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  5. Haloperidol

Haloperidol is a potent dopamine D2 receptor antagonist, widely used as an antipsychotic.

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Haloperidol Chemical Structure

Haloperidol Chemical Structure

CAS No. : 52-86-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 73 In-stock
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10 mM * 1 mL in DMSO USD 73 In-stock
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Based on 14 publication(s) in Google Scholar

Other Forms of Haloperidol:

Haloperidol Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Haloperidol is a potent dopamine D2 receptor antagonist, widely used as an antipsychotic.

IC50 & Target

D2 Receptor

 

In Vivo

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 Mmodeling Methods
Rat: 200-350 g • male Wistar
Administration: 1 mg/KG • i.p. • daily for 31 days
Note
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.
Correlated Product(s): /
Opposite Product(s): /

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 : 16.67 mg/mL (44.35 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
=
Concentration
×
Volume
×
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

×
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: 99.73%

COA (245 KB) LCMS (95 KB)

Handling Instructions (2659 KB)
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
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Haloperidol Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

Haloperidol52-86-8Dopamine ReceptorInhibitorinhibitorinhibit

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