BD1063 is potent and selective sigma-1 antagonist (IC50s: sigma1 = 9nM, sigma2 = 449nM).1 BD1063 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 sigma1 dependent manner.2 BD1063 potentiated µ-opioid antinociception in mice in a sigma-dependent manner.3 BD-1063 has been used in animal models to successfully treat compulsive eating4 and excessive ethanol drinking5.
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