BD 1047 dihydrobromide

BD-1047 dihydrobromide is a selective functional antagonist of sigma receptors, shows antipsychotic activity in animal models predictive of efficacy in schizophrenia. IC50 value: Target: sigma receptorin vitro: Moreover, Progesterone and BD 1047 (a sigma 1 receptor antagonist) counteracted the antidepressant-like effect induced by co-administration of Pramipexole and Sertraline (but not Pramipexole and Fluoxetine). [2] This increased pNR1 expression is significantly reduced by pretreatment with the specific Sig-1 R antagonist, BD-1047. In another set of experiments Sig-1 R agonists further potentiated NMDA-induced pain behaviour and pNR1 immunoreactivity and this is also reversed with BD-1047. [3]in vivo: BD 1047 does not decrease amphetamine-induced hyperactivity in mice in a statistically significant manner. BD 1047 does not modify the hyperactivity induced by NMDA receptor antagonists. BD 1047 shows a moderate activity in models used in this study suggesting that its usefulness as an antipsychtic drug is doubtful. [1]

Signaling Pathways >> GPCR/G Protein >> Sigma Receptor

Research Areas >> Neurological Disease

[1]. Skuza G, et al. Effect of BD 1047, a sigma1 receptor antagonist, in the animal models predictive of antipsychotic activity. Pharmacol Rep. 2006 Sep-Oct;58(5):626-635.

[2]. Rogóz Z, et al. Mechanism of synergistic action following co-treatment with pramipexole and fluoxetine or sertraline in the forced swimming test in rats. Pharmacol Rep. 2006 Jul-Aug;58(4):493-500.

[3]. Kim HW, et al. Activation of the spinal sigma-1 receptor enhances NMDA-induced pain via PKC- and PKA-dependent phosphorylation of the NR1 subunit in mice. Br J Pharmacol. 2008 Jul;154(5):1125-1134.

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