NS9283

NS9283 is a **selective positive allosteric modulator** of the (α4)3(β2)2 subtype of **nicotinic acetylcholine receptors (nAChRs)**. It acts at the α4-α4 interface of the receptor, increasing the **potency of acetylcholine (ACh)-evoked currents** without significantly altering the maximal efficacy or desensitization kinetics of the receptor. NS9283 is notable for its stoichiometry-selective activity—it potentiates receptors containing three α4- and two β2-subunits but not the (α4)2(β2)3 subtype. Mechanistically, it slows deactivation kinetics of the receptor, shifting the concentration–response curve to the left and enhancing synaptic responses. Preclinical experiments have shown NS9283 can improve cognitive function in animal models and modulate sensory information processing, suggesting therapeutic potential in neurological diseases linked to α4β2 nAChRs, such as Alzheimer's disease and possibly as an adjunct therapy in Parkinson's disease for L-DOPA-induced dyskinesias. NS9283 was developed by NeuroSearch[1][2][3][4][5][7].

Other names

3-(3-pyridyl)-5-(3-cyanophenyl)-1,2,4-oxadiazole