N-methyl-D-aspartate (NMDA) Receptor Screening Service

N-methyl-D-aspartate receptors, abbreviated as NMDA receptors, are predominantly a kind of Ca²⁺ channel distributed in neurons. Creative Biolabs can provide trustworthy NMDA receptor screening services to scientists all around the world to help them with their study of finding promising NMDA receptor modulators based on our well-established ion channel screening platform.

Introduction of NMDA Receptor

NMDA highly selectively binds and activates NMDA receptors as a member of ionotropic glutamate receptors. Once the NMDA receptor is activated, the ion channel is opened, showing nonselective cation transduction in sufficiently depolarized neurons. Ligand binding gates the open and close states of this ion channel via the ligand-binding domain located in the extracellular domain. Glycine or D-serine and glutamate function as ligands based on the subunit composition of the NMDA receptor. Typical NMDA receptors are heterotetramers composed by different subunits GluN1, GluN2, and GluN3 from three gene families known as GRIN1, GRIN2, and GRIN3, respectively. Two GluN1 subunits plus two same types of GluN2 subunits compose the canonical diheteromeric NMDA receptors, while two GluN1 subunits plus two different types of GluN subunits or four GluN subunits from 3 different gene families consist of triheteromeric NMDA receptors. NMDA receptor-mediated Ca²⁺ flux is important in synaptic plasticity in cell learning and memory, and overactivation of NMDA receptor results in excitotoxicity, further involved in some neurodegenerative disorders such as Huntington's disease and Parkinson's disease.

Fig.1 The structure of the human NMDA receptor. Distributed under CC BY-SA 4.0, from Wiki, without modification.

NMDA Receptor Screening Service

As a ligand-gated ion channel, NMDA receptors play a critical role in various physiological functions, especially in neural activity. Excitotoxicity of NMDA receptors is caused by overactivation. There is not surprising that a ligand will be a spotlight if it can block the NMDA receptor from overactivation while keeping physiological activity. NMDA receptor screening paves a path for discovering the unknown stars in the NMDA receptor-associated pharmacological research and disease treatment.

Usually, NMDA receptor screening starts with a high-throughput non-electrophysiological strategy like fluorescence-based assay, together with the verified custom cell models and client-interested compound library. Fluorescence-based assays enable cells to reflect the tiny intracellular calcium concentration change via fluorescence signals monitored by automated machines, which quickly narrows down the scope of promising candidates.

Next, patch clamp-leading electrophysiological methods can be used to depict the reliable and physiologically meaningful data of ligand function, which further confirms the ligand effects at the physiological cell level. Electrophysiological methods can also be directly used when you have fewer candidates to be tested at the beginning. Data from electrophysiological methods is more real but low-throughput.

Fig.2 Fluorescence-based assay involved screening found promising candidates on the NMDA receptor cell model.¹

In mammals, NMDA receptors have different subunits, as described below. Construction of suitable NMDA receptor cell models will greatly succeed your entire project at initial.

• GRIN1 family, subunit GluN1
• GRIN2 family, subunit GluN2A
• GRIN2 family, subunit GluN2B
• GRIN2 family, subunit GluN2C
• GRIN2 family, subunit GluN2D
• GRIN3 family, subunit GluN3A
• GRIN3 family, subunit GluN3B

Features of Our Service

• Rich experience in custom cell model construction and ion channel screening
• Customized assay strategy and tailored assay development
• Quality-guaranteed one-stop service but cost-saving
• Comprehensive data interpretation and best after-sale service

Creative Biolabs, with considerable expertise in ligand-gated channel screening research, can conduct both electrophysiological assays and non-electrophysiological screenings on your desired NMDA receptors and corresponding cell models, accelerating your vital research development. Do not hesitate to contact us for additional information.

In addition to NMDA Receptor Screening, Creative Biolabs also provides you with the following ligand-gated channel screening services

• CNG Channel Screening
• nAChR Screening
• GABA_AR Screening
• AMPAR Screening
• P2X Receptor Screening
• TRP Channel Screening
• Calcium-activated Channel Screening
• Sodium-activated Channel Screening

Reference

1. Guo, Hongqiu, et al. "A NMDA-receptor calcium influx assay sensitive to stimulation by glutamate and glycine/D-serine." Scientific reports 7.1 (2017): 11608. Distributed under Open Access license CC BY 4.0. The image was modified by extracting and using only Part C-D of the original image.

For Research Use Only. Not For Clinical Use.