HTR1A Membrane Protein Introduction

Introduction of HTR1A

5-hydroxytryptamine receptor 1A (5-HT-1A or 5-HT1A), which in human is encoded by HTR1A gene, is a subtype of serotonin receptor (5-HT receptor) that binds the neurotransmitter serotonin (5-hydroxytryptamine, 5-HT). It is a G protein-coupled receptor (GPCR) that mediates inhibitory neurotransmission, coupled to the Gi protein. HTR1A has been found in several tissues of the central nervous system, including cerebral cortex, hippocampus, amygdala, septum, and raphe nucleus in high densities, while low amounts also exist in the basal ganglia and thalamus.

Function of HTR1A Membrane Protein

The binding of HTR1A and its ligand leads to a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors, such as adenylate cyclase. HTR1A, a member of beta-arrestin family, inhibits signaling via G proteins and mediates activation of alternative signaling pathways. HTR1A signaling inhibits adenylate cyclase activity and activates a phosphatidylinositol-calcium second messenger system that regulates the release of Ca²⁺ ions from intracellular stores. HTR1A is shown to be involved in the regulation of 5-hydroxytryptamine release and dopamine as well as 5-hydroxytryptamine metabolism. Studies have demonstrated that HTR1A plays a role in the regulation of dopamine and 5-hydroxytryptamine levels in the brain, and thus affecting neural activity, mood and behavior. Besides, it is also involved in the response to anxiogenic stimuli. Consequently, HTR1A functions as a receptor for various drugs and psychoactive substances.

Fig.1 Gα-specific signaling of the 5-HT1A receptor. (Albert, 2001)

Application of HTR1A Membrane Protein in Literature

1. Li X., et al. A behavioral mechanistic investigation of the role of 5-HT1A receptors in the mediation of rat maternal behavior. Pharmacol Biochem Behav. 2018, 169:16-26. PubMed ID: 29649502
   
   

   The results of this article suggested that stimulation of 5-HT1A receptors by 8-OH-DPAT impaired maternal care by partially interfering with the attentional processing or basal anxiety.

2. Vidal B., et al. ¹⁸F-F13640 preclinical evaluation in rodent, cat and primate as a 5-HT1A receptor agonist for PET neuroimaging. Brain Struct Funct. 2018, 223(6):2973-2988. PubMed ID: 29730825
   
   

   This study was carried out to propose the first preclinical evaluation of ¹⁸F-F13640, a 5-HT1A receptor agonist, since agonists could bind preferentially to the high-affinity state of receptors and it would be of great interest to develop agonist radioligands which could provide a measure of the functional 5-HT1A receptors in pathophysiological processes.

3. Zanderigo F., et al. In vivo relationship between serotonin 1A receptor binding and gray matter volume in the healthy brain and in major depressive disorder. Brain Struct Funct. 2018, 223(6):2609-2625. PubMed ID: 29550938
   
   

   The findings indicated a trend towards dissociation between major depressive disorder (MDD) and healthy controls (HCs) in the relationship of raphe 5-HT1A binding with postsynaptic gray matter volume (GMV). These results suggested that 5-HT1A receptors contributed to altered neuroplasticity in MDD, possibly via the effects predating depression onset.

4. Pillai R. L. I., et al. Relations between cortical thickness, serotonin 1A receptor binding, and structural connectivity: A multimodal imaging study. Hum Brain Mapp. 2018, 39(2):1043-1055. PubMed ID: 29323797
   
   

   Authors of this article posited a defect in the raphe may affect the posterior cingulate cortex (PCC) within the default mode network in major depressive disorder (MDD) through serotonergic fibers, resulting in an increased ruminative processing.

5. Ostrowska K., et al. 5-HT1A and 5-HT2A receptors affinity, docking studies and pharmacological evaluation of a series of 8-acetyl-7-hydroxy-4-methylcoumarin derivatives. Bioorg Med Chem. 2018, 26(2):527-535. PubMed ID: 29269256
   
   

   This article described the synthesis, docking studies and biological evaluation of a focused library of novel arylpiperazinyl derivatives of 8-acetyl-7-hydroxy-4-methylcoumarin.

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Reference

1. Albert P R. and Tiberi M. (2001). Receptor signaling and structure: insights from serotonin-1 receptors. Trends in Endocrinology & Metabolism. 12(10), pp.453-460.

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