Protein Domain : IPR002232

Type:  Family Name:  5-Hydroxytryptamine 6 receptor
Description:  5-hydroxytryptamine (5-HT) or serotonin, is a neurotransmitter that it is primarily found in the gastrointestinal (GI) tract, platelets, and in the central nervous system (CNS). It is implicated in a vast array of physiological and pathophysiological pathways. Receptors for 5-HT mediate both excitatory and inhibitory neurotransmission, and modulate the release of many neurotransmitters including glutamate, GABA, dopamine, epinephrine/norepinephrine, and acetylcholine, as well as many hormones, including oxytocin, prolactin, vasopressin and cortisol. In the CNS, 5-HT receptors can influence various neurological processes, such as aggression, anxiety and appetite and, as a, result are the target of a variety of pharmaceutical drugs, including many antidepressants, antipsychotics and anorectics []. The 5-HT receptors are grouped into a number of distinct subtypes, classified according to their antagonist susceptibilities and their affinities for 5-HT. With the exception of the 5-HT3 receptor, which is a ligand-gated ion channel [], all 5-HT receptors are members of the rhodopsin-like G protein-coupled receptor family [], and they activate an intracellular second messenger cascade to produce their responses. 5-HT6 receptors are positively coupled to adenylyl cyclase. They are expressed almost exclusively in the brain [] and prominently expressed in the caudate nucleus [, , ]. Based on their abundance in extrapyramidal, limbic and cortical regions of the brain, it has been suggested that the 5-HT6 receptors play a role in functions like motor control, emotionality, cognition and memory [, , ]. Blockade of central 5-HT6 receptors has been shown to increase glutamatergic and cholinergic neurotransmission in various brain areas [, , ], whereas activation enhances GABAergic signaling in a widespread manner []. Antagonism of 5-HT6 receptors also facilitates dopamine and norepinephrine release in the frontal cortex [, ], while stimulation has the opposite effect []. 5-HT6 receptors have high affinity for several typical and atypical antipsychotic agents, including clozapine, olanzapine fluperlapine and seroquel [, ]. This attribute has led to speculation of potential involvement of the 5-HT6 receptor in the pathogenesis of psychiatric disorders. 5-HT6 receptor antagonists have been demonstrated to be active in rodent models of depression, anxiety and obsessive-compulsive disorder, and such agents may be useful treatments for these conditions [, ]. There is also some evidence of enhanced retention of spatial learning following treatment with such compounds [, ]. However, it should be noted that the rodent brain has a notably different regional pattern of 5-HT6 receptor expression in comparison to humans, and little data has been generated in actual clinical populations. Short Name:  5HT6_rcpt

0 Child Features

0 Contains

1 Cross References

Identifier
PR01102

0 Found In

3 GO Annotations

GO Term Gene Name
GO:0004993 IPR002232
GO:0007186 IPR002232
GO:0016021 IPR002232

3 Ontology Annotations

GO Term Gene Name
GO:0004993 IPR002232
GO:0007186 IPR002232
GO:0016021 IPR002232

1 Parent Features

DB identifier Type Name
IPR000276 Family G protein-coupled receptor, rhodopsin-like

0 Proteins

17 Publications

First Author Title Year Journal Volume Pages PubMed ID
            18476671
            11989819
            7908055
            8522988
            10780993
            11682249
            1522329
            17625499
            18625457
            14618683
            14965245
            8389146
            9037500
            10432491
            20217056
            11489457
            11163639