ARN25657 is a dual regulator of D3R/GSK-3beta. It demonstrates partial agonist activity at the D3 receptor (EC50 = 15.2 nM, Ki = 1.5 nM) alongside potent inhibitor activity against GSK-3beta (IC50 = 19.3 nM). ARN25657 shows excellent GSK-3beta selectivity over FYN, PKA, and CDK5/p35. It inhibits P-gp-mediated efflux of acetoxymethyl calcein, enhancing in vitro ADME properties while maintaining balanced dual-target distribution. ARN25657 is applicable in the study of bipolar disorder and related neuropsychiatric conditions.
Target:
GSK-3|||Dopamine Receptor|||P-gp|||PKA
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