BD1047 dihydrobromide
Sigma-1 antagonist / BD1047 is a potent and selective sigma-1 antagonist (IC50’s: sigma1 = 0.93nM, sigma2 = 47nM). .1 Pretreatment of mice with BD1047 reduced convulsions, lethality, and locomotor activity induced by cocaine.2 BD1047 attenuated high fat diet-induced peripheral neuropathy in mice.3 BD1047 displayed antinociceptive effects in several rodent pain models.4-6 It also inhibits the beta-adrenoreceptor (IC50 = 145 nM).1
Biochemicals & reagents
138356-21-5
1) Matsumoto et al. (1995), Characterisation of two novel ? receptor ligands: antidystonic effects in rats suggest ? receptor antagonism; Eur.J.Pharmacol. 280 301 2) McCracken et al. (1999), Two novel sigma receptor ligands, BD1047 and LR172, attenuate cocaine-induced toxicity and locomotor activity; Eur.J.Pharmacol. 370 225 3) Song et al. (2017), Role of sigma 1 receptor in high fat diet-induced peripheral neuropathy; Biol.Chem. 398 1141 4) Jeong et al. (2005), The spinal antinociceptive mechanism determined by systemic administration of BD1047 in zymosan-induced hyperalgesia in rats; Brain Res. Bull. 119(Pt.A) 93 5) Roh and Yoon (2014), Sigma-1 receptor antagonist BD1047 reduces nociceptive response and phosphorylation of p38 MAPK in mice orofacial formalin model; Biol.Pharm.Bull. 37 145 6) Zhu et al. (2015), Sigma-1 Receptor Antagonist BD1047 Reduces Mechanical Allodynia in a Rat Model of Bone Cancer Pain through the Inhibition of Spinal NR1 Phosphorylation and Microglia Activation; Mediators Inflamm. 2015 265056
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TARGET: ER/Golgi -- PATHWAY: Calcium signaling; cAMP / cGMP signaling -- RESEARCH AREA: Neuroscience -- DISEASE AREA: Pain; NeurodegenerationAddiction