CVN424 (CVN 424) is a highly potent, selective, brain-penetrant, orally active GPR6 inverse agonist with EC50 of 38 nM.
Oral administration of CVN424 dose-dependently increases locomotor activity and reverses haloperidol-induced catalepsy.
CVN424 restored mobility in bilateral 6-hydroxydopamine lesion model of Parkinson disease.
CVN424 is brain-penetrant and shows dose-dependent receptor occupancy that attained brain 50% of receptor occupancy at plasma concentrations of 6.0 and 7.4 ng/ml in mice and rats, respectively.
CVN424 is effective in preclinical models and is a potential therapeutic for improving motor function in patients with Parkinson disease.
