GSK598809 (GSK-598809) is a potent, selective, CNS penetrant and orally bioavailable dopamine D3 receptor (D3R) antagonist with pKi of 8.9.
GSK598809 displays >100-fold selectivity over D2 and H1 receptors.
GSK598809 significantly attenuates the expression of conditioned place preference (CPP) to nicotine and cocaine.
GSK598809 potentiates the hemodynamic effects of cocaine in dogs, also increases mean arterial blood pressure and heart rate in vivo.
