| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: ≥98%
BD-1063 HCl (BD1063 hydrochloride) is a novel, potent and selective sigma receptor antagonist with the potential for treating alcoholism. It exhibits a Ki of 9 ± 1 nM for the sigma-1 receptor and shows more than 49 times selectivity over the sigma-2 receptor. Consistent with other reported sigma receptor antagonists, pretreating Swiss Webster mice with BD1063 significantly decreases the convulsivity and lethality of cocaine. In other animal studies, BD1063 blocks the effects of MDMA, and reduces alcohol intake in rodent models of alcoholism.
| ln Vivo |
At dosages that do not alter the mean ethanol self-administration in non-dependent Wistar controls, BD1063 dose-dependently decreases the amount of ethanol self-administration in sP rats (3.3-11 mg/kg) and withdrawn, dependent Wistar rats (4-11 mg/kg). Additionally, BD1063 lowers the breakpoints for sP rats to labor for ethanol in a reinforcement schedule with a progressive ratio[1]. In Palatable rats, BD1063 inhibits the elevated eating rate and decreases binge-like eating as well as the regularity of food response in a dose-dependent manner. Without influencing motor activity, BD1063 opposes both the increased consumption of the palatable food and the longer time spent in the unpleasant compartment in the light/dark conflict test[2]. In WT mice, BD1063 is administered half an hour prior to each paclitaxel treatment, preventing the development of mechanical and cold allodynia. Furthermore, both forms of paclitaxel-induced allodynia are reversed by the acute dose-dependent injection of BD1063[3].
|
|
|---|---|---|
| Animal Protocol |
|
|
| References |
[1]. Sabino V, et al. The sigma-receptor antagonist BD-1063 decreases ethanol intake and reinforcement in animal models of excessive drinking. Neuropsychopharmacology. 2009 May;34(6):1482-93.
[2]. Cottone P, et al. Antagonism of sigma-1 receptors blocks compulsive-like eating. Neuropsychopharmacology. 2012 Nov;37(12):2593-604. [3]. Nieto FR, et al. Role of sigma-1 receptors in paclitaxel-induced neuropathic pain in mice. J Pain. 2012 Nov;13(11):1107-21 |
| Molecular Formula |
C13H18N2CL2.2[HCL]
|
|---|---|
| Molecular Weight |
346.1233
|
| CAS # |
206996-13-6
|
| Related CAS # |
Related CAS 206996-13-6 (HCl); 150208-28-9
|
| SMILES |
CN1CCN(CCC2=CC=C(Cl)C(Cl)=C2)CC1.[H]Cl.[H]Cl
|
| InChi Key |
NXFDBTLQOARIMH-UHFFFAOYSA-N
|
| InChi Code |
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
|
| Chemical Name |
1-[2-(3,4-dichlorophenyl)ethyl]-4-methyl-piperazine, dihydrochloride
|
| Synonyms |
BD1063; BD 1063; BD-1063;
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
H2O : ~100 mg/mL (~288.92 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (288.92 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8892 mL | 14.4459 mL | 28.8917 mL | |
| 5 mM | 0.5778 mL | 2.8892 mL | 5.7783 mL | |
| 10 mM | 0.2889 mL | 1.4446 mL | 2.8892 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA