BD1063
 | |
| Identifiers | |
|---|---|
| |
| CAS Number | 150208-28-9 |
| ChemSpider | 499765 |
| Chemical and physical data | |
| Formula | C13H18Cl2N2 |
| Molar mass | 273.20 g/mol |
| 3D model (Jmol) | Interactive image |
| |
| |
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]
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 2 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.
- ↑ 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. - ↑ 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.
This article is issued from Wikipedia - version of the 6/7/2016. The text is available under the Creative Commons Attribution/Share Alike but additional terms may apply for the media files.