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 K i s of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 monohydrochloride has antinociceptive activity In Vivo EST73502 monohydrochloride (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 . 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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%. IC50& Target:Ki: 64 nM (MOR), 118 nM (σ1R)
All
Chemical Reagents
Biomedicine
Organic raw materials
Inorganic chemical industry
intermediate
Agricultural chemicals
Auxiliaries and catalysts
Fragrances and Flavors
Dyes and Pigments
Daily chemical industry
EST73502 monohydrochloride
CAS number：2535970-65-9(DMSO) molecular formula：C19H27ClF2N2O2
overview
compound introduction
Specs
| Chinese alias | EST73502 单盐酸盐 | ||
| English alias | - | ||
| CAS number | 2535970-65-9(DMSO) | molecular formula | C19H27ClF2N2O2 |
| molecular weight | 388.88 g/mol | Exact mass | 10mM in DMSO |
| PSA | - | logp | - |
numbering system
No numbering system information yet
physicochemical properties
No physical and chemical property information yet
Safety information
No safety information yet
Production methods and uses
No production method and use information yet
Related
upstream information
No upstream information yet
downstream information
No downstream information yet
MSDS
Found 0 shareMSDS
