S1RA

S1RA (E-52862) is a potent and selective 1 antagonist with weak binding at 2 (IC50’s: 1 = 17nM, 2 = 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 1 dependent manner.3 BD1063 potentiated µ-opioid antinociception in mice in a -dependent manner.4 S1RA displayed neuroprotective effects in a mouse model of ischemic stroke.5