| Identification | Back Directory | [Name]
1-Oxa-4,9-diazaspiro[5.5]undecan-3-one, 9-[2-(2,5-difluorophenyl)ethyl]-4-ethyl-2-methyl-, hydrochloride (1:1), (2R)- | [CAS]
2535970-65-9 | [Synonyms]
1-Oxa-4,9-diazaspiro[5.5]undecan-3-one, 9-[2-(2,5-difluorophenyl)ethyl]-4-ethyl-2-methyl-, hydrochloride (1:1), (2R)- | [Molecular Formula]
C19H27ClF2N2O2 | [MDL Number]
MFCD32878295 | [MOL File]
2535970-65-9.mol | [Molecular Weight]
388.88 |
| Hazard Information | Back Directory | [Uses]
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[1]. | [Biological Activity]
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 Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 hydrochloride has antinociceptive activity[1].
EST73502 hydrochloride (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[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]. | [in vivo]
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[1].
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[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%. |
| [References]
[1]. Mónica García, et al. Discovery of EST73502, a Dual μ-Opioid Receptor Agonist and σ 1 Receptor Antagonist Clinical Candidate for the Treatment of Pain. J Med Chem. 2020 Oct 16. |
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