PF-592379 is a potent agonist of dopamine D3 receptor (EC50: 21 nM).

D3 receptor:（EC50）21 nM

PF-592379 is a potent and selective dopamine 3 agonist with an Emax of 95% compared to Pramipexole [1]. It exhibits an EC50 of 21 nM and Ki of 322 nM [2], showing high affinity to human D3 receptors (Ki=215 nM) and a 19-fold selectivity over D4 receptors (Ki=4165 nM). PF-592379 does not bind to D1, human D2, or D5 receptors at concentrations up to 10 μM (Ki≥10 μM) [3].

PF-592379 acts as an oral dopamine 3 agonist in rats and dogs. It exhibits a clearance rate of 6.3 and 8.5 mL/min/kg in dogs and 44.8 and 58.2 mL/min/kg in rats, considered low to moderate relative to liver blood flow. The compound demonstrates high permeability in Caco-2 cells and shows complete absorption in pharmacokinetic studies carried out on rats and dogs, achieving oral bioavailability rates of 28% in rats and 61 to 87% in dogs [1].