Sigma-1 antagonist / S1RA (E-52862) is a potent and selective σ1 antagonist with weak binding at σ2 (IC50’s: σ1 = 17nM, σ2 = 9300nM).1,2 S1RA 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 σ1 dependent manner.3 BD1063 potentiated µ-opioid antinociception in mice in a σ-dependent manner.4 S1RA displayed neuroprotective effects in a mouse model of ischemic stroke.5
Biochemicals & reagents
1265917-14-3
E-52862 HCl
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
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TARGET: ER/Golgi -- PATHWAY: Calcium signaling; cAMP / cGMP signaling -- RESEARCH AREA: Neuroscience -- DISEASE AREA: Pain; InflammationAddiction; Ischemia