Discussion

Evidence suggests that the activation of the muscarinic acetycholine receptors (mAChRs) in the central nervous system (CNS) may have therapeutic benefit in the treatment of a number of CNS disorders. The use of non-selective agonists is limited due to un-desirable peripheral side effects. One approach to overcome this issue is to identify compounds that selectively positively modulate the M4 mAChR subtype via an allosteric binding site. Here we describe the use of backscattering interferometry, a label free assay technology, to investigating the nature of modulator binding and its co-operative effects upon the binding of the natural ligand acetylcholine to the M4 mAChR.