5-HT6 receptor The 5HT6 receptor is a subtype of 5HT receptor that binds the endogenous neurotransmitter serotonin . It is a G protein-coupled receptor that is coupled to Gs and mediates excitatory neurotransmission . HTR6 denotes the human gene encoding for the receptor.Distribution The 5HT6 receptor is expressed almost exclusively in the brain . It is distributed in various areas including, but not limited to, the olfactory tubercle , cerebral cortex , nucleus accumbens , striatum , caudate nucleus , hippocampus , and the molecular layer of the cerebellum . Based on its abundance in extrapyramidal , limbic , and cortical regions it can be suggested that the 5HT6 receptor plays a role in functions like motor control , emotionality , cognition , and memory .Function Blockade of central 5HT6 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 5HT6 receptors also facilitates dopamine and norepinephrine release in the frontal cortex , while stimulation has the opposite effect.Despite the 5HT6 receptor having a functionally excitatory action, it is largely co-localized with GABAergic neurons and therefore produces an overall inhibition of brain activity . In parallel with this, 5HT6 antagonists are hypothesized to improve cognition, learning, and memory. Agents such as latrepirdine , idalopirdine , and intepirdine were evaluated as novel treatments for Alzheimer's disease and other forms of dementia . However, phase III trials of latrepirdine, idalopirdine, and intepirdine have failed to demonstrate efficacy. 5HT6 antagonists have also been shown to reduce appetite and produce weight loss , and as a result, PRX-07034 , BVT-5,182, and BVT-74,316 are being investigated for the treatment of obesity .As a drug target for agonists Recently, the 5HT6 agonists WAY-181,187 and WAY-208,466 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. Additionally, indirect 5HT6 activation may play a role in the therapeutic benefits of serotonergic antidepressants like the selective serotonin reuptake inhibitors and tricyclic antidepressants .Ligands A large number of selective 5HT6 ligands have now been developed.Agonists Full agonists 2-Ethyl-5-methoxy-N,N-dimethyltryptamine WAY-181,187 WAY-208,466 N -imidazothiazole-5-sulfonamide : K i = 4.5nM, EC50 = 0.9nM, Emax = 98% E-6837 - Full agonist at human 5HT6 receptorsPartial agonists E-6801 E-6837 - partial agonist at rat 5-HT6 receptors. Orally active in rats, and caused weight loss with chronic administration EMD-386,088 - potent partial agonist but non-selective LSD - Emax = 60% ALX-1161 AVN-211 BVT-5182 BVT-74316 Cerlapirdine - selective EGIS-12233 - mixed 5HT6 / 5HT7 antagonist Idalopirdine - selective Intepirdine - selective antagonist Landipirdine Latrepirdine and analogues MS-245 PRX-07034 SB-258,585 SB-271,046 SB-357,134 SB-399,885 Ro 04-6790 Ro-4368554 Atypical antipsychotics WAY-255315 / SAM-315: Ki = 1.1 nM , IC50 = 13 nM Rosa rugosa extractGenetics in the HTR6 gene are associated with neuropsychiatric disorders . For example, an association between the C267T polymorphism and Alzheimer's disease has been shown. Others have studied the polymorphism in relation to Parkinson's disease .
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