BD 1063 dihydrochloride
(Synonyms: BD1063(盐酸盐)) 目录号 : GC15838
An antagonist of σ1 receptors
Cas No.:206996-13-6
Sample solution is provided at 25 µL, 10mM.
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BD 1063 dihydrochloride is an antagonist of σ-1 receptor with Ki value of 9.15 nM [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 [2].
BD 1063 dihydrochloride is a σ-1 receptor antagonist with Ki values of 9.15 and 449 nM for σ-1 receptor and σ-2 receptor, respectively. BD1063 reduced the dystonia induced by haloperidol and di-o-tolylguanidine (DTG) in a dose-dependent way [1].
In mice, BD1063 inhibited up-regulation of fra-2 and σ-1 receptor induced by cocaine in whole brain, cortex and striatum [2]. In mice, BD1063 significantly inhibited convulsions, lethality and locomotor stimulatory effects induced by cocaine [3]. In two excessive drinking rat models, BD-1063 reduced ethanol self-administration in a dose-dependent way and inhibited the expression of σ-1 receptor in the nucleus accumbens [4]. In mice, BD-1063 reversed thermal (radiant heat) hyperalgesia and inflammatory mechanical (paw pressure) in a dose-dependent way. However, BD-1063 had no effect on thermal hyperalgesia in σ1 knockout (σ1-KO) mice. These results suggested that σ1 receptor played an important role in inflammatory hyperalgesia [5].
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]. Liu Y, Chen GD, Lerner MR, et al. Cocaine up-regulates Fra-2 and sigma-1 receptor gene and protein expression in brain regions involved in addiction and reward. J Pharmacol Exp Ther, 2005, 314(2): 770-779.
[3]. Matsumoto RR, McCracken KA, Friedman MJ, et al. Conformationally restricted analogs of BD1008 and an antisense oligodeoxynucleotide targeting sigma1 receptors produce anti-cocaine effects in mice. Eur J Pharmacol, 2001, 419(2-3): 163-174.
[4]. Sabino V, Cottone P, Zhao Y, et al. The sigma-receptor antagonist BD-1063 decreases ethanol intake and reinforcement in animal models of excessive drinking. Neuropsychopharmacology, 2009, 34(6): 1482-1493.
[5]. Tejada MA, Montilla-García A, Sánchez-Fernández C, et al. Sigma-1 receptor inhibition reverses acute inflammatory hyperalgesia in mice: role of peripheral sigma-1 receptors. Psychopharmacology (Berl), 2014, 231(19): 3855-3869.
Animal experiment: | Rats: BD1063 is solubilized in isotonic saline and injected subcutaneously (s.c. 1 ml/kg), 15 min before testing. Rats are pretreated with BD1063 (0, 4.4, 7 and 11 mg/kg of body weight, free base weights, s.c.) using a within-subject Latin square design. sP rats: Rats are pretreated with BD1063 (0, 3, 4.4, 7 and 11 mg/kg of body weight, free base basis, s.c.) using a within-subject Latin square design[1]. |
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. | |
| Cas No. | 206996-13-6 | SDF | |
| 别名 | BD1063(盐酸盐) | ||
| 化学名 | 1-(3,4-dichlorophenethyl)-4-methylpiperazine dihydrochloride | ||
| Canonical SMILES | CN(CC1)CCN1CCC2=CC(Cl)=C(Cl)C=C2.Cl.Cl | ||
| 分子式 | C13H18Cl2N2.2HCl | 分子量 | 346.13 |
| 溶解度 | DMF: 11 mg/ml,DMSO: 16 mg/ml,Ethanol: 5 mg/ml,PBS (pH 7.2): 10 mg/ml | 储存条件 | Store at RT |
| 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 | 2.8891 mL | 14.4454 mL | 28.8909 mL |
| 5 mM | 0.5778 mL | 2.8891 mL | 5.7782 mL |
| 10 mM | 0.2889 mL | 1.4445 mL | 2.8891 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