A-77636 is a potent, selective, and long-acting oral dopamine D1 receptor agonist with an effective concentration (EC50) of 1.1 nM and a corresponding pEC50 value of 8.13. It demonstrates the highest affinity for the dopamine D1 receptor with a dissociation constant (Ki) of 39.8 nM and a pKi of 7.40 ± 0.09. Notably, A-77636 exhibits antiparkinsonian activity [1].

D1 receptor:39.8 nM (Ki), D1 receptor:1.1 nM (EC50)

A-77636（0-3.2 μmol/kg，皮下注射）在6-OHDA损伤的大鼠中引起旋转行为，有效剂量为ED 50 =0.32 μmol/kg [1]。以1-10 mg/kg剂量的A-77636减轻了成瘾剂引发的运动亢进，显示出剂量依赖性[2]。该化合物在大鼠和小鼠中以ED 50 =12.3 μmol/kg和ED 50 =12.1 μmol/kg剂量引发前肢阵挛[1]。在给予MPTP以诱发帕金森氏症模型的狨猴中，A-77636（0.5、1.0 或 2.0 μmol/kg，口服）能够增加活动性和减轻症状，无论是通过皮下注射还是口服给药均有效[1]。