S1RA - CAS 878141-96-9
Catalog number: 878141-96-9
Category: Inhibitor
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Molecular Formula:
C20H23N3O2
Molecular Weight:
337.42
COA:
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Targets:
Sigma Receptor
Description:
The sigma-1 (σ1) receptor is an intracellular, non-opioid receptor that is abundantly expressed in the central nervous system as well as peripherally. S1RA is a potent, selective antagonist of σ1 receptors (Ki = 17 nM) that weakly binds σ2 receptors (Ki = 9,300 nM).
MSDS:
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InChIKey:
DGPGXHRHNRYVDH-UHFFFAOYSA-N
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
Canonical SMILES:
CC1=CC(=NN1C2=CC3=CC=CC=C3C=C2)OCCN4CCOCC4
1.S1RA, a selective sigma-1 receptor antagonist, inhibits inflammatory pain in the carrageenan and complete Freund's adjuvant models in mice.
Gris G1, Merlos M, Vela JM, Zamanillo D, Portillo-Salido E. Behav Pharmacol. 2014 Jun;25(3):226-35. doi: 10.1097/FBP.0000000000000038.
The therapeutic potential of S1RA (E-52862), a selective sigma-1 receptor (σ1R) antagonist, has been explored in experimental neuropathic pain, but not in inflammatory pain models. The present study investigated the effect of the intraperitoneal administration of S1RA on the hind paw withdrawal response to thermal and mechanical stimulation following an intraplantar injection of carrageenan (CARR) and complete Freund's adjuvant (CFA), which are two well-characterized models of acute and chronic inflammatory pain, respectively. S1RA fully reversed both mechanical [dose of drug that produced half of its maximal response (ED50)=35.9 and 42.1 mg/kg for CARR-induced and CFA-induced pain, respectively] and thermal (ED50=27.9 mg/kg, CARR) hypersensitivity, whereas ibuprofen (CARR, mechanical allodynia) and celecoxib (CARR, thermal hyperalgesia; CFA, mechanical allodynia) failed to reach maximum efficacy. Morphine also showed maximum efficacy in all tests.
2.Effects of the selective sigma-1 receptor antagonist S1RA on formalin-induced pain behavior and neurotransmitter release in the spinal cord in rats.
Vidal-Torres A1, Fernández-Pastor B, Carceller A, Vela JM, Merlos M, Zamanillo D. J Neurochem. 2014 May;129(3):484-94. doi: 10.1111/jnc.12648. Epub 2014 Jan 29.
We have previously shown that the selective sigma-1 receptor (σ1 R) antagonist S1RA (E-52862) inhibits neuropathic pain and activity-induced spinal sensitization in various pre-clinical pain models. In this study we characterized both the behavioral and the spinal neurochemical effects of S1RA in the rat formalin test. Systemic administration of S1RA produced a dose-related attenuation of flinching and lifting/licking behaviors in the formalin test. Neurochemical studies using concentric microdialysis in the ipsilateral dorsal horn of awake, freely moving rats revealed that the systemic S1RA-induced antinociceptive effect occurs concomitantly with an enhancement of noradrenaline levels and an attenuation of formalin-evoked glutamate release in the spinal dorsal horn. Intrathecal pre-treatment with idazoxan prevented the systemic S1RA antinociceptive effect, suggesting that the S1RA antinociception depends on the activation of spinal α2 -adrenoceptors which, in turn, could induce an inhibition of formalin-evoked glutamate release.
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CAS 878141-96-9 S1RA

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