BRL 52537 hydrochloride
(Synonyms: 2-(3,4-二氯苯基)-1-(2-(吡咯烷-1-甲基)哌啶-1-基)乙酮盐酸盐) 目录号 : GC15313
κ/μ opioid receptor agonist,potent and selective
Cas No.:112282-24-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
BRL 52537 hydrochloride is a potent and selective agonist of κ/μ-opioid receptor with Ki value of 0.24 nM for κ-opioid receptor [1].
The κ-opioid receptor (KOR) is a type of opioid receptor for opioid peptide dynorphin and controls addiction. Also, KOR plays an important role in stress, anxiety, anhedonia, depression and increased drug-seeking behavior.
BRL 52537 hydrochloride is a potent and selective κ/μ-opioid receptor agonist. In the mouse tail flick model, BRL 52537 showed antinociception with ED50 value of 0.05 mg/kg, which was 25 times more potent than morphine [1]. In WT male mice with middle cerebral artery occlusion, BRL 52537 significantly decreased infarct volumes at 72 h of reperfusion. However, BRL 52537 had no effect in neuronal NO synthase null mutants (nNOS-/-) mice or in the WT female mice. These results suggested that BRL 52537 exhibited neuroprotection through inhibition of ischemia-evoked NO production and nNOS activity [2]. In adult rat dorsal root ganglia (DRGs), BRL 52537 inhibited tetrodotoxin-resistant (TTX-r) sodium currents in an opioid receptor-independent way, which also contributed to the antinociceptive effects [3]. In rats with cerebral ischemia/reperfusion (I/R) injury, BRL52537 inhibited neuronal apoptosis and brain damage. Also, BRL52537 increased the level of phosphorylated STAT3 and reduced caspase-3 expression [4].
References:
[1]. Vecchietti V, Giordani A, Giardina G, et al. (2S)-1-(arylacetyl)-2-(aminomethyl)piperidine derivatives: novel, highly selective kappa opioid analgesics. J Med Chem, 1991, 34(1): 397-403.
[2]. Zeynalov E, Nemoto M, Hurn PD, et al. Neuroprotective effect of selective kappa opioid receptor agonist is gender specific and linked to reduced neuronal nitric oxide. J Cereb Blood Flow Metab, 2006, 26(3): 414-420.
[3]. Su X, Castle NA, Antonio B, et al. The effect of kappa-opioid receptor agonists on tetrodotoxin-resistant sodium channels in primary sensory neurons. Anesth Analg, 2009, 109(2): 632-640.
[4]. Fang S, Xu H, Lu J, et al. Neuroprotection by the kappa-opioid receptor agonist, BRL52537, is mediated via up-regulating phosphorylated signal transducer and activator of transcription-3 in cerebral ischemia/reperfusion injury in rats. Neurochem Res, 2013, 38(11): 2305-2312.
| Cas No. | 112282-24-3 | SDF | |
| 别名 | 2-(3,4-二氯苯基)-1-(2-(吡咯烷-1-甲基)哌啶-1-基)乙酮盐酸盐 | ||
| 化学名 | 2-(3,4-dichlorophenyl)-1-(2-(pyrrolidin-1-ylmethyl)piperidin-1-yl)ethanone hydrochloride | ||
| Canonical SMILES | ClC1=C(Cl)C=C(CC(N2CCCCC2CN3CCCC3)=O)C=C1.Cl | ||
| 分子式 | C18H24Cl2N2O.HCl | 分子量 | 391.77 |
| 溶解度 | <1.96mg/ml in Water | 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 | 2.5525 mL | 12.7626 mL | 25.5252 mL |
| 5 mM | 0.5105 mL | 2.5525 mL | 5.105 mL |
| 10 mM | 0.2553 mL | 1.2763 mL | 2.5525 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。