BD 1047 dihydrobromide

Description: BD 1047 dihydrobromide is a selective functional antagonist of sigma receptors (sigma receptors). BD 1047 is demonstrated to attenuate the dystonia produced by the high affinity sigma receptor ligands di-o-tolylguanidine and Haloperidol. BD 1047 is described to have similar activity at the sigma-1 receptor to BD 1063 (sc-203838) and to show higher affinity at sigma-2 than BD 1063. BD 1047 is demonstrated to antagonize the effects of Trazodone on neurotransmitter release. BD 1047 did not decrease amphetamine-induced hyperactivity in mice in a statistically significant manner. Likewise, it did not modify the hyperactivity induced by NMDA receptor antagonists, phencyclidine, memantine or dizocilpine. On the other hand, BD 1047 attenuated apomorphine-induced climbing in mice and phencyclidine-induced head twitches in rats, like rimcazole and panamesine did. Summing up, BD 1047 shows a moderate activity in models used in this study suggesting that its usefulness as an antipsychtic drug is doubtful. However, more detailed studies are required for definitive confirmation of this conclusion.

References: Pharmacol Rep. 2006 Sep-Oct; 58(5):626-35.