产品
编 号:F753634
分子式:C19H27ClF2N2O2
分子量:388.88
产品类型
结构图
CAS No: 2535970-65-9
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产品详情
生物活性:
EST73502 monohydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 monohydrochloride has antinociceptive activity.
体内研究:
EST73502 monohydrochloride (10-40 mg/kg; p.o.) shows a dose-response analgesic effect reaching a maximum of 64% and an EC50 of 14 mg/kg in the paw pressure test in CD1 male mice.EST73502 monohydrochloride (5 mg/kg; i.p.; twice a day; for 10 days) attenuates partial sciatic nerve ligation (PSNL)-induced mechanical allodynia in male CD1 mice.Animal Model:Male CD1 mice, PSNL model
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%.