EST73502 是一种选择性的，具有口服活性的，可透过血脑屏障的 μ-opioid 受体 (μ-Opioid Receptor/MOR) 激动剂和 σ1 受体(σ1R) 拮抗剂，对 MOR 和 σ1R 作用的Ki值分别为 64 nM 和 118 nM。EST73502 可用于缓解疼痛研究。

EST73502 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 has antinociceptive activity [1].

EST73502 (10-40 mg/kg; p.o.) shows 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 (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%.

1838622-25-5

C19H26F2N2O2

352.42

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years