1. Induced Disease Models Products GPCR/G Protein Neuronal Signaling
  2. Nervous System Disease Models Dopamine Receptor
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  4. Haloperidol

Haloperidol is a potent dopamine D2 receptor antagonist, widely used as an antipsychotic agent. Haloperidol can be used in the study of schizophrenia, tics in Tourette syndrome, mania in bipolar disorder, delirium, agitation, acute psychosis, and hallucinations from alcohol withdrawal.

For research use only. We do not sell to patients.

CAS No. : 52-86-8

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10 mM * 1 mL in DMSO
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Customer Review

Based on 21 publication(s) in Google Scholar

Other Forms of Haloperidol:

Top Publications Citing Use of Products

    Haloperidol purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Sep;12(33):e02276.  [Abstract]

    Western blotting of DRD1, ALP, OCN, BAX, Bcl2, cleaved‐caspase3, and β‐actin in osteogenesis‐induced BMSCs treated with Haloperidol (1 µM), DA and then stimulated with MP.

    Haloperidol purchased from MedChemExpress. Usage Cited in: ACS Omega. 2025 Oct 17;10(42):50208-50217.  [Abstract]

    Haloperidol (Halo; 20 ng/mL; 24 h). ISR induction by various drugs. N2a cells were treated with the indicated drugs for 24 h. The cell extracts were analyzed by Western blot analysis with anti-ATF4, anti-CHOP, and anti-β actin antibodies.

    Haloperidol purchased from MedChemExpress. Usage Cited in: Clin Exp Pharmacol Physiol. 2021 Mar;48(3):370-380.  [Abstract]

    Haloperidol (10 μM; 48 h). Cell viability was measured by CCK-8 assay. The cells incubated with control medium were considered 100% viable.

    Haloperidol purchased from MedChemExpress. Usage Cited in: Clin Exp Pharmacol Physiol. 2021 Mar;48(3):370-380.  [Abstract]

    Haloperidol (10 μM; 48 h). ROS production in HSCs measured by staining with DCFH-DA and imaged by fluorescent microscopy.

    Haloperidol purchased from MedChemExpress. Usage Cited in: Clin Exp Pharmacol Physiol. 2021 Mar;48(3):370-380.  [Abstract]

    Haloperidol (10 μM; 48 h). Immunoblotting and optical density analysis of DRD2 and NOX-5, and the data were normalized to GAPDH.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Haloperidol is a potent dopamine D2 receptor antagonist, widely used as an antipsychotic agent. Haloperidol can be used in the study of schizophrenia, tics in Tourette syndrome, mania in bipolar disorder, delirium, agitation, acute psychosis, and hallucinations from alcohol withdrawal.

    IC50 & Target

    D2 Receptor

     

    Cellular Effect
    Cell Line Type Value Description References
    5637 IC50
    2.3 μM
    Compound: Haloperidol
    Growth inhibition of human 5637 cells incubated for 96 hrs by crystal violet assay
    Growth inhibition of human 5637 cells incubated for 96 hrs by crystal violet assay
    [PMID: 27156565]
    5637 IC50
    > 20 μM
    Compound: Haloperidol
    Cytotoxicity against human 5637 cells after 96 hrs by crystal violet staining
    Cytotoxicity against human 5637 cells after 96 hrs by crystal violet staining
    [PMID: 19243173]
    A-427 IC50
    10 μM
    Compound: Haloperidol
    Growth inhibition of human A427 cells after 96 hrs
    Growth inhibition of human A427 cells after 96 hrs
    [PMID: 17967001]
    A-427 IC50
    10 μM
    Compound: Haloperidol
    Cytotoxicity against human A427 cells after 96 hrs by crystal violet staining
    Cytotoxicity against human A427 cells after 96 hrs by crystal violet staining
    [PMID: 19243173]
    A-427 IC50
    9.6 μM
    Compound: Haloperidol
    Growth inhibition of human A427 cells incubated for 96 hrs by crystal violet assay
    Growth inhibition of human A427 cells incubated for 96 hrs by crystal violet assay
    [PMID: 27156565]
    CHO IC50
    0.006 μM
    Compound: haloperidol
    Inhibitory concentration against human Dopamine receptor D4.2 in CHO cells
    Inhibitory concentration against human Dopamine receptor D4.2 in CHO cells
    [PMID: 8831770]
    CHO IC50
    1.1 μM
    Compound: Haloperidol
    Inhibition of human ERG expressed in CHO cells after 30 mins by Rb+ flux assay
    Inhibition of human ERG expressed in CHO cells after 30 mins by Rb+ flux assay
    [PMID: 22677319]
    CHO IC50
    1.3 μM
    Compound: haloperidol
    Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
    Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
    [PMID: 23812503]
    CHO IC50
    32 nM
    Compound: haloperidol
    Inhibition of K+ channel activity in CHO cells expressing HERG Kv11.1
    Inhibition of K+ channel activity in CHO cells expressing HERG Kv11.1
    [PMID: 12729675]
    CHO IC50
    4.8 nM
    Compound: Haloperidol
    Binding affinity to rat Dopamine receptor D2 expressed in CHO cells was determined using [125 I ] iodosulpride as radioligand
    Binding affinity to rat Dopamine receptor D2 expressed in CHO cells was determined using [125 I ] iodosulpride as radioligand
    [PMID: 8759642]
    CHO-K1 IC50
    0.16 nM
    Compound: Haloperidol
    Antagonist activity against human D2LR expressed in CHOK1 cells assessed as inhibition of pergolide-induced beta-arrestin translocation by beta-galactosidase based beta-arrestin recruitment assay
    Antagonist activity against human D2LR expressed in CHOK1 cells assessed as inhibition of pergolide-induced beta-arrestin translocation by beta-galactosidase based beta-arrestin recruitment assay
    [PMID: 25126833]
    CHO-K1 IC50
    5500 nM
    Compound: 5
    Inhibition of binding of 1.0 nM [3H]pirenzepine to cloned human Muscarinic acetylcholine receptor M1 expressed in membranes from CHO-K1 cells
    Inhibition of binding of 1.0 nM [3H]pirenzepine to cloned human Muscarinic acetylcholine receptor M1 expressed in membranes from CHO-K1 cells
    [PMID: 10377229]
    CHO-K1 IC50
    5500 nM
    Compound: haloperidol
    Inhibitory binding of [3H]pirenzepine to human Muscarinic acetylcholine receptor M1 in membranes from CHO-K1 cells
    Inhibitory binding of [3H]pirenzepine to human Muscarinic acetylcholine receptor M1 in membranes from CHO-K1 cells
    [PMID: 9406603]
    CHO-hD3 IC50
    8.8 nM
    Compound: Haloperidol
    Compound was tested for stimulation of mitogenesis in CHO.hD3 cells in a dose dependent manner
    Compound was tested for stimulation of mitogenesis in CHO.hD3 cells in a dose dependent manner
    [PMID: 9873609]
    DAN-G IC50
    > 20 μM
    Compound: Haloperidol
    Growth inhibition of human DAN-G cells incubated for 96 hrs by crystal violet assay
    Growth inhibition of human DAN-G cells incubated for 96 hrs by crystal violet assay
    [PMID: 27156565]
    HEK293 EC50
    > 10000 nM
    Compound: Haloperidol
    Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5
    Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5
    [PMID: 15380206]
    HEK293 IC50
    0.23 μM
    Compound: haloperidol
    Inhibition of human ERG expressed in HEK293 cells coexpressing Kir2.3 after 30 mins by FluxOR based FLIPR assay
    Inhibition of human ERG expressed in HEK293 cells coexpressing Kir2.3 after 30 mins by FluxOR based FLIPR assay
    [PMID: 22694270]
    HEK293 IC50
    0.55 μM
    Compound: Haloperidol
    Antagonist activity at dopamine D2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay
    Antagonist activity at dopamine D2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay
    [PMID: 23332346]
    HEK293 IC50
    0.7 nM
    Compound: Haloperidol
    Antagonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assay
    Antagonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assay
    [PMID: 24831693]
    HEK293 IC50
    1.16 μM
    Compound: Haloperidol
    Inhibition of human ERG expressed in HEK293 cells measured after 30 mins by FluxOR dye based FLIPR TETRA assay
    Inhibition of human ERG expressed in HEK293 cells measured after 30 mins by FluxOR dye based FLIPR TETRA assay
    [PMID: 32392053]
    HEK293 IC50
    141.9 μM
    Compound: haloperidole
    Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
    Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
    [PMID: 18788725]
    HL-60 IC50
    > 20 μM
    Compound: Haloperidol
    Growth inhibition of human HL60 cells incubated for 48 hrs by MTT assay
    Growth inhibition of human HL60 cells incubated for 48 hrs by MTT assay
    [PMID: 27156565]
    Jurkat IC50
    0.021 μM
    Compound: haloperidol
    Displacement of [3H]Haloperidol from sigma 1 receptor in human jurkat cells after 4 hrs
    Displacement of [3H]Haloperidol from sigma 1 receptor in human jurkat cells after 4 hrs
    [PMID: 23403082]
    Jurkat IC50
    1.7 x 10-8 M
    Compound: Haloperidol
    Displacement of [3H]DTG from sigma receptor in human jurkat cells
    Displacement of [3H]DTG from sigma receptor in human jurkat cells
    [PMID: 26988801]
    Jurkat IC50
    1.7 x 10-8 M
    Compound: Haloperidol
    Displacement of [3H]DTG from sigma receptor in human Jurkat cells measured after 120 mins by scintillation counting method
    Displacement of [3H]DTG from sigma receptor in human Jurkat cells measured after 120 mins by scintillation counting method
    [PMID: 27876250]
    Jurkat IC50
    230 nM
    Compound: haloperidol
    Displacement of [3H](+)-pentazocine from sigma 1 opioid receptor in human Jurkat cells by scintillation counting
    Displacement of [3H](+)-pentazocine from sigma 1 opioid receptor in human Jurkat cells by scintillation counting
    [PMID: 19875205]
    MCF7 IC50
    20.17 μM
    Compound: Haloperidol
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
    [PMID: 31042618]
    MCF7 IC50
    24.9 μM
    Compound: Haloperidol
    Growth inhibition of human MCF7 cells after 96 hrs
    Growth inhibition of human MCF7 cells after 96 hrs
    [PMID: 17967001]
    MCF7 IC50
    68 μM
    Compound: Halo
    Cytotoxicity against ER/PR-positive HER2-negative human MCF7 cells harbouring p53 R175H mutant assessed as inhibition of cell growth incubated for 48 hrs by resazurin dye based assay
    Cytotoxicity against ER/PR-positive HER2-negative human MCF7 cells harbouring p53 R175H mutant assessed as inhibition of cell growth incubated for 48 hrs by resazurin dye based assay
    [PMID: 35724925]
    MCF7 IC50
    > 20 μM
    Compound: Haloperidol
    Cytotoxicity against human MCF7 cells after 96 hrs by crystal violet staining
    Cytotoxicity against human MCF7 cells after 96 hrs by crystal violet staining
    [PMID: 19243173]
    MCF7 IC50
    > 20 μM
    Compound: Haloperidol
    Growth inhibition of human MCF7 cells incubated for 96 hrs by crystal violet assay
    Growth inhibition of human MCF7 cells incubated for 96 hrs by crystal violet assay
    [PMID: 27156565]
    RT-4 IC50
    16 μM
    Compound: Haloperidol
    Growth inhibition of human RT4 cells incubated for 96 hrs by crystal violet assay
    Growth inhibition of human RT4 cells incubated for 96 hrs by crystal violet assay
    [PMID: 27156565]
    RT-4 IC50
    > 20 μM
    Compound: Haloperidol
    Cytotoxicity against human RT4 cells after 96 hrs by crystal violet staining
    Cytotoxicity against human RT4 cells after 96 hrs by crystal violet staining
    [PMID: 19243173]
    SK-BR-3 IC50
    131 μM
    Compound: Halo
    Cytotoxicity against ER/PR-negative HER2-positive human SK-BR-3 cells harbouring wild type p53 assessed as inhibition of cell growth incubated for 48 hrs by resazurin dye based assay
    Cytotoxicity against ER/PR-negative HER2-positive human SK-BR-3 cells harbouring wild type p53 assessed as inhibition of cell growth incubated for 48 hrs by resazurin dye based assay
    [PMID: 35724925]
    ScN2a EC50
    > 10 μM
    Compound: Haloperidol
    Half maximal inhibition of Prion protein PrPsc formation was assayed in ScN2a cells
    Half maximal inhibition of Prion protein PrPsc formation was assayed in ScN2a cells
    [PMID: 12904059]
    U2OS IC50
    0.06 nM
    Compound: Haloperidol
    Antagonist activity against D3R in human U2OS cells assessed as inhibition of (+)-PD128907-induced beta-arrestin translocation by beta-galactosidase based beta-arrestin recruitment assay
    Antagonist activity against D3R in human U2OS cells assessed as inhibition of (+)-PD128907-induced beta-arrestin translocation by beta-galactosidase based beta-arrestin recruitment assay
    [PMID: 25126833]
    In Vivo

    Note:
    Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.

    Haloperidol can be used to create tardive dyskinesia models. In rats, the oral half-life of Haloperidol is 5.9 hours, with a Tmax of 0.9 hours, a Cmax of 6.8 ng/mL, and an oral bioavailability of 23.0%. When administered intravenously, the AUC0-∞ of Haloperidol is 188.4 ng·h/mL, and the t1/2 is 2.9 hours[3].

    Induction oftardive dyskinesia[4]
    Background
    Haloperidolreduces gene expression of superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GHP), thus reducing the complex cellular antioxidant defenses and increasing lipid peroxidation and nitrite/nitrate levels in the prefrontal cortex, hippocampus, and striatum[4].
    Specific Modeling Methods
    Rat: 200-350 g • male Wistar
    Administration: 1 mg/KG • i.p. • daily for 31 days
    Modeling Indicators
    Behavior: Showed a significant reduction of locomotor activity in the open field test and also developed a cataleptic state, vacuous chewing movements (VCM), and tongue protrusion.

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    Molecular Weight

    375.86

    Formula

    C21H23ClFNO2

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    ClC(C=C1)=CC=C1C2(O)CCN(CCCC(C3=CC=C(F)C=C3)=O)CC2

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 40 mg/mL (106.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Concentration
    ×
    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 1.67 mg/mL (4.44 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 1.67 mg/mL (4.44 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 1.67 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.69%

    References
    Animal Administration
    [2]

    Male albino mice of Swiss-Webster strain (33-36 g) are used, and all substances are given by i.p. injection in a volume of 0.5 mL. CPZ, haloperidoi and mescaline are all in time form of timeir imydrochlorides and the dose solutions are prepared at concentrations of 1.0, 0.66 and 3.3 mg/mL of 0.9% saline, respectively. The doses are: CPZ, 15 mg/kg; haloperidol, 10 mg/kg; mescaline, 50 mg/kg. Mice are pretreated with either CPZ or haloperidol 30 minutes before administration of mescaline. In some instances CPZ is injected 45 minutes after mescaline. Time animals are hmoused individually in a plexiglas cage and the gross behavior and locomotor activity. At selected intervals after mescaline, groups of mice are sacrificed by decapitation. Plasma is separated and stored at -20°C. The brain, liver, kidney, lung, spleen and heart are frozen on dry ice and stored at -20°C for 18 to 20 hours before they are used for assays.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.6606 mL 13.3028 mL 26.6057 mL 66.5141 mL
    5 mM 0.5321 mL 2.6606 mL 5.3211 mL 13.3028 mL
    10 mM 0.2661 mL 1.3303 mL 2.6606 mL 6.6514 mL
    15 mM 0.1774 mL 0.8869 mL 1.7737 mL 4.4343 mL
    20 mM 0.1330 mL 0.6651 mL 1.3303 mL 3.3257 mL
    25 mM 0.1064 mL 0.5321 mL 1.0642 mL 2.6606 mL
    30 mM 0.0887 mL 0.4434 mL 0.8869 mL 2.2171 mL
    40 mM 0.0665 mL 0.3326 mL 0.6651 mL 1.6629 mL
    50 mM 0.0532 mL 0.2661 mL 0.5321 mL 1.3303 mL
    60 mM 0.0443 mL 0.2217 mL 0.4434 mL 1.1086 mL
    80 mM 0.0333 mL 0.1663 mL 0.3326 mL 0.8314 mL
    100 mM 0.0266 mL 0.1330 mL 0.2661 mL 0.6651 mL
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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
    Haloperidol
    Cat. No.:
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