Nicotinic Acetylcholine Receptor (nAChR) Screening Service

Nicotinic acetylcholine receptors, also known as nAChRs, are receptor polypeptides reacting to neurotransmitter acetylcholine and are found in many organisms, like the nervous system and muscle. To make research easier for scientists throughout the world, Creative Biolabs, ion channel screening specialists, provides trustworthy nAChR screening services.

Introduction of nAChR

nAChR, mainly distributed in the central nervous system, peripheral nervous system, and muscle, gains its name because nicotine and acetylcholine selectively bind to it. As a non-selective cation channel, nAChRs open and allow the sodium influx and potassium outflux when are agonists binding. Usually, nAChRs remain open till the agonist diffuses away. nAChRs are composed by 5 subunits surrounding a central pore symmetrically, and each subunit consists of four transmembrane domains, the N- and C-termini of which are positioned outside the cell. In vertebrates, different subunit combinations and expression locations divide the nAChRs into different forms. Muscle-type nAChRs are founded at the neuromuscular junction and have embryonic and adult forms, while neuronal-type nAChRs are divided into homomeric or heteromeric types based on the number of subunit types. nAChRs in particular subunit combinations are also permeable to calcium. nAChRs function in neural signal transmission, muscle contraction, and inflammatory process regulation. nAChR mutations may lead to chronic obstructive pulmonary disease, peripheral arterial disease, and lung cancer.

Fig.1 The structure of nAChR.Distributed under CC BY-SA 3.0, from Wiki, without modification.

nAChR Screening Service

Ion channels are crucial targets for the creation of novel therapeutic lead compounds. As an important ion channel target in mammals, nAChRs gain more and more attention because of their crucial role in many routine biological activities and disease development.

Several classical methodologies are employed in ligand discovery and development targeting nAChRs, like patch clamp. Patch clamp assays measuring ion fluxes and membrane potential changes across the cell membrane with precise resolution are common procedures in the initial screening process and lead optimization phase.

More improved, automated, and quicker screening approaches have evolved in recent years. The fluorescence-based assay and calcium-flux assay are examples of innovative test formats with high throughput, expanding the candidate scope dramatically and emitting labor-intensive and costly drawbacks of traditional methods. Aside from these high-throughput screening assay designs, medium/high throughput may now be performed with automated patch-clamp technologies and the most recent HTS apparatus for automated electrophysiological ion-flux assays to reflect more physiological and trustworthy results.

With its benefits of speed, affordability, and high throughput, virtual screening can also be taken into consideration as a method to your interested ligand discovery.

Fig.2 Diagram depicting variants of the patch clamp method. Distributed under Public Domain, from Wiki.

In mammals, 16 nAChR subunits from neuronal type and muscle type were discovered and divided into 4 subfamilies because of protein sequence similarity, marked as subfamily I, II, III, and IV. Constructing a suitable cell model helps your screening project win at the starting point.

Neuronal type

• Subfamily I, subunit α9
• Subfamily I, subunit α10
• Subfamily II, subunit α7
• Subfamily III-1, subunit α2
• Subfamily III-1, subunit α3
• Subfamily III-1, subunit α4
• Subfamily III-1, subunit α6
• Subfamily III-2, subunit β2
• Subfamily III-2, subunit β4
• Subfamily III-3, subunit β3
• Subfamily III-3, subunit α5

Muscle type

• Subfamily IV, subunit α1
• Subfamily IV, subunit β1
• Subfamily IV, subunit δ
• Subfamily IV, subunit γ
• Subfamily IV, subunit ε

Features of Our Service

• Off-the-shelf and customized nAChR cell lines
• Customized assay design and development
• High-quality, cost-effective screening services
• Fast reporting and comprehensive data analysis
• Reliable findings and excellent after-sales service

In order to expedite your crucial study development, Creative Biolabs, which has vast expertise in nAChR screening research, can offer both electrophysiological and non-electrophysiological nAChR screening on your interested nAChRs. Do not hesitate to contact us for additional information.

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

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

For Research Use Only. Not For Clinical Use.