The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors, abbreviated as AMPARs, are transmembrane sodium ion channels for fast synaptic transmission. To make research easier for scientists throughout the world, Creative Biolabs, ion channel screening specialists, provides a trustworthy AMPAR screening service.
AMPAR gains its name from artificial glutamate analog AMPA-mediated channel activation selectively and is a tetramer consisting of four kinds of subunits called GluA1-4. The majority of AMPARs are heterotetrameric, containing symmetric GluA2 dimer plus either GluA1, 3, or 4. Each subunit contains four transmembrane domains, together with the N terminal out of the cell and the C terminal in the cell. When the agonist binds to the extracellular binding site, the channel conformation changes and the pore is opened for ion transduction. If the GluA2 subunit exists, AMPARs will be impermeable to calcium. If not, AMPARs will be permeability to calcium, sodium, and potassium. After then, the channel may quickly become desensitized, which would cut off the current and block the pore. The rapid opening and closing of AMPARs empowers them to fast excitatory synaptic transmission in the central nervous system. Dysfunction of AMPARs is related to several acute and chronic neurological diseases, like stroke, Amyotrophic Lateral Sclerosis, and Huntington's diseases.
Fig.1 The structure of AMPAR. Distributed under CC BY-SA 3.0, from Wiki, without modification.
AMPARs are crucial for in synaptic transmission and plasticity, whose malfunctions are linked to numerous neurological and mental illnesses. It is intrinsically challenging to strike a balance between beneficial therapies and crippling adverse effects when trying to increase or decrease AMPAR activity. AMPAR screening provides a clue for finding ligands with custom expected effects.
There are various methods that can be chosen for your AMPAR screening projects. Different method combinations lead to the most trustworthy results for your research.
Approaches | In silico strategy | Non-electrophysiological strategy | Electrophysiological strategy | |
Examples | Virtual screening | Fluorescence-based assay | Automated patch clamp | Patch clamp |
Throughput | High | High | Low to mid | Low |
Results | Theoretically accurate | Less accurate | Physiologically accurate | |
Cost | Low | Mid | High | High |
Turnaround time | Fast | Mid | Slow | Slower |
Four separate subunit types are encoded by distinct genes in AMPARs. Establishing a cell model with correct expression and functional validation is a critical first step in AMPAR screening.
With a wealth of experience in AMPAR screening research, Creative Biolabs can expedite your vital study by doing various ion channel screening approaches or combinations on your interested AMPARs. Do not hesitate to contact us for more details.
In addition to AMPAR Screening, Creative Biolabs also provides you with the following ligand-gated channel screening services
For Research Use Only. Not For Clinical Use.