Haloperidol
(Synonyms: 氟哌啶醇) 目录号 : GC17599
Haloperidol是一种典型的抗精神病药和多巴胺D2样受体拮抗剂，也是离子通道抑制剂，可抑制多种离子通道，如G蛋白激活的内向整流钾通道、钙激活钾通道、HERG和HEAG钾通道以及L、N和P型钙通道。
Cas No.:52-86-8
Sample solution is provided at 25 µL, 10mM.
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Haloperidol is a classic antipsychotic and dopamine D2-like receptor antagonist, as well as an ion channel inhibitor that inhibits a variety of ion channels, such as G-protein-activated inwardly rectifying potassium channels, calcium-activated potassium channels, HERG and HEAG potassium channels, as well as L-, N- and P-type calcium channels[1-4].
Haloperidol (5-100 μM) treatment significantly decreased the viability of U87, U251, and T98 cells with IC50 values of 23, 38, and 35 μM, respectively. Haloperidol induced apoptosis of glioblastoma cells in a dose-dependent manner and inhibited cell migration and expression of CD24 and CD44[2]. Nontoxic concentrations of Haloperidol (1-30 μM) showed a dose-dependent enhancement of VBL cytotoxicity in VBL-resistant human leukemia (K562/VBL) cells, but had no similar effect in parent cells[3].
In adult male Sprague-Dawley rats, Haloperidol (0.05 and 2 mg/kg) had no effect on cell proliferation in the dentate gyrus (DG) and the number of surviving newly generated neurons in DG after bromodeoxyuracil (BrdU) administration[4]. In adult male Wistar rats treated with Haloperidol (1-10 mg/kg), levels of the thiobarbituric acid (TBA) active substance (TBAR) in the striatum (ST) were increased and TBAR levels in the cortex (CX) were decreased[5].
References:
[1] Yang S B, Proks P, Ashcroft F M, et al. Inhibition of ATP‐sensitive potassium channels by haloperidol[J]. British journal of pharmacology, 2004, 143(8): 960-967.
[2] Papadopoulos F, Isihou R, Alexiou G A, et al. Haloperidol induced cell cycle arrest and apoptosis in glioblastoma cells[J]. Biomedicines, 2020, 8(12): 595.
[3] Kataoka Y, Ishikawa M, Miura M, et al. Reversal of vinblastine resistance in human leukemic cells by haloperidol and dihydrohaloperidol[J]. Biological and Pharmaceutical Bulletin, 2001, 24(6): 612-617.
[4] Halim N D, Weickert C S, McClintock B W, et al. Effects of chronic haloperidol and clozapine treatment on neurogenesis in the adult rat hippocampus[J]. Neuropsychopharmacology, 2004, 29(6): 1063-1069.
[5] Toru M, Takashima M. Haloperidol in large doses reduces the cataleptic response and increases noradrenaline metabolism in the brain of the rat[J]. Neuropharmacology, 1985, 24(3): 231-236.
| Cell experiment [1]: | |
Cell lines | U87 and U251 cell lines |
Preparation Method | U87 and U251 cells were exposed to increasing concentrations of Haloperidol for 72 h, and cell viability was measured using the MTT assay. |
Reaction Conditions | 5, 10, 20, 50 and 100 μM, 72 h |
Applications | Haloperidol inhibited the viability of U87 and U251 cells with IC50 values of 23 μM and 38 μM, respectively. |
| Animal experiment [2]: | |
Animal models | Adult female Long-Evans rats |
Preparation Method | After intraperitoneal injection of haloperidol, the rats were decapitated and the brain tissue was removed for frozen sections. |
Dosage form | 1, 2.5, 5, 7.5 or 10 mg/kg, 2 h, i.p. |
Applications | Haloperidol in large doses reduces the cataleptic response and increases noradrenaline metabolism in the brain of the rat. |
References: [1] Papadopoulos F, Isihou R, Alexiou G A, et al. Haloperidol induced cell cycle arrest and apoptosis in glioblastoma cells[J]. Biomedicines, 2020, 8(12): 595. [2] Toru M, Takashima M. Haloperidol in large doses reduces the cataleptic response and increases noradrenaline metabolism in the brain of the rat[J]. Neuropharmacology, 1985, 24(3): 231-236. | |
| Cas No. | 52-86-8 | SDF | |
| 别名 | 氟哌啶醇 | ||
| 化学名 | 4-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-1-(4-fluorophenyl)butan-1-one | ||
| Canonical SMILES | C1CN(CCC1(C2=CC=C(C=C2)Cl)O)CCCC(=O)C3=CC=C(C=C3)F | ||
| 分子式 | C21H23ClFNO2 | 分子量 | 375.86 |
| 溶解度 | 100mg/mL in DMSO（ultrasonic and warming and heat to 60°C) | 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 | 2.6606 mL | 13.3028 mL | 26.6057 mL |
| 5 mM | 0.5321 mL | 2.6606 mL | 5.3211 mL |
| 10 mM | 0.2661 mL | 1.3303 mL | 2.6606 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
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- Purity: >98.00%
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