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BD 1063 dihydrochloride
- Parent CAS: 150208-28-9
- Soluble in water and DMSO
- MF: C13H18Cl2N2.2HCl
- MW: 346.12
Description
BD 1063 dihydrochloride is a potent and selective sigma-1 receptor antagonist with reported Ki activity of 9 nM. It is approximately 50-fold selective over sigma-2 receptors and over 100-fold selective versus multiple tested neurotransmitter receptors.
Sigma-1 receptors modulate calcium signaling, ER stress responses, neurotransmission and psychostimulant-related behavioral effects. BD 1063 is useful for studying sigma-1 receptor pharmacology and antagonism of cocaine-associated responses.
Key Features
- Potent sigma-1 receptor antagonist
- Reported Ki: 9 nM
- Selectivity over sigma-2 and multiple neurotransmitter receptors
- Useful for CNS receptor pharmacology
Applications
- Sigma-1 receptor binding assays
- Cocaine response model research
- CNS neurotransmission studies
- Receptor selectivity profiling
More Information
| Parent CAS No. | 150208-28-9 |
|---|---|
| Chemical Name | 1-(3,4-dichlorophenethyl)-4-methylpiperazine dihydrochloride |
| SMILES | N1(CCC2=CC=C(Cl)C(Cl)=C2)CCN(C)CC1.Cl.Cl |
| MFCD | MFCD00792740 |
| InChi | InChI=1S/C13H18Cl2N2.2ClH/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;2*1H |
| InChiKey | NXFDBTLQOARIMH-UHFFFAOYSA-N |
| CID | 11617161 |
| Short Description | Sigma-1 antagonist |
References
- V Sabino et al. The σ-Receptor Antagonist BD-1063 Decreases Ethanol Intake and Reinforcement in Animal Models of Excessive Drinking. Neuropsychopharmacology 34.6 (2008): 1482-1493.
- KA McCracken et al. Novel σ receptor ligands attenuate the locomotor stimulatory effects of cocaine. Eur. J. Pharmacol. 1995, 365(1), 35-38.
- FP Monnet et al. Neurosteroids, via sigma receptors, modulate the [3H] norepinephrine release evoked by N-methyl-D-aspartate in the rat hippocampus. Proc. Nat. Acad. Sci. 1995, 92(9), 3774-3778.
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