Introduction of HTR6
HTR6, encoded by HTR6 gene, is a member of the seven-transmembrane G protein-coupled receptor family, coupled with the Gs alpha subunit. It is found in the central and peripheral nervous systems, involved in the mediation of excitatory and inhibitory neurotransmission. Now most studies are designed to investigate the characters of HTR6 acting as a potential therapeutic target for neurological disorders, such as Alzheimer's disease.
|Basic Information of HTR6|
|Protein Name||5-hydroxytryptamine receptor 6|
|Organism||Homo sapiens (Human)|
Function of HTR6 Membrane Protein
HTR6 is one of the several different receptors for 5-hydroxytryptamine (serotonin) which is a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activated receptor by interacting with serotonin promotes adenylate cyclase, resulting in the activation of cyclic AMP-dependent signaling pathway. It is reported that the receptor functions as a regulator of cholinergic neuronal transmission in the brain and is associated with neurological disorders, such as Alzheimer's disease, depression, schizophrenia, and epilepsy. Moreover, most studies have been identified that inhibition of HTR6 can relieve the impairments of cognitive, working memory and behavioral flexibility which is linked to Alzheimer's disease. Hence HTR6 can be used as a promising therapeutic target for treating neurological disorders. Recently more and more antidepressants and antipsychotic drugs targeting toward to HTR6 have been developed for neurological disorders treatment and they have a high affinity with HTR6.
Fig.1 HTR6 has been proposed as a promising drug target for cognition enhancement in AD. (Benhamú B, 2014)
Application of HTR6 Membrane Protein in Literature
The study indicates that the inhibition of 5-HT6 receptor may be an effective therapeutic strategy for relieving working memory and behavioral flexibility impairments associated with neuropsychiatric disorders such as Alzheimer's disease and schizophrenia.
The research identifies 5-HT6 antagonist SB258585 can relieve cognitive and behavioral impairments associated with Alzheimer's disease (AD) via suppressing the apoptosis of hippocampus.
The study suggests that 5-HT6 regulates the morphology and function of neuronal primary cilia which is linked to the axon initial segment (AIS) and axon alterations in Alzheimer's disease (AD) development. Hence 5-HT6 may be involved in the development of AD.
The review reports the recent studies in the understanding of this modulation as well as the medicinal chemistry of 5-HT6R or 5-HT4R ligands from synthesis to ongoing clinical trials.
In this review, authors describe the recent fundamental and clinical investigations about 5-HT6 receptor as a therapeutic target for cognitive and/or behavioral symptoms of Alzheimer's disease (AD). The conclusion is made that 5-HT6 receptor antagonists can reasonably be regarded as potential drug candidates for the treatment of AD.
HTR6 Preparation Options
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