HTR6 Membrane Protein Introduction

Introduction of HTR6

HTR6, encoded by HTR6 gene, is a member of the seven-transmembrane G protein-coupled receptor family, coupled with the G_s 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.

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

1. Amodeo D.A., et al. 5-HT6 receptor agonist EMD386088 impairs behavioral flexibility and working memory. Behavioural Brain Research. 2018, 349: 8-15. PubMed ID: 29715539
   
   

   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.

2. Hashemi-Firouzi N., et al. 5-Hydroxytryptamine receptor 6 antagonist, SB258585 exerts neuroprotection in a rat model of Streptozotocin-induced Alzheimer’s disease. Metabolic Brain Disease. 2018. PubMed ID: 29667108
   
   

   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.

3. Hu L., et al. Serotonin 5-HT6 receptors affect cognition in a mouse model of Alzheimer’s disease by regulating cilia function. Alzheimers Research & Therapy. 2017, 9(1):76. PubMed ID: 28931427
   
   

   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.

4. Lalut J., et al. Modulating 5-HT4 and 5-HT6 receptors in Alzheimer's disease treatment. Future Medicinal Chemistry. 2017, 9(8):781-795. PubMed ID: 28504917
   
   

   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.

5. Ferrero H., et al. Serotonin 5-HT6 receptor antagonists in Alzheimer's disease: therapeutic rationale and current development status. Cns Drugs. 2017, 31(1):19-32. PubMed ID: 27914038
   
   

   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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Reference

1. Benhamú B, et al. (2014). Serotonin 5-HT6 receptor antagonists for the treatment of cognitive deficiency in Alzheimer's disease. Journal of Medicinal Chemistry, 57(17), 7160-81.

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