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BD1063

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Chemical compound
Pharmaceutical compound
BD1063
Identifiers
  • 1-[2-(3,4-dichlorophenyl)ethyl]-4-methylpiperazine
CAS Number
ChemSpider
UNII
CompTox Dashboard(EPA)
ECHA InfoCard100.229.843Edit this at Wikidata
Chemical and physical data
FormulaC13H18Cl2N2
Molar mass273.20 g·mol−1
3D model (JSmol)
  • CN1CCN(CC1)CCc2ccc(c(c2)Cl)Cl
  • 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 or1-[2-(3,4-dichlorophenyl)ethyl]-4-methylpiperazine is a selectivesigma receptorantagonist, with a reportedbinding affinity ofKi = 9 ± 1 nM for thesigma-1 receptor and more than 49 times selectivity over thesigma-2 receptor.[1]

Consistent with other reportedsigma receptorantagonists, pretreating Swiss Webster mice with BD1063 significantly decreases the convulsivity and lethality of cocaine.[1]

In other animal studies, BD1063 blocks the effects ofMDMA,[2] and reduces alcohol intake in rodent models ofalcoholism.[3]

See also

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References

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  1. ^abMatsumoto 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.
σ1
σ2
Unsorted
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