S1RA (E-52862) is a potent and selective σ1 antagonist with weak binding at σ2 (IC50’s: σ1 = 17nM, σ2 = 9300nM). 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...
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S1RA (E-52862) is a potent and selective σ1 antagonist with weak binding at σ2 (IC50’s: σ1 = 17nM, σ2 = 9300nM). 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. BD1063 potentiated µ-opioid antinociception in mice in a σ-dependent manner. S1RA displayed neuroprotective effects in a mouse model of ischemic stroke
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