Biochemicals & reagents
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
BD1047 is a potent and selective σ1 antagonist withIC50’s for σ1 = 0.93nM and σ2 = 47nM (1). Pretreatment of mice with this compound reduced convulsions, lethality, and locomotor activity induced by cocaine (2). It attenuated high fat diet-induced peripheral neuropathy in mice (3), it displayed antinociceptive effects in several rodent pain models (4-6) and it also inhibits the beta-adrenoreceptor with an IC50 = 145 nM (1).