BD 1047 dihydrobromide
(Synonyms: BD-1047盐酸盐) 目录号 : GC15374
A selective antagonist of σ1 receptors
Cas No.:138356-21-5
Sample solution is provided at 25 µL, 10mM.
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BD 1047 dihydrobromide is an antagonist of σ1 receptor with Ki values of 0.93 and 47 nM for σ-1 receptor and σ-2 receptor, respectively [1].
σ-receptor is a type of opioid receptor. There are two subtypes of σ-receptor: σ-1 and σ-2.σ-1 receptor plays an important role in stimulating dopamine release and modulating the actions of cocaine.
BD 1047 dihydrobromide is a σ-1 receptor antagonist. BD 1047 reduced the dystonia induced by haloperidol and di-o-tolylguanidine (DTG) in a dose-dependent way [1].
In male Wistar rats, BD1047 (20 or 30 mg/kg) reversed response reinstatement induced by the cocaine discriminative stimulus (SD). However, BD1047 had no effect on sweetened condensed milk (SCM) SD-induced responding [2]. In rats with chronic constriction injury (CCI) of the right sciatic nerve, BD1047 significantly relieved CCI-induced mechanical allodynia during the induction. Also, BD1047 significantly increased the expression of σ-1 receptor in the ipsilateral spinal cord dorsal horn and inhibited N-methyl-D-aspartate receptor subunit 1 (NR1) expression and phosphorylation induced by CCI [3].
References:
[1]. Matsumoto RR, Bowen WD, Tom MA, et al. Characterization of two novel sigma receptor ligands: antidystonic effects in rats suggest sigma receptor antagonism. Eur J Pharmacol, 1995, 280(3): 301-310.
[2]. Martin-Fardon R, Maurice T, Aujla H, et al. Differential effects of sigma1 receptor blockade on self-administration and conditioned reinstatement motivated by cocaine vs natural reward. Neuropsychopharmacology, 2007, 32(9): 1967-1973.
[3]. Roh DH, Kim HW, Yoon SY, et al. Intrathecal injection of the sigma(1) receptor antagonist BD1047 blocks both mechanical allodynia and increases in spinal NR1 expression during the induction phase of rodent neuropathic pain. Anesthesiology, 2008, 109(5): 879-889.
| Cas No. | 138356-21-5 | SDF | |
| 别名 | BD-1047盐酸盐 | ||
| 化学名 | N1-(3,4-dichlorophenethyl)-N1,N2,N2-trimethylethane-1,2-diamine dihydrobromide | ||
| Canonical SMILES | ClC1=CC(CCN(C)CCN(C)C)=CC=C1Cl.Br.Br | ||
| 分子式 | C13H20Cl2N2.2HBr | 分子量 | 437.04 |
| 溶解度 | ≥ 43.9 mg/mL in DMSO with gentle warming, ≥ 43.5 mg/mL in Water with gentle warming | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2881 mL | 11.4406 mL | 22.8812 mL |
| 5 mM | 0.4576 mL | 2.2881 mL | 4.5762 mL |
| 10 mM | 0.2288 mL | 1.1441 mL | 2.2881 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet