BD1063 (206996-13-6) is potent and selective sigma-1 antagonist (IC50’s: σ1 = 9nM, σ2 = 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 σ1 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.
1) Matsumoto et al. (1995), Characterisation of two novel σ receptor ligands: antidystonic effects in rats suggest &sigma receptor antagonism; Eur. J. Pharmacol. 280 301
2) Tejada et al. (2017), Sigma-1 receptors control immune-driven peripheral opioid analgesia during inflammation in mice; Proc. Natl. Acad. Sci. USA 114 8396
3) Sanchez-Fernandez et al. (2014), Modulation of peripheral µ-opioid analgesia by σ1 receptors; J. Pharmacol. Exp. Ther. 348 32
4) Cottone et al. (2012), Antagonism of sigma-1 receptors blocks compulsive-like eating; Neuropsychopharmaology 37 2593
5) Sabino et al. (2009), The sigma-receptor antagonist BD-1063 decreases ethanol intake and reinforcement in animal models of excessive drinking; Neuropsychopharmaology 34 1482