S1RA hydrochloride

  • Chemical Properties
CAS No. 1265917-14-3 Cat. No. BCP24076
Name S1RA hydrochloride
Synonyms E52862 HCl;E-52862 hydrochloride;; E-52862 HCl; E 52862 hydrochloride; S1RA hydrochloride;
Formula C20H24ClN3O2 M. Wt 373.88
  • Biological Activity
Description S1RA Hcl(E-52862 Hcl) is a potent and selective sigma-1 receptor(σ1R, Ki=17 nM) antagonist, showed good selectivity against σ2R (Ki > 1000 nM).E-52862, also known as S1RA, is a selective sigma-1 receptor antagonist, with a reported binding affinity of Ki = 17.0 ± 7.0 nM, selective over the sigma-2 receptor and against a panel of other 170 receptors, enzymes, transporters and ion channels. In preclinical studies, S1RA has demonstrated efficacy in relieving neuropathic pain and pain in other sensitizing conditions, associated with an improvement of the emotional negative state. E-52862 attenuates neuropathic pain of different aetiology in rats.
Pathways GPCR/G Protein 
Targets Sigma Receptor 

Structure

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