HTR2A: A G Protein-Coupled Receptor for The Treatment of Psychiatric and Neurological Disorders

Target Name: HTR2A

NCBI ID: G3356

HTR2A: A G Protein-Coupled Receptor for The Treatment of Psychiatric and Neurological Disorders

Human Serotonin Receptor 2A (HTR2A) is a G protein-coupled receptor that plays a crucial role in the regulation of mood, anxiety, and pain perception. It is one of the most well-studied GPRs in the brain, and its dysfunction has been implicated in a wide range of psychiatric and neurological disorders. Despite its importance, the biology of HTR2A remains relatively well understood, and there is an urgent need for new treatments and biomarkers.

In this article, we will explore the biology of HTR2A and its potential as a drug target. We will discuss the current state of research on HTR2A, including its structure, function, and potential therapeutic interventions. We will also examine the potential utility of HTR2A as a biomarker for various psychiatric and neurological disorders.

Structure and Function

HTR2A is a G protein-coupled receptor that was identified in the late 1990s as a highly homophilic receptor for serotonin agonists.1 HTR2A is composed of an extracellular domain, a transmembrane region, and an intracellular domain. The extracellular domain consists of a N-terminus that is involved in the formation of a complex with a G protein, a catalytic center, and a C-terminus that is involved in the interaction with intracellular signaling pathways.2

The transmembrane region of HTR2A is composed of a single transmembrane alpha-helices that are involved in the formation of a complex with the extracellular domain of the receptor.3 The intracellular domain of HTR2A is composed of a single transmembrane alpha-helices that is involved in the interaction with intracellular signaling pathways.4

HTR2A is a potent receptor for serotonin agonists, with a high affinity for agonists at concentrations that are typically effective in clinical settings.5 HTR2A has been shown to play a role in the regulation of mood, anxiety, and pain perception, and is involved in the development of various psychiatric and neurological disorders.6

Despite its importance, the biology of HTR2A remains relatively well understood. The functions of HTR2A are regulated by a complex interplay of intracellular signaling pathways, including the action of neurotransmitters, ion channels, and intracellular signaling pathways.7 HTR2A has been shown to interact with a wide range of intracellular signaling pathways, including the modulation of neurotransmitter release by neurotransmitter agonists, the regulation of ion channels by ions, and the modulation of protein kinase activity by signaling molecules.8

The potential therapeutic applications of HTR2A as a drug target are vast. Given its importance in the regulation of mood, anxiety, and pain perception, HTR2A is a promising target for the treatment of various psychiatric and neurological disorders.9 For example, HTR2A has been shown to be involved in the development of depression, anxiety, and chronic pain, and may be a useful target for the development of new treatments for these disorders.10

Potential Biomarkers

HTR2A has the potential to serve as a biomarker for a wide range of psychiatric and neurological disorders. Given its involvement in the regulation of mood, anxiety, and pain perception, HTR2A may be a useful biomarker for the diagnosis and assessment of symptoms of these disorders.11 For example, HTR2A has been shown to be involved in the regulation of pain perception, and may be a useful biomarker for the assessment of pain severity in patients with chronic pain.12

In addition to its potential as a biomarker, HTR2A may also serve as a drug target in its own right. Given its importance in the regulation of mood, anxiety, and pain perception, HTR2A may be a useful target for the treatment of various psychiatric and neurological disorders.9 For example, HTR2A has been shown to be involved in the regulation of

Protein Name: 5-hydroxytryptamine Receptor 2A

Functions: G-protein coupled receptor for 5-hydroxytryptamine (serotonin) (PubMed:1330647, PubMed:18703043, PubMed:19057895). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and lysergic acid diethylamide (LSD) (PubMed:28129538). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors (PubMed:28129538). Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways (PubMed:28129538). Signaling activates phospholipase C and a phosphatidylinositol-calcium second messenger system that modulates the activity of phosphatidylinositol 3-kinase and promotes the release of Ca(2+) ions from intracellular stores (PubMed:18703043, PubMed:28129538). Affects neural activity, perception, cognition and mood (PubMed:18297054). Plays a role in the regulation of behavior, including responses to anxiogenic situations and psychoactive substances. Plays a role in intestinal smooth muscle contraction, and may play a role in arterial vasoconstriction

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