BD1063

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

BD1063
Identifiers
IUPAC name
  • 1-[2-(3,4-dichlorophenyl)ethyl]-4-methylpiperazine
CAS Number
ChemSpider
CompTox Dashboard (EPA)
ECHA InfoCard100.229.843
Chemical and physical data
FormulaC13H18Cl2N2
Molar mass273.20 g·mol−1
3D model (JSmol)
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

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

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. PMID 11426838.
  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.
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