HTR5A Membrane Protein Introduction

Introduction of HTR5A

5-hydroxytryptamine receptor 5A (HTR5A), alternatively called serotonin receptor 5A, is a multi-pass membrane protein that belongs to the 5-hydroxytryptamine receptor family. Only the HTR5A subtype is expressed in human brain and it is encoded by HTR5A gene. Within the CNS (central nervous system), HTR5A shows a relatively broad distribution in human brain, including the cerebral cortex, thalamus, hypothalamus, hippocampus, habenula, cerebellum, and spinal cord. The HTR5A receptor has been supposed to be functional in a native expression system.

Function of HTR5A Membrane Protein

The 5-hydroxytryptamine (5-HT, also known as neurotransmitter serotonin) has been implicated in a wide range of psychiatric conditions and also has vasoconstrictive and vasodilatory effects. HTR5A receptor functions as a receptor for 5-hydroxytryptamine and couples to G proteins, negatively influencing cAMP levels via Gi and Go. This receptor has been supposed to function in part through the regulation of intracellular Ca²⁺ mobilization. HTR5A has been shown to be functional in a native expression system. It also appears to act as a presynaptic serotonin autoreceptor. Several studies have investigated the contribution of HTR5A receptor polymorphisms to the risk of bipolar and unipolar depression. A selective HTR5A receptor antagonist has been identified and has been shown to decrease 5-carboxyamidotryptamine-induced inhibition of raphe neuronal cell firing in vitro and to increase 5-HT levels in prefrontal cortex in vivo, suggesting a role for the 5-HT5A receptor in the modulation of raphe 5-HT neuronal activity.

Fig.1 Schematic model involving presynaptic 5-HT heteroreceptors (red). (Vinkers, 2010)

Application of HTR5A Membrane Protein in Literature

1. Yamazaki M., et al. Functional mechanism of ASP5736, a selective serotonin 5-HT5A receptor antagonist with potential utility for the treatment of cognitive dysfunction in schizophrenia. Eur Neuropsychopharmacol. 2018, 28(5):620-629. PubMed ID: 29571967
   
   

   The results showed that ASP5736 might block the inhibitory 5-HT5A receptors on DAergic neurons in the VTA that projected to the mPFC, and interneurons in the mPFC, and thereby improved cognitive impairment by preferentially enhancing DAergic and GABAergic neurons in the mPFC.

2. Nikiforuk A., et al. The effects of a 5-HT5A receptor antagonist in a ketamine-based rat model of cognitive dysfunction and the negative symptoms of schizophrenia. Neuropharmacology. 2016, 105:351-360. PubMed ID: 26826431
   
   

   The observations of this study revealed that the preclinical efficacy of a strategy based on the blockade of 5-HT5A receptors against schizophrenia-like cognitive deficits and negative symptoms.

3. Avila-Rojas S.H., et al. Role of spinal 5-HT5A, and 5-HT1A/1B/1D, receptors in neuropathic pain induced by spinal nerve ligation in rats. Brain Res. 2015, 1622:377-85. PubMed ID: 26168890
   
   

   This article showed that 5-HT5A receptors reduced pain processing in the spinal cord and that 5-HT and 5-CT reduced neuropathic pain through activation of 5-HT5A and 5-HT1A/1B/1D receptors.

4. Lopez-Esparza S., et al. Expression of hippocampal serotonin receptors 5-HT2C and 5-HT5A in a rat model of diet-induced obesity supplemented with tryptophan. Int J Dev Neurosci. 2015, 42:80-5. PubMed ID: 25720309
   
   

   The findings of this study indicated that 5-HT may facilitate nociception and intensified OAA (arm-induced antinociception), respectively, at 5-HT1A and 5-HT2C receptors located in the amygdala of mice.

5. Vidal-Cantú G.C., et al. Role of 5-HT5A and 5-HT1B/1D receptors in the antinociception produced by ergotamine and valerenic acid in the rat formalin test. Eur J Pharmacol. 2016, 781:109-16. PubMed ID: 27068146
   
   

   The findings suggested that variations of the two serotonin receptors subtypes supported their potential roles in obesity.

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Reference

1. Fink K B and Manfred G. (2007). 5-HT receptor regulation of neurotransmitter release. Pharmacological reviews. 59(4):360-417.

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