BD1063

BD1063

Systematic (IUPAC) name
1-[2-(3,4-dichlorophenyl)ethyl]-4-methylpiperazine
Identifiers
CAS Number	150208-28-9
ChemSpider	499765
Chemical data
Formula	C13H18Cl2N2
Molar mass	273.20 g/mol
SMILES CN1CCN(CC1)CCc2ccc(c(c2)Cl)Cl
InChI InChI=1S/C13H18Cl2N2/c1-16-6-8-17(9-7-16)5-4-11-2-3-12(14)13(15)10-11/h2-3,10H,4-9H2,1H3 Key:SUIZRDJCBVPASY-UHFFFAOYSA-N

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.^[1]

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

References

1. Matsumoto RR, McCracken KA, Friedman MJ, Pouw B, De Costa BR, Bowen WD (2001). "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. doi:10.1016/s0014-2999(01)00968-2.
2. Brammer MK, Gilmore DL, Matsumoto RR (December 2006). "Interactions between 3,4-methylenedioxymethamphetamine and sigma1 receptors". European Journal of Pharmacology 553 (1-3): 141–5. doi:10.1016/j.ejphar.2006.09.038. PMC 1780037. PMID 17070798.
3. Sabino V, Cottone P, Zhao Y, Iyer MR, Steardo L, Steardo L, Rice KC, Conti B, Koob GF, Zorrilla EP (May 2009). "The sigma-receptor antagonist BD-1063 decreases ethanol intake and reinforcement in animal models of excessive drinking". Neuropsychopharmacology 34 (6): 1482–93. doi:10.1038/npp.2008.192. PMC 2669694. PMID 18946467.