Compound A (α2C adrenoceptor agonist 1) is an orally active, highly selective α2C-adrenoceptor agonist that does not penetrate the central nervous system. It exhibits EC50 and Ki values of 108 nM and 12 nM, respectively. This compound is utilized in research on nasal congestion [1].

α2C-adrenoceptor:12 nM (Ki), α2C-adrenoceptor:108 nM (EC50)

Sprague-Dawley 大鼠口服单剂量 α2C adrenoceptor agonist 1 (Compound A) (5 mg/kg) 后，其脑渗透性较低，平均 C max 为 0.8 μM，T max 为 0.7 h，曲线下面积为 2 μM•h [1]。