S1RA

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].

Product Specifications

CAS Number

[878141-96-9]

Product Name Alternative

E-52862

UNSPSC

12352005

Hazard Statement

H302, H315, H320, H335

Target

5-HT Receptor; Sigma Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/s1ra.html

Concentration

10mM

Purity

99.43

Solubility

1M HCl : 50 mg/mL (ultrasonic; adjust pH to 1 with HCl) |DMSO : 33.33 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

CC1=CC(OCCN2CCOCC2)=NN1C3=CC(C=CC=C4)=C4C=C3

Molecular Formula

C20H23N3O2

Molecular Weight

337.42

Precautions

H302, H315, H320, H335

References & Citations

[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.