产品
编 号：F747491
分子式：C19H26F2N2O2
分子量：352.42
分子式：C19H26F2N2O2
分子量：352.42
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CAS No: 1838622-25-5
产品详情
生物活性：
EST73502 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 has antinociceptive activity.
体内研究：
EST73502 (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 (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%.
EST73502 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 has antinociceptive activity.
体内研究：
EST73502 (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 (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%.
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