BD1063 explained

BD1063 or 1-[2-(3,4-dichlorophenyl)ethyl]-4-methylpiperazine is a selective sigma receptor antagonist, with a reported binding affinity of K_i = 9 ± 1 nM for the sigma-1 receptor and more than 49 times selectivity over the sigma-2 receptor.^[1]

Consistent with other reported sigma receptor antagonists, pretreating Swiss Webster mice with BD1063 significantly decreases the convulsivity and lethality of cocaine.

In other animal studies, BD1063 blocks the effects of MDMA,^[2] and reduces alcohol intake in rodent models of alcoholism.^[3]

See also

• BD1008
• BD1031
• LR132

Notes and References

1. Matsumoto RR, McCracken KA, Friedman MJ, Pouw B, De Costa BR, Bowen WD . Conformationally restricted analogs of BD1008 and an antisense oligodeoxynucleotide targeting sigma1 receptors produce anti-cocaine effects in mice . Eur. J. Pharmacol. . 419 . 2–3 . 163–74 . 2001 . 11426838. 10.1016/s0014-2999(01)00968-2.
2. Brammer MK, Gilmore DL, Matsumoto RR . Interactions between 3,4-methylenedioxymethamphetamine and sigma1 receptors . European Journal of Pharmacology . 553 . 1–3 . 141–5 . December 2006. 17070798 . 1780037 . 10.1016/j.ejphar.2006.09.038 .
3. Sabino V, Cottone P, Zhao Y, Iyer MR, Steardo L, Steardo L, Rice KC, Conti B, Koob GF, Zorrilla EP . The sigma-receptor antagonist BD-1063 decreases ethanol intake and reinforcement in animal models of excessive drinking . Neuropsychopharmacology . 34 . 6 . 1482–93 . May 2009. 18946467 . 2669694 . 10.1038/npp.2008.192 .