GSK598809

GSK598809 is a potent and highly selective dopamine D3 receptor antagonist developed by GSK (formerly GlaxoSmithKline) as an orally administered small molecule. It exhibits approximately 120-fold selectivity for the dopamine D3 receptor over the D2 receptor, with a Ki of 6.2 nM for D3 and 740 nM for D2[1][4]. The drug was investigated primarily for the treatment of substance-related disorders, including cocaine use disorder, smoking withdrawal, and eating disorders such as binge eating disorder[1][5]. Mechanistically, antagonism of the dopamine D3 receptor is thought to increase extracellular dopamine levels by inhibiting autoreceptor-mediated feedback inhibition on dopaminergic neurons[6]. Clinical studies have shown that single doses can achieve high occupancy of central D3 receptors in humans (72–89%), with side effects including headache and somnolence but minimal extrapyramidal symptoms or sedation[1][3]. Development appears to have reached phase 2 clinical trials in indications such as smoking cessation but has not progressed further or been reported recently[5][7].

Other names

GSK-598809GSK598809GSK 598809