Characterization of 5-HT₃ Receptors

Creative Bioarray is committed to revealing the structure of 5-HT₃ receptors with higher resolution and helping clients analyze their expression patterns and binding sites, providing valuable information for understanding the relationship between the structure and function of 5-HT₃ receptors and studying their (patho)physiology correlation.

Introduction

5-Hydroxyamine type-3 (5-HT₃) receptors are members of the Cys-loop family of ligand-gated ion channels, which exist in the peripheral and central nervous system and mediate neuronal depolarization and excitation. The 5-HT3A and 5-HT3B subunits are usually components of 5-HT₃ receptors with many different properties, and a variety of compounds can regulate receptor activity. Additional HTR3C, HTR3D, and HTR3E genes were reported to expand the potential for molecular diversity within this family.

The development of cryo-electron microscopy (Cryo-SEM) technology has brought biochemistry into a new era. Using real cell membrane cryo-electron microscopy, the high-resolution three-dimensional fine structure of the serotonin 5-HT₃ receptors has been resolved. At present, much is known about the structure and function of the 5-HT₃ receptors, but there are still many difficulties and disputes. A deeper understanding of the structure, function, and regulatory mechanism of 5-HT₃ receptors will help to analyze a series of clinical symptoms involving 5-HT₃ receptors and accelerate the design of more selective and effective potential therapies.

Fig. 1 A homology model of the 5-HT₃A receptor binding domain, showing 2 of the 5 subunits. (Barnes, 2009)

Our Services

We help our clients analyze the structure and function of 5-HT₃ receptors through various technologies. Our services include but not limited to:

• Structural analysis of 5-HT₃ receptors. Through X-ray crystallography, Cryo-SEM, and other technologies, combined with optimized sample processing and experimental methods, we help our clients analyze the structures of 5-HT₃ receptors in different functional states, including:
• The inhibited antagonist-bound closed conformation.
• The open-pore state and putative pre-active state in the presence of serotonin.
• The putative pre-active state in the presence of serotonin and allosteric modulators.
• Localization and expression analysis of 5-HT₃ receptors. We help clients map the distribution of 5-HT₃ receptors expression in the central nervous system using various radioligands, oligonucleotides, and antibodies.
• Model generation, such as the structural model of extracellular N-terminal domain of 5-HT₃ receptors.
• Characterization of the ligand-binding site of 5-HT₃ receptors through multiple methods, such as electrophysiology, radioligand binding, and immunochemistry.

Applications

• Research on the mechanism of agonist recognition at the binding site
• Research on the mechanism of ion permeation and selectivity
• Research on the relationship between structure and function

Creative Bioarray has accumulated a lot of successful experience in the field of ion channel analysis. We have the strength to provide our clients with high-quality 5-HT₃ receptor characterization services and deliver scientific experimental data in a short period of time that deepens the knowledge of the receptors' gating mechanism and the molecular basis of their structure and function. If you are interested in our services, please contact us for more details.

Reference

1. Barnes, N. M.; et al. The 5-HT₃ receptor–the relationship between structure and function. Neuropharmacology, 2009, 56(1): 273-284.