BD1063 dihydrochloride
Sigma-1 antagonist / BD1063 is potent and selective sigma-1 antagonist (IC50’s: 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.
Biochemicals & reagents
206996-13-6
1) Matsumoto et al. (1995), Characterisation of two novel ? receptor ligands: antidystonic effects in rats suggest ? 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 ?1 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 decrease ethanol intake and reinforcement in animal models of excessive drinking; Neuropsychopharmaology 34 1482
-20°C
TARGET: ER/Golgi -- PATHWAY: Calcium signaling; cAMP / cGMP signaling -- RESEARCH AREA: Neuroscience -- DISEASE AREA: Pain; InflammationAddiction