For research use only. Not for therapeutic Use.
S1RA (E-52862) is a highly selective σ1 receptor (σ1R) antagonist with Kis of 17 nM and 23.5 nM for human σ1R and guinea pig σ1R, respectively. S1RA has Moderate antagonistic activity for human 5-HT2B receptor (Ki= 328 nM). S1RA has antinociceptive effects in neuropathic pain models. S1RA prevents mechanical and cold hypersensitivity in Oxaliplatin (HY-17371)-treated mice[1][2].
S1RA (E-52862; 100 µM; 4 h) inhibit intracellular calcium responses in TRPA1 expressing HEK293 cells[2].
S1RA (100 µM; 4 h) impairs the formation of TRPA1–Sigma-1R complexes and reduces TRPA1 expression at the plasma membrane[2].
S1RA (E-52862; 40 mg/kg; IP; single dose) produces a substantial reduction in pain-related responses to intradermal Allylisothiocyanate (AITC) in WT mice[2].
S1RA (40 mg/kg; IP; once a day for 11 consecutive days; starting 3 days before Oxaliplatin injection) prevents mechanical and cold hypersensitivity in Oxaliplatin (6 mg/kg; i.p.; Day 0, Day 2, Day 4)-treated mice[2].
| Catalog Number | I005283 |
| CAS Number | 878141-96-9 |
| Synonyms | 4-[2-(5-methyl-1-naphthalen-2-ylpyrazol-3-yl)oxyethyl]morpholine |
| Molecular Formula | C20H23N3O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C20H23N3O2/c1-16-14-20(25-13-10-22-8-11-24-12-9-22)21-23(16)19-7-6-17-4-2-3-5-18(17)15-19/h2-7,14-15H,8-13H2,1H3 |
| InChIKey | DGPGXHRHNRYVDH-UHFFFAOYSA-N |
| SMILES | CC1=CC(=NN1C2=CC3=CC=CC=C3C=C2)OCCN4CCOCC4 |
| Reference | [1]. Díaz JL, et al. Synthesis and biological evaluation of the 1-arylpyrazole class of σ(1) receptor antagonists: identification of 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862). J Med Chem. 2012 Oct 11;55(19):8211-24. [2]. Aida Marcotti, et al. TRPA1 modulation by Sigma-1 receptor prevents oxaliplatin-induced painful peripheral neuropathy. Brain. 2023 Feb 13;146(2):475-491. |
