Haloperidol
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MedKoo CAT#: 317987

CAS#: 52-86-8

Description: Haloperidol, marketed under the trade name Haldol, is a typical antipsychotic medication. It is used in the treatment of schizophrenia, tics in Tourette syndrome, nausea and vomiting, delirium, agitation, acute psychosis, and hallucinations in alcohol withdrawal. It may be used by mouth, as an injection into a muscle, or intravenously. Haloperidol typically works within thirty to sixty minutes. A long-acting formulation may be used as an injection every four weeks in people with schizophrenia or related illnesses who either forget or refuse to take the medication by mouth.


Chemical Structure

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Haloperidol
CAS# 52-86-8

Theoretical Analysis

MedKoo Cat#: 317987
Name: Haloperidol
CAS#: 52-86-8
Chemical Formula: C21H23ClFNO2
Exact Mass: 375.14
Molecular Weight: 375.860
Elemental Analysis: C, 67.11; H, 6.17; Cl, 9.43; F, 5.05; N, 3.73; O, 8.51

Price and Availability

Size Price Availability Quantity
1g USD 150
2g USD 250
5g USD 450
10g USD 650
20g USD 950 2 Weeks
Bulk inquiry

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

IUPAC/Chemical Name: 4-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-1-(4-fluorophenyl)butan-1-one

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

SMILES Code: C1CN(CCC1(C2=CC=C(C=C2)Cl)O)CCCC(=O)C3=CC=C(C=C3)F

Appearance: White to light yellow crystalline powder.

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 375.86 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Fragoso VM, Hoppe LY, Araújo-Jorge TC, Azevedo MJ, Campos JD, Cortez CM,
Oliveira GM. Use of haloperidol and risperidone in highly aggressive Swiss
Webster mice by applying the model of spontaneous aggression (MSA). Behav Brain
Res. 2016 Mar 15;301:110-8. doi: 10.1016/j.bbr.2015.12.010. Epub 2015 Dec 14.
PubMed PMID: 26698401.

2: Al-Qadheeb NS, Skrobik Y, Schumaker G, Pacheco MN, Roberts RJ, Ruthazer RR,
Devlin JW. Preventing ICU Subsyndromal Delirium Conversion to Delirium With
Low-Dose IV Haloperidol: A Double-Blind, Placebo-Controlled Pilot Study. Crit
Care Med. 2016 Mar;44(3):583-91. doi: 10.1097/CCM.0000000000001411. PubMed PMID:
26540397; PubMed Central PMCID: PMC4779647.

3: Palasz A, Rojczyk E, Golyszny M, Filipczyk L, Worthington JJ, Wiaderkiewicz R.
Long-term treatment with haloperidol affects neuropeptide S and NPSR mRNA levels
in the rat brain. Acta Neuropsychiatr. 2016 Apr;28(2):110-6. doi:
10.1017/neu.2015.56. Epub 2015 Oct 15. PubMed PMID: 26467816.

4: Carrasco G, Baeza N, Cabré L, Portillo E, Gimeno G, Manzanedo D, Calizaya M.
Dexmedetomidine for the Treatment of Hyperactive Delirium Refractory to
Haloperidol in Nonintubated ICU Patients: A Nonrandomized Controlled Trial. Crit
Care Med. 2016 Feb 29. [Epub ahead of print] PubMed PMID: 26925523.

5: Dold M, Tardy M, Samara MT, Li C, Kasper S, Leucht S. Are all first-generation
antipsychotics equally effective in treating schizophrenia? A meta-analysis of
randomised, haloperidol-controlled trials. World J Biol Psychiatry. 2016 Feb
26:1-11. [Epub ahead of print] PubMed PMID: 26919194.

6: Yamamoto S, Ohta N, Matsumoto A, Horiguchi Y, Koide M, Fujino Y. Haloperidol
Suppresses NF-kappaB to Inhibit Lipopolysaccharide-Induced Pro-Inflammatory
Response in RAW 264 Cells. Med Sci Monit. 2016 Feb 4;22:367-72. PubMed PMID:
26842661; PubMed Central PMCID: PMC4747317.

7: Shen AN, Newland MC. Examination of clozapine and haloperidol in improving
ketamine-induced deficits in an incremental repeated acquisition procedure in
BALB/c mice. Psychopharmacology (Berl). 2016 Feb;233(3):485-98. doi:
10.1007/s00213-015-4120-x. Epub 2015 Oct 29. PubMed PMID: 26514554.

8: Gawlik-Kotelnicka O, Mielicki W, Rabe-Jabłońska J, Lazarek J, Strzelecki D.
Impact of lithium alone or in combination with haloperidol on oxidative stress
parameters and cell viability in SH-SY5Y cell culture. Acta Neuropsychiatr. 2016
Feb;28(1):38-44. doi: 10.1017/neu.2015.47. Epub 2015 Aug 19. PubMed PMID:
26286703.

9: Thomas T, Fang Y, Yuriev E, Chalmers DK. Ligand Binding Pathways of Clozapine
and Haloperidol in the Dopamine D2 and D3 Receptors. J Chem Inf Model. 2016 Feb
22;56(2):308-21. doi: 10.1021/acs.jcim.5b00457. Epub 2016 Feb 2. PubMed PMID:
26690887.

10: Schubert KO, Föcking M, Wynne K, Cotter DR. Proteome and pathway effects of
chronic haloperidol treatment in mouse hippocampus. Proteomics. 2016
Feb;16(3):532-8. doi: 10.1002/pmic.201500242. Epub 2016 Jan 13. PubMed PMID:
26607048.

11: Correa M, Pardo M, Bayarri P, López-Cruz L, San Miguel N, Valverde O, Ledent
C, Salamone JD. Choosing voluntary exercise over sucrose consumption depends upon
dopamine transmission: effects of haloperidol in wild type and adenosine A2AKO
mice. Psychopharmacology (Berl). 2016 Feb;233(3):393-404. doi:
10.1007/s00213-015-4127-3. Epub 2015 Nov 10. PubMed PMID: 26554387.

12: Lisbeth P, Vincent H, Kristof M, Bernard S, Manuel M, Hugo N. Genotype and
co-medication dependent CYP2D6 metabolic activity: effects on serum
concentrations of aripiprazole, haloperidol, risperidone, paliperidone and
zuclopenthixol. Eur J Clin Pharmacol. 2016 Feb;72(2):175-84. doi:
10.1007/s00228-015-1965-1. Epub 2015 Oct 30. PubMed PMID: 26514968.

13: Brettner F, Janitza S, Prüll K, Weninger E, Mansmann U, Küchenhoff H,
Jovanovic A, Pollwein B, Chappell D, Zwissler B, von Dossow V. Gender-Specific
Differences in Low-Dose Haloperidol Response for Prevention of Postoperative
Nausea and Vomiting: A Register-Based Cohort Study. PLoS One. 2016 Jan
11;11(1):e0146746. doi: 10.1371/journal.pone.0146746. eCollection 2016. PubMed
PMID: 26751066; PubMed Central PMCID: PMC4713839.

14: Vandael E, Vandenberk B, Vandenberghe J, Spriet I, Willems R, Foulon V. Risk
management of QTc-prolongation in patients receiving haloperidol: an
epidemiological study in a University hospital in Belgium. Int J Clin Pharm. 2016
Jan 9. [Epub ahead of print] PubMed PMID: 26749342.

15: Datta S, Jamwal S, Deshmukh R, Kumar P. Beneficial effects of lycopene
against haloperidol induced orofacial dyskinesia in rats: Possible
neurotransmitters and neuroinflammation modulation. Eur J Pharmacol. 2016 Jan
15;771:229-35. doi: 10.1016/j.ejphar.2015.12.032. Epub 2015 Dec 19. PubMed PMID:
26712377.

16: Schrijver EJ, de Graaf K, de Vries OJ, Maier AB, Nanayakkara PW. Efficacy and
safety of haloperidol for in-hospital delirium prevention and treatment: A
systematic review of current evidence. Eur J Intern Med. 2016 Jan;27:14-23. doi:
10.1016/j.ejim.2015.10.012. Epub 2015 Nov 6. Review. PubMed PMID: 26553001.

17: Witten L, Bastlund JF, Glenthøj BY, Bundgaard C, Steiniger-Brach B, Mørk A,
Oranje B. Comparing Pharmacological Modulation of Sensory Gating in Healthy
Humans and Rats: The Effects of Reboxetine and Haloperidol.
Neuropsychopharmacology. 2016 Jan;41(2):638-45. doi: 10.1038/npp.2015.194. Epub
2015 Jul 1. PubMed PMID: 26129678.

18: Manchia M, Pinna M, Carpiniello B. Haloperidol and loss of gray matter in
schizophrenia: Reconciling meta-analytical results with molecular pharmacology.
Psychiatry Res. 2016 Jan 30;235:209-10. doi: 10.1016/j.psychres.2015.12.010. Epub
2015 Dec 19. PubMed PMID: 26724909.

19: Slawson MH, Johnson-Davis KL. Quantitation of Haloperidol, Fluphenazine,
Perphenazine, and Thiothixene in Serum or Plasma Using Liquid
Chromatography-Tandem Mass Spectrometry (LC-MS/MS). Methods Mol Biol.
2016;1383:49-57. doi: 10.1007/978-1-4939-3252-8_6. PubMed PMID: 26660173.

20: An HM, Tan YL, Shi J, Wang ZR, Li J, Wang YC, Lv MH, Zhou DF, Soares JC,
Kosten TR, Yang FD, Zhang XY. Beneficial effects of EGb761 and vitamin E on
haloperidol-induced vacuous chewing movements in rats: Possible involvement of
S100B mechanisms. Behav Brain Res. 2016 Jan 15;297:124-30. doi:
10.1016/j.bbr.2015.10.004. Epub 2015 Oct 9. PubMed PMID: 26455874.