Nicotinic Acetylcholine Receptors

Nicotinic acetylcholine receptors (nAChRs) are found in the central and peripheral nervous system, muscle, and many other tissues of many organisms which respond to the neurotransmitter acetylcholine. These receptors belong to a superfamily of ligand-gated ion channels and are known to play key roles in synaptic transmission throughout the central nervous system. Many subtypes of nAChR are known to exist, composed of different combinations of subunits which in combination with their broad distribution throughout the central and peripheral nervous systems, enable them to play multiple, varied roles.

Fig. 1 Functional characterization of DB04763, DB08122 and pefloxacin on the α7nAChR

Here in Creative Bioarray, we provide target screening on nAChRs listed as below:

nAChR (α7) (CHRNA7)

Tissue-specific Location: CNS neurons and non-neuronal cells (placenta, endothelia, vascular smooth muscle).

Therapeutic target: inflammation, schizophrenia, and cognitive impairment.

nAChR (α4/β2) (CHRNA4/CHRNB2)

Tissue-specific location: predominates in the brain.

Disease: mutations in CHRNA4 are linked to seizure disorders such as frontal lobe epilepsy as well as a possible role in nicotinic addiction.

Reference

1. Smelt CLC, et al. Identification by virtual screening and functional characterisation of novel positive and negative allosteric modulators of the alpha7 nicotinic acetylcholine receptor. Neuropharmacology 2018; 139: 194–204.

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