5-ht5A receptors as a therapeutic target.

@article{Thomas20065ht5ARA,
  title={5-ht5A receptors as a therapeutic target.},
  author={David R. Thomas},
  journal={Pharmacology \& therapeutics},
  year={2006},
  volume={111 3},
  pages={
          707-14
        }
}
The 5-ht5A receptor is enigmatic among 5-HT receptors since, although the human receptor was cloned in 1994, until recently, very little has been learnt about the function of the receptor in native tissues. Findings from 5-ht5A receptor mRNA localisation and immunolabelling studies have revealed widespread expression in the CNS, and have provided pointers to the potential functional role(s) of the receptor. The expression of the 5-ht5A receptor in raphe nuclei and in higher brain areas, such as… Expand
Recent Advances on the 5-HT5A, 5-HT6 and 5-HT7 Receptors
TLDR
The diversity of structures reported for this receptor indicates continued interest in the development of selective 5-HT 7 receptor ligands with suitable drug-like properties for pre-clinical validation. Expand
Functional mechanism of ASP5736, a selective serotonin 5-HT5A receptor antagonist with potential utility for the treatment of cognitive dysfunction in schizophrenia
TLDR
The hypothesis that ASP5736 might block the inhibitory 5-HT5A receptors on DAergic neurons in the VTA that project to the mPFC, and interneurons in the mFFC,and thereby improve cognitive impairment by preferentially enhancing DAergic and GABAergic neuron in themPFC is supported. Expand
Novel 5-HT5A receptor antagonists ameliorate scopolamine-induced working memory deficit in mice and reference memory impairment in aged rats.
TLDR
Treatment with 5-HT5A receptor antagonists might be broadly effective for cognitive impairment associated with not only schizophrenia but also dementia, as indicated by results of evaluated the chemically diverse, potent and brain-penetrating 5- HT5A receptors in rodent models of cognitive dysfunction associated with dementia. Expand
Serotonin receptors - from molecular biology to clinical applications.
TLDR
The present review describes the different populations and nomenclature of recently discovered 5-HT receptors and their pharmacological relevance. Expand
Modulation of the Serotonergic Receptosome in the Treatment of Anxiety and Depression: A Narrative Review of the Experimental Evidence
TLDR
This review presents the experimental evidence of the modulation of the “serotonergic receptosome” in the treatment of anxiety and depression, as well as demonstrating state-of-the-art research related to phytochemicals and these disorders. Expand
ASP5736, a novel 5-HT5A receptor antagonist, ameliorates positive symptoms and cognitive impairment in animal models of schizophrenia
TLDR
It is suggested that ASP5736 is a novel and potent 5-HT5A receptor antagonist that not only ameliorates positive-like symptoms but also cognitive impairments in animal models of schizophrenia, without adverse effects. Expand
Serotonin and molecular neuroimaging in humans using PET
TLDR
This review aims at illustrating the distribution and summarizing the main functions of the serotonin (5-hydroxytryptamin, 5-HT) receptors as well as the serotonin transporter, the vesicular monoamine transporter 2, monoamine oxidase type A and5-HT synthesis in the human brain. Expand
5-HT receptors and reward-related behaviour: A review
TLDR
It is concluded that the actions of 5-HT in reward are receptor subtype-dependent (and thus should not be generalized) and that all studied subtypes appear to have a unique profile which is determined by content. Expand
The effects of a 5-HT5A receptor antagonist in a ketamine-based rat model of cognitive dysfunction and the negative symptoms of schizophrenia
TLDR
The present study suggests the preclinical efficacy of a strategy based on the blockade of 5-HT5A receptors against schizophrenia-like cognitive deficits and negative symptoms and the utility of this receptor as a target for improvement of cognitive and social dysfunctions warrants further studies. Expand
The blockade of the serotoninergic receptors 5-HT5A, 5-HT6 and 5-HT7 in the basolateral amygdala, but not in the hippocampus facilitate the extinction of fear memory
TLDR
Investigation of the role of serotoninergic receptors in the CA1 region of the hippocampus and the BLA region in the extinction of contextual fear conditioning shows that the infusion immediately after extinction training of 5-HT5A, 5- HT6 and5-HT7 antagonists, and 3 h after extinctionTraining of5- HT5A and 5-ht7 antagonists in theBLA region, but not in CA1, facilitates theinction of CFC memory. Expand
...
1
2
3
4
5
...

References

SHOWING 1-10 OF 63 REFERENCES
5-HT7 receptors.
TLDR
Findings suggest that 5-HT(7) receptor-selective ligands might prove therapeutically useful for the treatment of psychiatric disorders and that the receptor may play a role in other CNS disorders including, anxiety, cognitive disturbances and also migraine probably via both peripheral and central mechanisms. Expand
A review of central 5-HT receptors and their function
TLDR
A number of 5-HT receptor ligands are currently utilised, or are in clinical development, to reduce the symptoms of CNS dysfunction and the functional responses attributed to each receptor in the brain are reviewed. Expand
Localization of 5-ht5A receptor-like immunoreactivity in the rat brain
TLDR
Interestingly, 5-ht(5A)-like immunoreactivity showed a predilection for the suprachiasmatic nucleus, suggesting its possible role in the regulation of circadian rhythms, a function previously ascribed to 5-HT(1A) and 5- HT(7) receptors. Expand
5-HT5 receptors.
  • D. Nelson
  • Chemistry, Medicine
  • Current drug targets. CNS and neurological disorders
  • 2004
TLDR
The 5- HT(5) receptors remain as two of the least studied and understood of the 5-HT receptor subtypes. Expand
The mouse 5HT5 receptor reveals a remarkable heterogeneity within the 5HT1D receptor family.
TLDR
The results demonstrate that the 5HT1D receptors constitute a heterogeneous family of receptors with distinct intracellular signalling properties and expression patterns, and are a distant relative of all previously identified 5‐HT receptors. Expand
Distribution of the 5-HT5A serotonin receptor mRNA in the human brain.
TLDR
The regional distribution and cellular localization of 5-HT5A receptor mRNA in human brain sections from autopsy samples by in situ hybridization histochemistry was studied to obtain anatomical information which might be useful in formulating hypotheses on possible functions subserved by this receptor in the central nervous system (CNS). Expand
The potential utility of 5-HT1A receptor antagonists in the treatment of cognitive dysfunction associated with Alzheimer s disease.
TLDR
Receptor blockade by a 5-HT1A receptor antagonist appears to enhance activation and signaling through heterosynaptic neuronal circuits known to be involved in cognitive processes and, as such, represents a novel therapeutic approach to the treatment of cognitive deficits associated with Alzheimer s disease and potentially other disorders with underlying cognitive dysfunction. Expand
Identification of one of the least well understood 5‐HT receptors (5‐ht5A) in the spinal cord
  • A. Ramage
  • Biology, Medicine
  • The Journal of comparative neurology
  • 2004
TLDR
The localization of one of the least well understood 5-HT receptors, the 5-ht5A receptor, in the spinal cord is reported, for the first time, and the authors conclude that these receptors may be involved in central motor control, somatosensory (nociception), and autonomic functions. Expand
Mouse 5-hydroxytryptamine5A and 5-hydroxytryptamine5B receptors define a new family of serotonin receptors: cloning, functional expression, and chromosomal localization.
TLDR
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. Expand
Localization of 5-HT2A, 5-HT3, 5-HT5A and 5-HT7 receptor-like immunoreactivity in the rat cerebellum
TLDR
The data relate serotonin receptor subtypes to specific cerebellar cell types and may contribute to the elucidation of serotonergic actions in the cerebellum. Expand
...
1
2
3
4
5
...