Haloperidol

Alias: R1625; HSDB3093; R 1625; HSDB 3093; R-1625; HSDB-3093; Eukystol ;Serenace; Haloperidol; Haldol; Aloperidin; Aloperidol

Cat No.:V22058 Purity: ≥98%

COA Product Data Instructions for use SDS

Haloperidol (R1625; Eukystol; HSDB-3093; Haldol; Serenace; Aloperidin) is a potent antipsychotic medication acting as adopamine D2 receptor antagonist.

Haloperidol Chemical Structure CAS No.: 52-86-8
Product category: Dopamine Receptor

This product is for research use only, not for human use. We do not sell to patients.

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Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information

Product Description

Haloperidol (R1625; Eukystol; HSDB-3093; Haldol; Serenace; Aloperidin) is a potent antipsychotic medication acting as a dopamine D2 receptor antagonist. It is authorized for use in the treatment of acute psychosis, delirium, agitation, nausea and vomiting, tics in Tourette syndrome, schizophrenia, and alcohol withdrawal hallucinations.

Biological Activity I Assay Protocols (From Reference)

Targets

D₂ Receptor

ln Vivo

Haloperidol (1 mg) intra-arterially attenuates the dopamine-induced pancreatic secretion. The action of 10 μg of dopamine in the dog pancreas is completely inhibited by 3 mg of haloperidol[1]. Both haloperidol (10 mg/kg) and chlorpromazine (CPZ, 15 mg/kg), when administered to mice 45 minutes after 50 mg/kg (2 μc) of mescaline, block the altered behavior caused by the drug within 7 to 10 minutes. The disappearance of mescaline is unaffected by haloperidol[2].

Animal Protocol

Swiss-Webster strain male albino mice weighing 33–36 g are used, and 0.5 mL of each substance is administered intraperitoneally (i.p.). The time-form imydrochlorides CPZ, haloperidoi, and mescaline are all prepared as dose solutions with concentrations of 1.0, 0.66, and 3.3 mg/mL of 0.9% saline, respectively. These are the doses: 50 mg/kg of mescaline; 10 mg/kg of haloperidol; and 15 mg/kg of CPZ. Before mescaline is given to the mice, either CPZ or haloperidol is administered 30 minutes beforehand. Sometimes, 45 minutes after mescaline injection, CPZ is administered. Individual animals are kept in plexiglass cages, and they are observed for their general behavior and locomotor activity. Mice are beheaded in groups and sacrificed at predetermined intervals following the mescaline injection. Separated plasma is kept in storage at -20°C. The liver, heart, spleen, lung, kidney, and brain are frozen on dry ice and kept at -20°C for a minimum of 18 to 20 hours prior to their use in tests.

References

[1]. Effects of enzyme inhibitors of catecholamine metabolism and of haloperidol on the pancreatic secretion induced by L-DOPA and by dopamine in dogs. Br J Pharmacol. 1973 Jan;47(1):77-84.

[2]. Effects of chlorpromazine and haloperidol on the disposition of mescaline-14C in mice. J Pharmacol Exp Ther. 1973 Aug;186(2):297-304.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula	C21H23CLFNO2
Molecular Weight	375.86
Exact Mass	375.14
Elemental Analysis	C, 67.11; H, 6.17; Cl, 9.43; F, 5.05; N, 3.73; O, 8.51
CAS #	52-86-8
Related CAS #	Haloperidol-d4; 1189986-59-1; Haloperidol-d4-1; 136765-35-0; Haloperidol hydrochloride; 1511-16-6; Haloperidol lactate; 53515-91-6; Haloperidol-d4 N-Oxide; 1246815-56-4; Haloperidol-13C6
Appearance	White to light yellow crystalline powder.
SMILES	C1CN(CCC1(C2=CC=C(C=C2)Cl)O)CCCC(=O)C3=CC=C(C=C3)F
InChi Key	LNEPOXFFQSENCJ-UHFFFAOYSA-N
InChi Code	InChI=1S/C21H23ClFNO2/c22-18-7-5-17(6-8-18)21(26)11-14-24(15-12-21)13-1-2-20(25)16-3-9-19(23)10-4-16/h3-10,26H,1-2,11-15H2
Chemical Name	4-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-1-(4-fluorophenyl)butan-1-one
Synonyms	R1625; HSDB3093; R 1625; HSDB 3093; R-1625; HSDB-3093; Eukystol ;Serenace; Haloperidol; Haldol; Aloperidin; Aloperidol
HS Tariff Code	2934.99.9001
Storage	Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)	DMSO: ~100 mg/mL (~266.1 mM)
Solubility (In Vivo)	Solubility in Formulation 1: ≥ 1.67 mg/mL (4.44 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 1.67 mg/mL (4.44 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More Solubility in Formulation 3: ≥ 1.67 mg/mL (4.44 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.)

Solubility (In Vitro)

DMSO: ~100 mg/mL (~266.1 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 1.67 mg/mL (4.44 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: 1.67 mg/mL (4.44 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

View More

Solubility in Formulation 3: ≥ 1.67 mg/mL (4.44 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
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The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

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The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

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The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

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Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03021486	Active Recruiting	Other: Chlorpromazine Drug: Haloperidol	Delirium Advanced Malignant Neoplasm	M.D. Anderson Cancer Center	June 5, 2017	Phase 2 Phase 3
NCT01949662	Active Recruiting	Drug: Placebo Drug: Haloperidol decanoate	Advanced Cancers	M.D. Anderson Cancer Center	January 2014	Phase 2
NCT03392376	Active Recruiting	Drug: Haloperidol Injection Other: Saline (0,9%)	Delirium	Zealand University Hospital	June 13, 2018	Phase 4
NCT04750395	Recruiting	Drug: Haloperidol Solution Drug: Olanzapine Tablets	Delirium Terminal Illness	HCA Hospice Care	September 1, 2021	Phase 2
NCT03743649	Recruiting	Drug: Haloperidol Drug: Lorazepam	Delirium Metastatic Malignant Neoplasm	M.D. Anderson Cancer Center	July 17, 2019	Phase 2 Phase 3