Abstract
Nicotinic acetylcholine receptors (nAChR) are ligand gated cation channels that are opened by agonists like Acetylcholine and Nicotine. They are widely distributed in neurons all over central nervous system, where they are mainly found at postsynaptic locations of cholinergic nerve endings.The most abundant homomeric nicotinic acetylcholine receptors in the mammalian brain are the pentameric alpha7 nAChRs which consist of five alpha7 subunits. Each subunit provides an orthosteric low affinity binding site for its endogenous ligand, acetylcholine. Several lines of evidence suggest a link between the alpha7 neuronal nicotinic acetylcholine receptor and brain disorders including schizophrenia, Alzheimer's disease, and traumatic brain injury. Alpha 7 receptors are also a target for non-CNS indications like diabetes and asthma.View Large Image | View Hi-Res Image | Download PowerPoint SlideHere we show the results of the screen of allosteric modulators on alpha 7 receptors. High parallelization without a compromise in data quality combined with fast and accurate solution exchange allows characterization of many compounds. A second analysis at physiological temperatures showed a pronounced effect on the allosteric modulation.
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