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QuickView for 5-Hydroxytryptamine 6 receptor (biogroup)
- 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.
- Taxonomy/Path:
- InterPro : G protein-coupled receptor, rhodopsin-like / 5-Hydroxytryptamine 6 receptor
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