Journal ArticleDOI
Influence of the 5-HT6 receptor on acetylcholine release in the cortex: pharmacological characterization of 4-(2-bromo-6-pyrrolidin-1-ylpyridine-4-sulfonyl)phenylamine, a potent and selective 5-HT6 receptor antagonist.
Claus Riemer,Edilio Borroni,Bernard Levet-Trafit,James R. Martin,Sonia Poli,Porter Richard Hugh Phillip,Michael Bös +6 more
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TLDR
A functional correlation between 5-HT(6) receptors and cholinergic neurotransmission could be shown, supporting the therapeutic potential of 5- HT( 6) receptors in the treatment of cognitive deficits.Abstract:
A small series of aryl pyridyl sulfones has been prepared and investigated for its 5-HT6 receptor binding properties. Thereof, pyrrolidinyl derivative 11 proved to be a very potent (pKi 9) and selective 5-HT6 receptor antagonist. By means of in vivo microdialysis in the frontal cortex and a passive avoidance paradigm, where 11 reversed a scopolamine induced retention deficit, a functional correlation between 5-HT6 receptors and cholinergic neurotransmission could be shown, supporting the therapeutic potential of 5-HT6 receptors in the treatment of cognitive deficits.read more
Citations
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Using the MATRICS to guide development of a preclinical cognitive test battery for research in schizophrenia.
TL;DR: There is a need for a "preclinical MATRICS" to develop a rodent test battery that is appropriate for drug development and outline an approach for translational research.
Journal ArticleDOI
The synthesis and coordination chemistry of 2,6-bis(pyrazolyl)pyridines and related ligands — Versatile terpyridine analogues
TL;DR: A review of the synthesis of 2,6-di(pyrazol-1-yl)pyridine and 3-yl pyridine can be found in this article.
Journal ArticleDOI
Serotonin receptors represent highly favorable molecular targets for cognitive enhancement in schizophrenia and other disorders.
TL;DR: Evidence is provided for and against the use of selective 5-HT receptor drugs as cognition enhancing agents for schizophrenia and other disorders, and it is likely that serotonergic drugs will soon be available as cognition enhances medications for disorders other than schizophrenia.
Journal ArticleDOI
A role for the 5-HT1A, 5-HT4 and 5-HT6 receptors in learning and memory
TL;DR: Evidence that compounds acting on serotonin receptors can have positive effects on learning and memory is reviewed, raising the possibility that such compounds could be developed as adjunct therapeutics with existing treatments to improvelearning and memory deficits, which are core symptoms of Alzheimer's disease, schizophrenia and depression.
Journal ArticleDOI
5-HT6 receptors: a novel target for cognitive enhancement.
TL;DR: Several clinically useful atypical antipsychotics and antidepressants have 5-HT6 affinity, but recently developed selective 5- HT6 receptor antagonists may present attractive, new therapeutic options for several types of disease states.
References
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Journal ArticleDOI
A novel rat serotonin (5-HT6) receptor: molecular cloning, localization and stimulation of cAMP accumulation.
Martial Ruat,Elisabeth Traiffort,J.M. Arrang,J. Tardivel-Lacombe,Jorge Diaz,R. Leurs,J.-C. Schwartz +6 more
TL;DR: 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.
Journal ArticleDOI
Immuno-localization of serotonin 5-HT6 receptor-like material in the rat central nervous system.
C. Gérard,Marie-Pascale Martres,Karine Lefèvre,Marie-Christine Miquel,Daniel Vergé,Laurence Lanfumey,E. Doucet,Michel Hamon,Salah El Mestikawy +8 more
TL;DR: 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.
Journal ArticleDOI
The 5-HT6 Receptor Antagonist SB-271046 Selectively Enhances Excitatory Neurotransmission in the Rat Frontal Cortex and Hippocampus
Lee A. Dawson,Huy Nguyen,Ping Li +2 more
TL;DR: The selective enhancement of excitatory neurotransmission by SB-271046 is demonstrated for the first time, and mechanistic evidence in support of a possible therapeutic role for 5-HT6 receptor antagonists in the treatment of cognitive and memory dysfunction is provided.
Journal ArticleDOI
Quantitative RT‐PCR distribution of serotonin 5‐HT6 receptor mRNA in the central nervous system of control or 5,7‐dihydroxytryptamine‐treated rats
C. Gérard,Salah El Mestikawy,Cécile Lebrand,Joëlle Adrien,Martial Ruat,Elisabeth Traiffort,Michel Hamon,Marie-Pascale Martres +7 more
TL;DR: The data showed that the 5‐HT6 receptor is not an autoreceptor, and exhibits probably no up regulation in postsynaptic target cells after the selective degeneration of serotoninergic projections.
Journal ArticleDOI
Characterization of Ro 04-6790 and Ro 63-0563: potent and selective antagonists at human and rat 5-HT6 receptors
TL;DR: In rats habituated to observation cages, Ro 04‐6790 produced a behavioural syndrome similar to that seen following treatment with antisense oligonucleotides designed to reduce the expression of 5‐HT6 receptors, suggesting that the compounds are neither agonists nor inverse agonists at the 5‐ HT6 receptor.
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The 5-HT6 Receptor Antagonist SB-271046 Selectively Enhances Excitatory Neurotransmission in the Rat Frontal Cortex and Hippocampus
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