Chemistry:BD1008
From HandWiki
Short description: Chemical compound
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| Formula | C15H22Cl2N2 |
| Molar mass | 301.26 g·mol−1 |
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BD1008 or N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-1-pyrrolidineethanamine is a selective sigma receptor antagonist, with a reported binding affinity of Ki = 2 ± 1 nM for the sigma-1 receptor and 4 times selectivity over the sigma-2 receptor.[1]
Consistent with other reported sigma receptor antagonists, pretreating Swiss Webster mice with BD1008 significantly attenuates the behavioral toxicity of cocaine, and may be potentially useful in the development of antidotes for the treatment of cocaine overdose.[1][2][3][4]
See also
- BD1031
- LR132
References
- ↑ 1.0 1.1 "N-alkyl substituted analogs of the sigma receptor ligand BD1008 and traditional sigma receptor ligands affect cocaine-induced convulsions and lethality in mice". Eur. J. Pharmacol. 411 (3): 261–73. 2001. doi:10.1016/s0014-2999(00)00917-1.
- ↑ "Differentiation of sigma ligand-activated receptor subtypes that modulate NMDA-evoked [3H-noradrenaline release in rat hippocampal slices"]. British Journal of Pharmacology 119 (1): 65–72. September 1996. doi:10.1111/j.1476-5381.1996.tb15678.x. PMID 8872358.
- ↑ "Conformationally restricted analogs of BD1008 and an antisense oligodeoxynucleotide targeting sigma1 receptors produce anti-cocaine effects in mice". European Journal of Pharmacology 419 (2-3): 163–74. May 2001. doi:10.1016/S0014-2999(01)00968-2. PMID 11426838.
- ↑ "Novel analogs of the sigma receptor ligand BD1008 attenuate cocaine-induced toxicity in mice". European Journal of Pharmacology 492 (1): 21–6. May 2004. doi:10.1016/j.ejphar.2004.03.037. PMID 15145701.
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