S1RA(E-52862)

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Chemical Information

Product name：S1RA(E-52862)	Purity：98% min
CAS NO：878141-96-9	Solubility：Soluble in DMSO
Molecular Formula：C₂₀H₂₃N₃O₂	Package：Package according to customer requirements
Molecular Weight：337.416	Storage：Store at -20℃

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Remarks

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.

Sigma Receptor Related Products:

Siramesine HCl; Cutamesine dihydrochloride; Siramesine(Lu 28-179); S1RA hydrochloride

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]. Romero L, et al. Pharmacological properties of S1RA, a new sigma-1 receptor antagonist that inhibits neuropathic pain and activity-induced spinal sensitization. Br J Pharmacol. 2012 Aug;166(8):2289-306.