Product Description: 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].
Applications: Neuroscience-Neuromodulation
Formula: C20H23N3O2
References: [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.
CAS Number: 878141-96-9
Molecular Weight: 337.42
Compound Purity: 99.43
Research Area: Neurological Disease
Solubility: 1M HCl : 50 mg/mL (ultrasonic;adjust pH to 1 with HCl)/DMSO : 33.33 mg/mL (ultrasonic;warming;heat to 60°C)
Target: 5-HT Receptor;Sigma Receptor
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