Description
BD 1047 is a selective antagonist of sigma-1 (σ
1) receptors (K
i = 0.9 nM in a radioligand binding assay). It is selective for σ
1 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.
References
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10.1016/0014-2999(95)00208-3[2] KARI A. MCCRACKEN . Two novel σ receptor ligands, BD1047 and LR172, attenuate cocaine-induced toxicity and locomotor activity[J]. European journal of pharmacology, 1999, 370 3: Pages 225-232. DOI:
10.1016/s0014-2999(99)00113-2[3] TIEYING SONG. Role of sigma 1 receptor in high fat diet-induced peripheral neuropathy.[J]. Biological Chemistry, 2017, 398 10: 1141-1149. DOI:
10.1515/hsz-2017-0117[4] YOUNG CHAN JEONG Young B K Ji Seon Son. The spinal antinociceptive mechanism determined by systemic administration of BD1047 in zymosan-induced hyperalgesia in rats[J]. Brain Research Bulletin, 2015, 119: Pages 93-100. DOI:
10.1016/j.brainresbull.2015.07.006[5] DAE-HYUN ROH S Y Y. Sigma-1 receptor antagonist, BD1047 reduces nociceptive responses and phosphorylation of p38 MAPK in mice orofacial formalin model.[J]. Accounts of Chemical Research, 2014: 145-151. DOI:
10.1248/bpb.b13-00690[6] SHANSHAN ZHU. 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.[J]. Mediators of Inflammation, 2015, 2015 1: 265056. DOI:
10.1155/2015/265056
