138356-21-5

BD 1047 is a selective antagonist of sigma-1 (σ₁) receptors (K_i = 0.9 nM in a radioligand binding assay). It is selective for σ₁ receptors with binding affinity values greater than 10,000 nM for human recombinant dopamine, opioid, PCP, and serotonin receptors in vitro. In vivo, pretreatment with BD 1047 protects against convulsions and lethality induced by cocaine (Item Nos. 16186 | ISO60176) and reduces cocaine-induced locomotor activity. It reduces dystonias induced by the σ receptor agonists haloperidol and di-o-tolylguanidine (DTG) in rats in a dose-dependent manner. In vivo administration of BD 1047 also attenuates mechanical allodynia and microglial activation in a rat model of bone cancer pain.

BD 1047 dihydrobromide is an σ1 receptor antagonist with higher affinity than BD 1063.

Sigma 1 Receptor

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1) Matsumoto?et al.?(1995),?Characterization of two novel σ receptor ligands: antidystonic effects in rats suggest σ 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