loop and a truncated protein containing 10 unique amino acids at its carboxyl end. Expand
Functional characteristics of heterologously expressed 5-HT receptors.
An overview of all cloned 5-HT receptor subtypes belonging to the superfamily of G-protein-coupled receptors with specific emphasis on the pharmacological and signaling properties of the receptors upon expression in several heterologous expression systems is given. Expand
Differences in the central nervous system distribution and pharmacology of the mouse 5-hydroxytryptamine-6 receptor compared with rat and human receptors investigated by radioligand binding, site-directed mutagenesis, and molecular modeling.
Molecular modeling of the receptor and docking of selective and nonselective compounds was undertaken to elucidate the ligand receptor interactions and predicted the binding pocket was predicted to be different in the mouse compared with rat and human 5-HT6 receptors. Expand
Molecular Biology and Genomic Organization of G Protein-Coupled Serotonin Receptors
This chapter summarizes naturally occurring variation in serotonin receptor sequences, which vary by species and by class and subclass and are further modified from their canonical sequences by RNA editing, alternative splicing, and the existence of single-nucleotide polymorphisms. Expand
Antibodies and Antisense Oligonucleotide for Probing the Distribution and Putative Functions of Central 5-HT6Receptors
Infusion with an antisense oligonucleotide for 3–4 days resulted in decreased 5-HT6receptor-like immunostaining of the nucleus accumbens and anxiogenic behaviours in the social interaction and elevated plus maze tests. Expand