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