HALOPERIDOL

Details

Stereochemistry	ACHIRAL
Molecular Formula	C21H23ClFNO2
Molecular Weight	375.864
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OC1(CCN(CCCC(=O)C2=CC=C(F)C=C2)CC1)C3=CC=C(Cl)C=C3

InChI

InChIKey=LNEPOXFFQSENCJ-UHFFFAOYSA-N

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

HIDE SMILES / InChI

Description
Sources: http://www.drugbank.ca/drugs/DB00502
Curator's Comment: Description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2011/015923s079lbl.pdf

Haloperidol is a phenyl-piperidinyl-butyrophenone that is used primarily to treat schizophrenia and other psychoses. It is also used in schizoaffective disorder, delusional disorders, ballism, and Tourette syndrome (a drug of choice) and occasionally as adjunctive therapy in mental retardation and the chorea of Huntington disease. It is a potent antiemetic and is used in the treatment of intractable hiccups. Haloperidol also exerts sedative and antiemetic activity. Haloperidol principal pharmacological effects are similar to those of piperazine-derivative phenothiazines. The drug has action at all levels of the central nervous system-primarily at subcortical levels-as well as on multiple organ systems. Haloperidol has strong antiadrenergic and weaker peripheral anticholinergic activity; ganglionic blocking action is relatively slight. It also possesses slight antihistaminic and antiserotonin activity. The precise mechanism whereby the therapeutic effects of haloperidol are produced is not known, but the drug appears to depress the CNS at the subcortical level of the brain, midbrain, and brain stem reticular formation. Haloperidol seems to inhibit the ascending reticular activating system of the brain stem (possibly through the caudate nucleus), thereby interrupting the impulse between the diencephalon and the cortex. The drug may antagonize the actions of glutamic acid within the extrapyramidal system, and inhibitions of catecholamine receptors may also contribute to haloperidol's mechanism of action. Haloperidol may also inhibit the reuptake of various neurotransmitters in the midbrain, and appears to have a strong central antidopaminergic and weak central anticholinergic activity. The drug produces catalepsy and inhibits spontaneous motor activity and conditioned avoidance behaviours in animals. The exact mechanism of antiemetic action of haloperidol has also not been fully determined, but the drug has been shown to directly affect the chemoreceptor trigger zone (CTZ) through the blocking of dopamine receptors in the CTZ. Haloperidol is marketed under the trade name Haldol among others.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Dopamine D4 receptor 71 Target ID: CHEMBL219 Sources: https://www.ncbi.nlm.nih.gov/pubmed/14611858	Inverse Agonist 80	17.0 nM [EC50]
Dopamine D2 receptor 297 Target ID: CHEMBL217 Sources: http://www.drugbank.ca/drugs/DB00502	Antagonist 2778
Serotonin 2a (5-HT2a) receptor 231 Target ID: CHEMBL224 Sources: https://www.ncbi.nlm.nih.gov/pubmed/7520908	Antagonist 2778	53.0 nM [EC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Schizophrenia 298 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2011/015923s079lbl.pdf	Primary		Approved 8429	HALDOL Approved Use HALDOL (haloperidol) is indicated for use in the treatment of schizophrenia. HALDOL is indicated for the control of tics and vocal utterances of Tourette’s Disorder. Launch Date 1986
Tourette's syndrome 20 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2011/015923s079lbl.pdf	Primary		Approved 8429	HALDOL Approved Use HALDOL (haloperidol) is indicated for use in the treatment of schizophrenia. HALDOL is indicated for the control of tics and vocal utterances of Tourette’s Disorder. Launch Date 1986

Doses

Dose	Population	Adverse events
0.9 mg single, oral Overdose Dose: 0.9 mg Route: oral Route: single Dose: 0.9 mg Sources: https://pubmed.ncbi.nlm.nih.gov/28128816	unknown, 11 years n = 1 Health Status: unknown Age Group: 11 years Sex: M Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/28128816	Other AEs: Drowsiness... Other AEs: Drowsiness (1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/28128816
2 mg 4 times / day multiple, intramuscular Recommended Dose: 2 mg, 4 times / day Route: intramuscular Route: multiple Dose: 2 mg, 4 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/015923s093s098,018701s071s076lbl.pdf	unhealthy, adult Health Status: unhealthy Condition: dementia-related psychosis Age Group: adult Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/015923s093s098,018701s071s076lbl.pdf	Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/015923s093s098,018701s071s076lbl.pdf
5 mg 3 times / day multiple, oral Recommended Dose: 5 mg, 3 times / day Route: oral Route: multiple Dose: 5 mg, 3 times / day Sources: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=c559b0b0-4087-d12a-e718-c18ccb6811e6	unhealthy, adult Health Status: unhealthy Condition: dementia-related psychosis Age Group: adult Sources: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=c559b0b0-4087-d12a-e718-c18ccb6811e6	Sources: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=c559b0b0-4087-d12a-e718-c18ccb6811e6
10 mg 2 times / day steady, intravenous Dose: 10 mg, 2 times / day Route: intravenous Route: steady Dose: 10 mg, 2 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT01211522	unhealthy n = 192 Health Status: unhealthy Condition: Delirium Population Size: 192 Sources: https://clinicaltrials.gov/ct2/show/NCT01211522	Other AEs: Torsades de pointes, Electrocardiogram QTc interval prolonged... Other AEs: Torsades de pointes (serious, 2 patients) Electrocardiogram QTc interval prolonged (below serious, 13 patients) Sources: https://clinicaltrials.gov/ct2/show/NCT01211522
10 mg 2 times / day steady, oral Dose: 10 mg, 2 times / day Route: oral Route: steady Dose: 10 mg, 2 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT00129220	unhealthy n = 20 Health Status: unhealthy Condition: Bipolar I Disorder Population Size: 20 Sources: https://clinicaltrials.gov/ct2/show/NCT00129220	Other AEs: Cheilitis, Constipation... Other AEs: Cheilitis (below serious, 1 patient) Constipation (below serious, 2 patients) Salivary hypersecretion (below serious, 1 patient) Vomiting (below serious, 1 patient) Malaise (below serious, 2 patients) Thirst (below serious, 1 patient) Fall (below serious, 1 patient) Blood pressure decreased (below serious, 1 patient) Weight increased (below serious, 1 patient) Increased appetite (below serious, 1 patient) Arthralgia (below serious, 1 patient) Osteoarthritis (below serious, 1 patient) Akathisia (below serious, 3 patients) Dystonia (below serious, 3 patients) Headache (below serious, 1 patient) Sedation (below serious, 1 patient) Tremor (below serious, 2 patients) Depressive symptom (below serious, 1 patient) Insomnia (below serious, 1 patient) Mania (below serious, 1 patient) Pruritus (below serious, 1 patient) Sources: https://clinicaltrials.gov/ct2/show/NCT00129220

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1737 inhibitor 1587	substrate 1037 inhibitor 1767	substrate 1217 activator 23 inhibitor 1852	inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2J2 16 P-gp 1461 OCT1 512 BCRP 699 MRP2 383 MDR3 8 Kv4.3 16 CYP1A2 1524 CYP2A6 707 CYP2C8 911 CYP2C19 1478 CYP2E1 882 BSEP 402 MRP3 157 MRP4 204 OATP1B1 788 OATP1B3 706	CYP1A2 1054 CYP1A1 349 CYP2C8 693 CYP2C19 991 CYP3A5 395 UGT 192 UGT1A1 418 UGT1A3 422 UGT1A4 347 UGT1A6 307 UGT1A9 380 UGT2B7 389 UGT2B15 203 P-gp 1537 OCT1 327 MATE1 135

Drug as perpetrator

Target	Modality	Activity
CYP2D6 1891	inhibitor 3277 Sources: https://link.springer.com/article/10.1007/s40262-016-0407-2/tables/3 \| https://pubmed.ncbi.nlm.nih.gov/10460810/	moderate [Ki 7.2 uM]
CYP2A6 739	inhibitor 3277 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkw1MjgyIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDU0In19	no [IC50 >10 uM]
CYP2E1 970	inhibitor 3277 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkw1MjgxIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDU0In19	no [IC50 >10 uM]
MRP2 475	inhibitor 3277 Sources: https://pubmed.ncbi.nlm.nih.gov/19421845/, https://pubmed.ncbi.nlm.nih.gov/23956101/, https://pubmed.ncbi.nlm.nih.gov/18457386/	no [IC50 >133 uM]
MRP3 207	inhibitor 3277 Sources: https://pubmed.ncbi.nlm.nih.gov/23956101/	no [IC50 >133 uM]
MRP4 238	inhibitor 3277 Sources: https://pubmed.ncbi.nlm.nih.gov/23956101/	no [IC50 >133 uM]
CYP2C8 965	inhibitor 3277 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3336800/	no [IC50 >30 uM]
CYP1A2 1692	inhibitor 3277 Sources: https://pubmed.ncbi.nlm.nih.gov/9431831/, https://pubmed.ncbi.nlm.nih.gov/23033255/	no [IC50 >50 uM]
BCRP 773	inhibitor 3277 Sources: https://pubmed.ncbi.nlm.nih.gov/19421845/	no
CYP2C9 1819	inhibitor 3277 Sources: https://pubmed.ncbi.nlm.nih.gov/9431831/, https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzMzk3IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDU0In19	yes [Activation 31.6228 uM]
MDR3 9	inhibitor 3277 Sources: https://pubmed.ncbi.nlm.nih.gov/26335978/	yes [IC50 10.7 uM]
OCT1 543	inhibitor 3277 Sources: https://pubmed.ncbi.nlm.nih.gov/18788725/	yes [IC50 141.9 uM]
CYP2C19 1553	inhibitor 3277 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3336800/	yes [IC50 2.87 uM]
BSEP 403	inhibitor 3277 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5891329/, https://pubmed.ncbi.nlm.nih.gov/23956101/	yes [IC50 25.3 uM]
P-gp 1650	inhibitor 3277 Sources: https://pubmed.ncbi.nlm.nih.gov/16810505/	yes [IC50 25.4 uM]
Kv4.3 16	inhibitor 3277 Sources: https://pubmed.ncbi.nlm.nih.gov/24998874/	yes [IC50 3.6 uM]
CYP2J2 19	inhibitor 3277 Sources: https://pubmed.ncbi.nlm.nih.gov/23033255/	yes [IC50 4.69 uM]
CYP3A4 1925	inhibitor 3277 Sources: https://pubmed.ncbi.nlm.nih.gov/9431831/, https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3336800/	yes [IC50 8.2 uM]
CYP2D6 1891	activator 214 Sources: https://pubmed.ncbi.nlm.nih.gov/9681669/, https://bioinformatics.charite.de/transformer/index.php?site=fullinfo&cname=000052868	yes
OATP1B1 803	inhibitor 3277 Sources: https://pubmed.ncbi.nlm.nih.gov/23571415/	yes
OATP1B3 715	inhibitor 3277 Sources: https://pubmed.ncbi.nlm.nih.gov/23571415/	yes

Drug as victim

Target	Modality	Activity	Clinical evidence
P-gp 1537	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/12031686/	likely [Km 33 uM]
UGT 192	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/015923s093s098,018701s071s076lbl.pdf#page=8 Page: (Label) 8, 27	major
UGT2B7 389	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/32294459/	major
CYP2D6 1217	substrate 3367 Sources: https://link.springer.com/article/10.1007/s40262-016-0407-2/tables/3, https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/015923s093s098,018701s071s076lbl.pdf#page=9, https://ncit-stage.nci.nih.gov/ncitbrowser/pages/concept_details.jsf?dictionary=NCI_Thesaurus&version=21.02d&code=C537&ns=ncit&type=relationship&key=113214754&b=1&n=0&vse=null Page: (Label) 9, 28	major	yes (co-administration study) Comment: Coadministration of CYP2D6 inhibitors (chlorpromazine, promethazine, quinidine, paroxetine, sertraline, venlafaxine) increased Haloperidol plasma concentrations. Sources: https://link.springer.com/article/10.1007/s40262-016-0407-2/tables/3, https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/015923s093s098,018701s071s076lbl.pdf#page=9, https://ncit-stage.nci.nih.gov/ncitbrowser/pages/concept_details.jsf?dictionary=NCI_Thesaurus&version=21.02d&code=C537&ns=ncit&type=relationship&key=113214754&b=1&n=0&vse=null Page: (Label) 9, 28
CYP3A4 1737	substrate 3367 Sources: https://link.springer.com/article/10.1007/s40262-016-0407-2/tables/3, https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/015923s093s098,018701s071s076lbl.pdf#page=9, https://ncit-stage.nci.nih.gov/ncitbrowser/pages/concept_details.jsf?dictionary=NCI_Thesaurus&version=21.02d&code=C537&ns=ncit&type=relationship&key=113214754&b=1&n=0&vse=null Page: (Label) 9, 28	major	yes (co-administration study) Comment: Coadministration of Rifampicin (strong CYP3A4 inducer) decreased plasma Haloperidol levels by a mean of 70%. Sources: https://link.springer.com/article/10.1007/s40262-016-0407-2/tables/3, https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/015923s093s098,018701s071s076lbl.pdf#page=9, https://ncit-stage.nci.nih.gov/ncitbrowser/pages/concept_details.jsf?dictionary=NCI_Thesaurus&version=21.02d&code=C537&ns=ncit&type=relationship&key=113214754&b=1&n=0&vse=null Page: (Label) 9, 28
CYP1A2 1054	substrate 3367 Sources: https://link.springer.com/article/10.1007/s40262-016-0407-2/tables/3, https://ncit-stage.nci.nih.gov/ncitbrowser/pages/concept_details.jsf?dictionary=NCI_Thesaurus&version=21.02d&code=C537&ns=ncit&type=relationship&key=113214754&b=1&n=0&vse=null	minor
UGT1A4 347	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/32294459/	minor
UGT1A9 380	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/32294459/	minor
UGT1A1 418	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/32294459/	no
UGT1A3 422	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/32294459/	no
UGT1A6 307	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/32294459/	no
UGT2B15 203	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/32294459/	no
CYP1A1 349	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/11717183/	yes
CYP2C19 991	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/11717183/	yes
CYP2C8 693	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/11717183/	yes
CYP2C9 1037	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/11717183/	yes
CYP3A5 395	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/11717183/	yes
MATE1 135	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/31842924/	yes
OCT1 327	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/31842924/	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1647	inhibitor 1626 Sources: https://pubmed.ncbi.nlm.nih.gov/18448342/, https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/015923s093s098,018701s071s076lbl.pdf#page=9, https://bpspubs.onlinelibrary.wiley.com/doi/epdf/10.1038/sj.bjp.0705025 Page: (Label) 9, 28

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:5613	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:5613
ChemicalBook	CB32131152	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB32131152
ChemicalBook	CB72509133	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB72509133
ChemicalBook	CB7774829	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB7774829
MolPort	MolPort-000-883-311	https://www.molport.com/shop/molecule-link/MolPort-000-883-311
Selleck Chemicals	Haloperidol(Haldol)	http://www.selleckchem.com/products/Haloperidol(Haldol).html
ZINC	ZINC000000537822	http://zinc15.docking.org/substances/ZINC000000537822
eMolecules	538987	https://www.emolecules.com/cgi-bin/more?vid=538987

PubMed

Title	Date	PubMed
Extrapyramidal reactions and amine metabolites in cerebrospinal fluid during haloperidol and clozapine treatment of schizophrenic patients.	1975	1096218
A comparative study of haloperidol and chlorpromazine in terms of clinical effects and therapeutic reversal with benztropine in schizophrenia. Theoretical implications for potency differences among neuroleptics.	1975 Aug 21	1103205
Atypical tardive dyskinesia.	1975 May	1119614
Drug-induced dystonia.	1975 May	1119613
Effect of drugs influencing central serotonergic mechanisms on haloperidol-induced catalepsy.	1979 Mar 29	108749
Haloperidol-induced within-session response decrement patterns and catalepsy in rats: behavioural dissociation.	1999 Feb	10780307
Quinpirole, 8-OH-DPAT and ketanserin modulate catalepsy induced by high doses of atypical antipsychotics.	1999 Nov	10669905
[The neurochemical mechanisms of the formation and consolidation of haloperidol-induced catalepsy].	1999 Nov-Dec	10693278
Detection and mapping of quantitative trait loci for haloperidol-induced catalepsy in a C57BL/6J x DBA/2J F2 intercross.	1999 Sep	10765558
The role of metabotropic glutamate receptor (mGluR) ligands in parkinsonian muscle rigidity.	2000	11026478
Effect of muscarinic receptor agonists on animal models of psychosis.	2000 Apr	10893700
Inhibition by various antipsychotic drugs of the G-protein-activated inwardly rectifying K(+) (GIRK) channels expressed in xenopus oocytes.	2000 Apr	10780978
Estrogen priming modulates autoreceptor-mediated potentiation of dopamine uptake.	2000 Aug 11	10936494
Effect of genetic cross on the detection of quantitative trait loci and a novel approach to mapping QTLs.	2000 Dec	11166067
Sildenafil and erectile dysfunction.	2000 Dec	11097980
Risperidone versus haloperidol in psychotic patients with disturbing neuroleptic-induced extrapyramidal symptoms: a double-blind, multi-center trial.	2000 Dec 15	11120421
Sub-chronic inhibition of nitric-oxide synthesis modifies haloperidol-induced catalepsy and the number of NADPH-diaphorase neurons in mice.	2000 Jan	10672628
Reduced number of striatal neurons expressing preprosomatostatin mRNA in rats with oral dyskinesias after long-term haloperidol administration.	2000 Jan 21	10670778
Prevention of cocaine-induced convulsions and lethality in mice: effectiveness of targeting different sites on the NMDA receptor complex.	2000 Jan 28	10698007
Manic episode in an ifosfamide-treated patient.	2000 Jan-Feb	10766557
The antidepressive-like effect of oxcarbazepine: possible role of dopaminergic neurotransmission.	2000 Jul	10871703
Further evidence that behavioral tests and neuropeptide mRNA and tissue level alterations can differentiate between typical and atypical antipsychotic drugs.	2000 Jul	10869885
[Neuropsychiatric symptoms in preventive antimalarial treatment with mefloquine: apropos of 2 cases].	2000 Jul-Aug	11064842
Repeated treatment with 8-OH-DPAT induces tolerance to its ability to produce the 5-HT1A behavioural syndrome, but not to its ability to attenuate haloperidol-induced catalepsy.	2000 Jun	11103884
Effect of magnesium sulfate on the haloperidol-induced QT prolongation assessed in the canine in vivo model under the monitoring of monophasic action potential.	2000 Jun	10875735
Double blind study of tiapride versus haloperidol and placebo in agitation and aggressiveness in elderly patients with cognitive impairment.	2000 Mar	10928308
Effect of dopamine agonists and antagonists on the lorazepam withdrawal syndrome in rats.	2000 Mar	10744342
Torsades de pointes secondary to intravenous haloperidol after coronary bypass grafting surgery.	2000 Mar	10730737
Effects of atypical neuroleptics on sustained attention deficits in schizophrenia: a trial of risperidone versus haloperidol.	2000 Mar	10693159
Haloperidol-induced catalepsy is absent in dopamine D(2), but maintained in dopamine D(3) receptor knock-out mice.	2000 Mar 10	10720636
Effects of blockade of metabotropic glutamate receptors in the subthalamic nucleus on haloperidol-induced Parkinsonism in rats.	2000 Mar 17	10713387
No changes in dopamine D(1) receptor mRNA expressing neurons in the dorsal striatum of rats with oral movements induced by long-term haloperidol administration.	2000 Mar 24	10719094
Propiverine-induced Parkinsonism: a case report and a pharmacokinetic/pharmacodynamic study in mice.	2000 May	10888308
Doses of olanzapine, risperidone, and haloperidol used in clinical practice: results of a prospective pharmacoepidemiologic study. EFESO Study Group. Estudio Farmacoepidemiologico en la Esquizofrenia con Olanzapina.	2000 May	10868556
The safety of olanzapine compared with other antipsychotic drugs: results of an observational prospective study in patients with schizophrenia (EFESO Study). Pharmacoepidemiologic Study of Olanzapine in Schizophrenia.	2000 May	10847307
Sex differences in catalepsy: evidence for hormone-dependent postural mechanisms in haloperidol-treated rats.	2000 May	10762690
Haloperidol-induced catalepsy is influenced by calcium channel antagonists.	2000 May-Jun	11143713
Biperiden hydrochlorate ameliorates dystonia of rats produced by microinjection of sigma ligands into the red nucleus.	2000 Nov	11164078
Enhancement of haloperidol-induced catalepsy by nicotine: an investigation of possible mechanisms.	2000 Nov	11100936
Role of prolactin in chloro-S-triazine rat mammary tumorigenesis.	2000 Nov	11071396
The serotonin 5-HT(2A) receptor subtype does not mediate apomorphine-induced aggressive behaviour in male Wistar rats.	2000 Oct	11124399
Contrasting patterns and cellular specificity of transcriptional regulation of the nuclear receptor nerve growth factor-inducible B by haloperidol and clozapine in the rat forebrain.	2000 Oct	10987852
The effects of olanzapine, risperidone, and haloperidol on plasma prolactin levels in patients with schizophrenia.	2000 Sep	11048906
Effects of antipsychotic drugs on cholecystokinin and preprotachykinin (substance P) mRNA expression in the rat hippocampal formation.	2000 Sep	10974607
Haloperidol-induced impotence improved by switching to olanzapine.	2000 Sep-Oct	11203037
FosB in rat striatum: normal regional distribution and enhanced expression after 6-month haloperidol administration.	2001 Feb	11180499
Increased dopamine d(2) receptor occupancy and elevated prolactin level associated with addition of haloperidol to clozapine.	2001 Feb	11156818
Neurotensin gene expression and behavioral responses following administration of psychostimulants and antipsychotic drugs in dopamine D(3) receptor deficient mice.	2001 Feb	11120399
The role of the D(2) dopamine receptor (D(2)R) in A(2A) adenosine receptor (A(2A)R)-mediated behavioral and cellular responses as revealed by A(2A) and D(2) receptor knockout mice.	2001 Feb 13	11172060
Double activity imaging reveals distinct cellular targets of haloperidol, clozapine and dopamine D(3) receptor selective RGH-1756.	2001 Mar	11166331

Patents

Sample Use Guides

In Vivo Use Guide

Parenteral medication, administered intramuscularly in doses of 2 to 5 mg, is utilized for prompt control of the acutely agitated schizophrenic patient with moderately severe to very severe symptoms. Depending on the response of the patient, subsequent doses may be given, administered as often as every hour, although 4 to 8 hour intervals may be satisfactory.

Route of Administration: Intramuscular

In Vitro Use Guide

10 uM Haloperidol induced a 54% decrease in the mRNA expression of ABCA1 in murineperitoneal macrophages.

Name

Type

Language

HALOPERIDOL

Official Name

English

HALOPERIDOL COMPONENT OF VESALIUM

Brand Name

English

EUKYSTOL

Common Name

English

HALOPERIDOL DECANOATE IMPURITY G [EP IMPURITY]

Common Name

English

VESALIUM COMPONENT HALOPERIDOL

Brand Name

English

HALOPERIDOL [HSDB]

Common Name

English

HALOPERIDOL [WHO-IP]

Common Name

English

SIGAPERIDOL

Common Name

English

HALDOL

Brand Name

English

KESELAN

Common Name

English

ALOPERIDIN

Common Name

English

NSC-170973

Code

English

Haloperidol [WHO-DD]

Common Name

English

HALOPERIDOL [EP MONOGRAPH]

Common Name

English

HALOPERIDOL [JAN]

Common Name

English

R-1625

Code

English

NSC-615296

Code

English

HALOPERIDOLUM [WHO-IP LATIN]

Common Name

English

SERENELFI

Common Name

English

SERENASE

Common Name

English

BIOPERIDOLO

Common Name

English

1-BUTANONE, 4-(4-(4-CHLOROPHENYL)-4-HYDROXY-1-PIPERIDINYL)-1-(4-FLUOROPHENYL)-

Systematic Name

English

HALOPERIDOL [MI]

Common Name

English

SERENACE

Common Name

English

HALOPERIDOL [USP MONOGRAPH]

Common Name

English

HALOPERIDOL DECANOATE IMPURITY, HALOPERIDOL- [USP IMPURITY]

Common Name

English

HALOPERIDOL [MART.]

Common Name

English

NEURODOL

Common Name

English

LINTON

Common Name

English

HALOPERIDOL [ORANGE BOOK]

Common Name

English

HALOPERIDOL [USP IMPURITY]

Common Name

English

HALOPERIDOL [USAN]

Common Name

English

haloperidol [INN]

Common Name

English

HALOPERIDOL [VANDF]

Common Name

English

DOZIC

Common Name

English

HALOPERIDOL [USP-RS]

Common Name

English

Classification Tree Code System Code

LIVERTOX

NBK548393