EST73502 hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with K i s of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 hydrochloride has antinociceptive activity with reduced opioid-induced relevant adverse events[1].

EST73502 hydrochloride (10-40 mg/kg; p.o.) exhibits a dose-response analgesic effect reaching a maximum of 64% and an EC 50 of 14 mg/kg in the paw pressure test in CD1 male mice [1]. EST73502 hydrochloride (5 mg/kg; i.p.; twice a day; for 10 days) attenuates partial sciatic nerve ligation (PSNL)-induced mechanical allodynia in male CD1 mice [1]. Animal Model: Male CD1 mice, PSNL model [1] Dosage: 5 mg/kg Administration: Intraperitoneal injection, twice a day, for 10 days Result: Attenuated the expression of mechanical allodynia induced by PSNL, reaching a maximal effect of 56%.