N-{4-[4-(2,3-Dichlorophenyl)-piperazin-1-yl]-trans-but-2-enyl}-4-(pyridin-2-yl)benzamide dihydrochloride hydrate

Description

PG-01037 is a selective dopamine D₃ receptor antagonist (K_is = 0.7, 93, and 375 nM for HEK293 cells expressing human D₃, D₂, and D₄ receptors, respectively). It inhibits quinpirole-induced stimulation of mitogenesis in CHO cells expressing human dopamine D₃ receptors (EC₅₀ = 3 nM). PG-01037 (32 mg/kg) reduces progressive-ratio methamphetamine self-administration in rats allowed extended access. It reduces loss of dopaminergic neurons in the substantia nigra pars compacta and improves motor performance in the coat-hanger test in a mouse model of Parkinson''s disease induced by MPTP.

Uses

PG01037 dihydrochloride is a selective D3DR antagonist.

storage

Desiccate at +4°C