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S1RA

Supplier:
Catalogue number:
10-4201-02
Size:
25 mg
Product is available in:
  • USA
  • Canada
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Sigma-1 antagonist (Selective). Sigma 1 receptor antagonist (SARS-CoV-2 Nsp6 protein interacts with the Sigma receptor). Gordon et al. bioRxiv, Mar 23 2020, https://doi.org/10.1101/2020.03.22.002386.

  • Datasheet:   view or download
  • Applications:In clinical trials for other indication(s)
Product Type:

Biochemicals & reagents

CAS Number:

1265917-14-3

Range:

1) Romero et al. (2012), Pharmacological properties of S1RA, a new sigma-1 receptor antagonist that inhibits neuropathic pain and activity-induced spinal sensitization; Br.J.Pharmacol. 166 2289 2) Diaz et al. (2012), Synthesis and biological evaluation of the 1-arylpyrazole class of (1) receptor antagonists: identification of 4-{2-[5-Methyl-1-(napthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine hydrochloride (S1RA, E-52862) ; J.Med.Chem. 55 8211 3) Tejada et al. (2017), Sigma-1 receptors control immune-driven peripheral opioid analgesia during inflammation in mice; Proc.Natl.Acad.Sci.USA 114 8396 4) Sanchez-Fernandez et al. (2014), Modulation of peripheral µ-opioid analgesia by 1 receptors; J.Pharmacol.Exp.Ther. 348 32 5) Sanchez-Blazquez et al. (2018), The Sigma-1 Receptor Antagonist, S1RA, Reduces Stroke Damage, Ameliorates Post-Stroke Neurological Deficits and Suppresses the Overexpression of MMP-9; Mol.Neurobiol. 55 4940

Limit of Detection:

373.88

Storage Temperature:

-20°C (des.)

Additional Information:

S1RA is a potent and selective σ1 antagonist with weak binding at σ2 with IC50’s: σ1 = 17nM and σ2 = 9300nM (1,2). This compound abolished mechanical and thermal hyperalgesia in mice with carrageenan-induced acute inflammation by enhancing the action of endogenous opioid peptides of immune origin in a σ dependent manner (3). BD1063 potentiated µ-opioid antinociception in mice in a σ-dependent manner (4). It also displayed neuroprotective effects in a mouse model of ischemic stroke (5).