Haloperidol (Synonyms: McNJR 1625, NSC 170973, NSC 615296, R 1625) |
| Catalog No.GC17599 |
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.
Products are for research use only. Not for human use. We do not sell to patients.
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 | |
| Synonyms | McNJR 1625, NSC 170973, NSC 615296, R 1625 | ||
| Chemical Name | 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 | ||
| Formula | C21H23ClFNO2 | M.Wt | 375.86 |
| Solubility | 100mg/mL in DMSO（ultrasonic and warming and heat to 60°C) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)
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