OralParenteralDosed ingredientTherapeutic flag

Haloperidol

CAS 52-86-8

Haloperidol (CAS 52-86-8) is a Phase 4 pharmaceutical compound with 48 bioactivity targets and 2,675 adverse event associations.

SOURCE NLM DailyMed
Label records
0
SOURCE EMBL-EBI ChEMBL
Bioactivity
93
SOURCE DrugCentral
Adverse signals
2,675
SOURCE IUPHAR/BPS
PubMed IDs
60
SOURCE EMBL-EBI ChEMBL B25820EEF0F0

Compound Identity

Matched identifiers and naming fields for the pharmaceutical compound record.

Primary Name
Haloperidol
CAS Number
52-86-8
UNII
J6292F8L3D
InChIKey
LNEPOXFFQSENCJ-UHFFFAOYSA-N
ChEMBL ID
CHEMBL54
Molecule Type
Small molecule
Source Match
EMBL-EBI ChEMBL (INCHIKEY)
Synonyms and normalized names
HALOPERIDOL DECANOATEhaloperidol lactateHaldol
black box warningdosed ingredientoralparenteraltherapeutic flag
SOURCE EMBL-EBI ChEMBL B25820EEF0F0

Clinical Development Phase

Highest clinical development phase rendered from the matched compound identifier rows.

Phase 4 (Approved)
Approved or marketed human pharmaceutical use is represented in the source phase field.
ChEMBL CHEMBL54 | Small molecule
SOURCE EMBL-EBI ChEMBL 80 bioactivity rows

Bioactivity & Target Interactions

Target-level activity records with assay counts, activity type, and measured value where present.

TargetActivity ValueAssaysOrganism
- Ki 404.21271789099524 nM 829 -
- IC50 4078.638089803922 nM 247 -
- AC50 16959.248639053254 nM 168 -
- Potency 14189.426470588236 nM 66 -
- GI50 34401.98072727273 nM 55 -
- Kd 16681.804422222223 nM 9 -
- EC50 10002.822857142857 nM 7 -
- MIC 57300 nM 6 -
- MIC 3.125 ug.mL-1 2 -
- EC50 0.2 mg kg-1 1 -
- EC50 0.88 umol/Kg 1 -
Calmodulin
Cytosolic other
IC50 6.3 - Homo sapiens
5-hydroxytryptamine receptor 5A
GPCR
Ki 5.648 - Homo sapiens
5-hydroxytryptamine receptor 1F
GPCR
Ki 5.301 - Homo sapiens
5-hydroxytryptamine receptor 1E
GPCR
Ki 5.301 - Homo sapiens
Beta-2 adrenergic receptor
GPCR
Ki 5.301 - Homo sapiens
Mu-type opioid receptor
GPCR
Ki 6.003 - Homo sapiens
D(1A) dopamine receptor
GPCR
Ki 7.82 - Homo sapiens
D(2) dopamine receptor
GPCR
Ki 9.15 - Homo sapiens
Alpha-2A adrenergic receptor
GPCR
Ki 5.947 - Homo sapiens
Sigma non-opioid intracellular receptor 1
Membrane receptor
EC50 8.92 - Homo sapiens
Potassium voltage-gated channel subfamily H member 2
Ion channel
IC50 7.5 - Homo sapiens
3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase
Enzyme
Ki 6.72 - Homo sapiens
Multidrug resistance protein 1
Transporter
Ki 6.7 - Homo sapiens
Sodium-dependent serotonin transporter
Transporter
Ki 5.74 - Homo sapiens
Sodium-dependent noradrenaline transporter
Transporter
Ki 5.74 - Homo sapiens
5-hydroxytryptamine receptor 1A
GPCR
Ki 5.55 - Homo sapiens
5-hydroxytryptamine receptor 2A
GPCR
Ki 7 - Homo sapiens
5-hydroxytryptamine receptor 2B
GPCR
Ki 6.1 - Homo sapiens
5-hydroxytryptamine receptor 2C
GPCR
Ki 5.33 - Homo sapiens
5-hydroxytryptamine receptor 6
GPCR
Ki 5.22 - Homo sapiens
5-hydroxytryptamine receptor 7
GPCR
Ki 6.45 - Homo sapiens
Alpha-1A adrenergic receptor
GPCR
Ki 7.9 - Homo sapiens
Alpha-2B adrenergic receptor
GPCR
Ki 6.319 - Homo sapiens
D(3) dopamine receptor
GPCR
Ki 8.52 - Homo sapiens
D(1B) dopamine receptor
GPCR
Ki 7.52 - Homo sapiens
Histamine H1 receptor
GPCR
Ki 6.36 - Homo sapiens
Histamine H2 receptor
GPCR
Ki 5.999 - Homo sapiens
Muscarinic acetylcholine receptor M1
GPCR
Ki 5.8 - Homo sapiens
Muscarinic acetylcholine receptor M3
GPCR
Ki 5 - Homo sapiens
Muscarinic acetylcholine receptor M5
GPCR
Ki 6.182 - Homo sapiens
5-hydroxytryptamine receptor 1B
GPCR
Ki 6.569 - Homo sapiens
5-hydroxytryptamine receptor 1D
GPCR
Ki 6.6 - Homo sapiens
Alpha-2C adrenergic receptor
GPCR
Ki 6.26 - Homo sapiens
Alpha-1D adrenergic receptor
GPCR
Ki 7.553 - Homo sapiens
Alpha-1B adrenergic receptor
GPCR
Ki 8.097 - Homo sapiens
Potassium channel subfamily K member 2
Ion channel
IC50 5.26 - Homo sapiens
Potassium voltage-gated channel subfamily H member 1
Ion channel
IC50 6.2 - Homo sapiens
Alpha-1B adrenergic receptor
GPCR
Ki 8.305 - Rattus norvegicus
Membrane-associated progesterone receptor component 1
Membrane receptor
Ki 7.444 - Rattus norvegicus
SOURCE DrugCentral 80 associations

Adverse Event Associations

DrugCentral / FAERS disproportionality signal rows matched to this compound.

Reaction PTDrug AE LLRMedDRA
Neuroleptic malignant syndrome 1425 4095.68 10029282
Extrapyramidal disorder 1264 3616.483 10015832
Intentional self-injury 760 1522.98 10022524
Akathisia 560 1375.96 10001540
Dystonia 607 1347.992 10013983
Catatonia 358 937.235 10007776
Drug interaction 1680 930.408 10013710
Muscle rigidity 452 924.612 10028330
Agitation 800 841.141 10001497
Psychotic disorder 540 783.3 10061920
Parkinsonism 375 754.958 10034010
Sedation 569 738.531 10039897
Salivary hypersecretion 345 714.265 10039424
Delirium 655 689.458 10012218
Sopor 423 673.428 10058709
Electrocardiogram QT prolonged 658 656.819 10014387
Hyperprolactinaemia 228 615.854 10020737
Hallucination, auditory 355 612.717 10019070
Aggression 506 608.515 10001488
Tardive dyskinesia 299 606.19 10043118
Suicide attempt 613 587.261 10042464
Delusion 337 564.094 10012239
Arthralgia 93 496.722 10003239
Blood creatine phosphokinase increased 482 487.383 10005470
Somnolence 988 483.564 10041349
Intentional overdose 568 422.883 10022523
Pain 238 411.833 10033371
Schizophrenia 245 401.897 10039626
Fatigue 445 387.828 10016256
Weight increased 1038 381.21 10047899
Dyskinesia 362 370.388 10013916
Tachycardia 704 364.089 10043071
Rhabdomyolysis 505 363.604 10039020
Tremor 706 346.512 10044565
Restlessness 343 340.097 10038743
Psychomotor hyperactivity 224 327.084 10037211
Rash 210 322.578 10037844
Hypothermia 238 320.978 10021113
Headache 235 320.248 10019211
Joint swelling 25 320.147 10023232
Antipsychotic drug level below therapeutic 119 317.398 10060145
Coma 479 316.756 10010071
Toxicity to various agents 1107 307.316 10070863
Infusion related reaction 13 286.696 10051792
Rheumatoid arthritis 7 284.425 10039073
Torsade de pointes 205 281.537 10044066
Abnormal behaviour 282 269.177 10061422
Hypertonia 147 264.654 10020852
Overdose 647 258.448 10033295
Disinhibition 114 257.662 10013142

Association rows are source-linked signal records, not incidence rates or clinical causality claims.

SOURCE IUPHAR/BPS 19 interactions

IUPHAR Ligand-Target Data

Curated ligand-target interaction rows with action, affinity, and literature identifiers.

TargetAction AffinityPubMed
5-HT 2A receptor
HTR2A
Antagonist 6.699999809265137 pKi 8935801|9732398|12629531|15102927|18308814
D 2 receptor
DRD2
Antagonist 7.400000095367432 pKi 8301582|7907989|1354163|7664822|7862709
D 3 receptor
DRD3
Antagonist 7.5 pKi 8301582|1354163|7862709|18308814
D 4 receptor
DRD4
Antagonist 8.699999809265137 pKi 8102973|7862709|18308814
5-HT 1A receptor
HTR1A
Antagonist 5.7 pKi 9760039|9067310|8935801|9732398
5-HT 1D receptor
HTR1D
Antagonist 6.6 pKi 8935801
5-HT 2A receptor
Htr2a
Antagonist 7.4 pKi 9655845
5-HT 2B receptor
HTR2B
Antagonist 5.8 pKi 9459568
5-HT 7 receptor
Htr7
Antagonist 6.3 pKi 8997630|7908055|8397408
5-HT 7 receptor
HTR7
Antagonist 6.3 pKi 9298538
5-HT 7 receptor
Htr7
Antagonist 6.3 pKi 8394987
D 1 receptor
DRD1
Antagonist 7.599999904632568 pKi 1826762|18308814
D 2 receptor
Drd2
Antagonist 8.300000190734863 pKi 1975644
D 3 receptor
Drd3
Antagonist 7.0 pKi 1975644
D 5 receptor
DRD5
Antagonist 6.3 pKi 1826762
H 1 receptor
HRH1
Antagonist 5.7 pKi 8935801|12629531
K ir 3.2
Kcnj6
Antagonist 4.1 pEC50 10780978
K v 10.1
KCNH1
Channel blocker 6.2 pIC50 12522086
TAS2R10
TAS2R10
Agonist - 20022913
SOURCE PharmGKB 60 phenotype rows

Pharmacogenomics

Drug-gene phenotype annotations and evidence levels from PharmGKB-mapped rows.

CYP2D6 (PA128) CYP2D6*1, CYP2D6*1xN
CYP2D6 *1/*1xN (assigned as ultrarapid metabolizer phenotype phenotype) is not associated with differences in treatment response or scores on the various subscales of the PANSS when treated with haloperidol or risperidone in people with Schizophrenia as compared to CYP2D6 normal metabolizer.
Evidence: -; PMID 22775532
CYP2D6 (PA128) CYP2D6*3, CYP2D6*4
CYP2D6 *4/*4 (assigned as poor metabolizer phenotype) is not associated with differences in treatment response or scores on the various subscales of the PANSS when treated with haloperidol or risperidone in people with Schizophrenia as compared to CYP2D6 normal metabolizer.
Evidence: -; PMID 22775532
HTR2C (PA194) rs3813929
Allele C is associated with increased risk of Weight gain when treated with amisulpride, clozapine, haloperidol, iloperidone, olanzapine, quetiapine, risperidone and ziprasidone as compared to allele T.
Evidence: -; PMID 21121776
HTR2C (PA194) rs3813929
Allele T is not associated with increased likelihood of Weight gain when treated with clozapine, haloperidol, olanzapine or risperidone in people with Schizophrenia as compared to allele C.
Evidence: -; PMID 17702092
HTR2C (PA194) rs518147
Allele G is associated with increased likelihood of Weight gain when treated with clozapine, haloperidol, olanzapine and risperidone in people with Schizophrenia as compared to allele C.
Evidence: -; PMID 21121776
HTR2C (PA194) rs6318
Allele C is not associated with increased likelihood of Weight gain when treated with clozapine, haloperidol, olanzapine or risperidone in people with Schizophrenia as compared to allele G.
Evidence: -; PMID 17702092
- rs7912580
Genotype GG is associated with increased response to haloperidol in people with Schizophrenia as compared to genotype AG.
Evidence: -; PMID 24751813
DTNBP1 (PA27512) rs909706
Genotype CT is associated with increased response to haloperidol in people with Schizophrenia as compared to genotype CC.
Evidence: -; PMID 19369910
CYP2D6 (PA128) CYP2D6*1, CYP2D6*10
CYP2D6 *10 is not associated with decreased metabolism of haloperidol as compared to CYP2D6 *1.
Evidence: -; PMID 12919180
EIF2AK4 (PA134947616) rs2412459
Genotype TT is associated with increased response to haloperidol in people with Schizophrenia as compared to genotype CT.
Evidence: -; PMID 24751813
SLC6A5 (PA35911) rs2298826
Genotype AA is associated with motor side effects when treated with haloperidol in people with Schizophrenia as compared to genotypes AG + GG.
Evidence: -; PMID 20859245
CYP2D6 (PA128) CYP2D6*1, CYP2D6*5
CYP2D6 *5 is associated with decreased metabolism of haloperidol in people with Schizophrenia as compared to CYP2D6 *1.
Evidence: -; PMID 9352580
ANKK1 (PA134872551) rs2587550
Allele G is associated with increased response to haloperidol in people with Schizophrenia as compared to allele A.
Evidence: -; PMID 22893251
CYP2D6 (PA128) CYP2D6*1, CYP2D6*10
CYP2D6 *10 is associated with decreased metabolism of haloperidol in people with Schizophrenia as compared to CYP2D6 *1.
Evidence: -; PMID 9352580
SLC6A4 (PA312) SLC6A4 HTTLPR long form (L allele), SLC6A4 HTTLPR short form (S allele)
SLC6A4 HTTLPR long form (L allele)/HTTLPR short form (S allele) is associated with increased response to antipsychotics, haloperidol, olanzapine or risperidone in people with Schizophrenia as compared to SLC6A4 HTTLPR long form (L allele)/HTTLPR long form (L allele) + HTTLPR short form (S allele)/HTTLPR short form (S allele).
Evidence: -; PMID 20031235
COMT (PA117) rs4680
Genotype AG is associated with increased likelihood of extrapyramidal symptoms when treated with haloperidol in men with Schizophrenia as compared to genotypes AA + GG.
Evidence: -; PMID 23963056
DRD2 (PA27478) rs1800497
Genotype AG is not associated with likelihood of Drug Toxicity when treated with haloperidol in men with Schizophrenia as compared to genotypes AA + GG.
Evidence: -; PMID 23963056
CYP2D6 (PA128) CYP2D6*1, CYP2D6*2
CYP2D6 *2/*2 is associated with increased concentrations of haloperidol in people with Schizophrenia as compared to CYP2D6 *1/*1 + *1/*2.
Evidence: -; PMID 12960748
CYP2D6 (PA128) CYP2D6*1, CYP2D6*10
CYP2D6 *10/*10 is associated with increased concentrations of haloperidol in people with Schizophrenia as compared to CYP2D6 *1/*1 + *1/*10.
Evidence: -; PMID 12960748
CYP2D6 (PA128) CYP2D6 poor metabolizer
CYP2D6 poor metabolizer is not associated with concentrations of haloperidol, paliperidone and zuclopenthixol in people with Bipolar Disorder, schizoaffective disorder or Schizophrenia as compared to CYP2D6 intermediate metabolizer and normal metabolizer.
Evidence: -; PMID 26514968
EPM2A (PA27832) rs1415744
Allele C is associated with increased response to chlorpromazine, clozapine, haloperidol, olanzapine, quetiapine, risperidone or trifluoperazine in people with Schizophrenia as compared to allele T.
Evidence: -; PMID 27092952
ABCB5 (PA24387) rs17143212
Genotype CT is associated with increased Drug Toxicity when treated with haloperidol in people with Psychotic Disorders as compared to genotype CC.
Evidence: -; PMID 25647612
CYP2D6 (PA128) rs3892097
Genotype CC is associated with decreased response to haloperidol in men with Alcohol-Related Disorders, Alcoholic psychosis NOS and Alcoholism as compared to genotype CT.
Evidence: -; PMID 27695358
CYP3A43 (PA427) rs680055
Genotype CG is associated with increased response to antipsychotics, aripiprazole, clozapine, haloperidol, olanzapine, quetiapine or risperidone in people with schizoaffective disorder or Schizophrenia as compared to genotype CC.
Evidence: -; PMID 25150845
CYP2D6 (PA128) CYP2D6 haplotype
CYP2D6 poor metabolizer genotype is associated with increased dose-adjusted trough concentrations of haloperidol in people with Psychotic Disorders as compared to CYP2D6 normal metabolizer genotype.
Evidence: -; PMID 25868121
CYP3A4 (PA130) CYP3A4*1, CYP3A4*22
CYP3A4 *22 is not associated with dose-adjusted trough concentrations of antipsychotics, aripiprazole, haloperidol, pimozide or risperidone in people with Psychotic Disorders as compared to CYP3A4 *1.
Evidence: -; PMID 25868121
CYP3A4 (PA130) rs2242480
Genotype CT is associated with increased concentrations of haloperidol in people with Psychotic Disorders as compared to genotype CC.
Evidence: -; PMID 23077486
- rs12970134
Allele A is not associated with increased risk of Weight gain when exposed to amisulpride, aripiprazole, clozapine, haloperidol, quetiapine, risperidone or ziprasidone in people with schizoaffective disorder and Schizophrenia as compared to allele G.
Evidence: -; PMID 22566560
CYP2D6 (PA128) CYP2D6*6
CYP2D6 *6/*6 is associated with adverse events and extrapyramidal symptoms when treated with ciprofloxacin and haloperidol.
Evidence: -; PMID 27469576
CYP3A4 (PA130) rs2242480
Genotype CT is associated with increased severity of adverse events when treated with haloperidol in people with Psychotic Disorders as compared to genotype CC.
Evidence: -; PMID 23077486
SOURCE NLM RxNorm 12 name rows

Drug Names / RxNorm

Normalized drug-name vocabulary rows, RxCUIs, and source abbreviations.

NameRxCUI TypeSource
Haloperidol 5093 SU MTHSPL
HALOPERIDOL 5093 SU MTHSPL
haloperidol 5093 SU MTHSPL
HALOPERIDOL DECANOATE 26420 SU MTHSPL
haloperidol decanoate 26420 SU MTHSPL
haloperidol lactate 217483 SU MTHSPL
HALOPERIDOL LACTATE 217483 SU MTHSPL
Haloperidol lactate 217483 SU MTHSPL
haloperidol 5093 IN RXNORM
haloperidol decanoate 26420 PIN RXNORM
Haldol 151839 BN RXNORM
haloperidol lactate 217483 PIN RXNORM
SOURCE SIDER 80 side-effect rows

Side Effects

SIDER side-effect terms mapped to the drug or same-CAS compound identity.

Side EffectDrug Name MedDRA TypeConcept ID
Abnormal behaviour haloperidol PT C0233514
Acute hepatic failure haloperidol LLT C0162557
Acute hepatic failure haloperidol PT C0162557
Agitation haloperidol LLT C0085631
Agitation haloperidol PT C0085631
Agitation haloperidol PT C0085631
Agranulocytosis haloperidol LLT C0001824
Agranulocytosis haloperidol PT C0001824
Akathisia haloperidol LLT C0392156
Akathisia haloperidol PT C0392156
Akinesia haloperidol LLT C0085623
Akinesia haloperidol PT C0085623
Alopecia haloperidol LLT C0002170
Alopecia haloperidol PT C0002170
Amenorrhoea haloperidol LLT C0002453
Amenorrhoea haloperidol PT C0002453
Anaemia haloperidol LLT C0002871
Anaemia haloperidol PT C0002871
Anaphylactic shock haloperidol LLT C0002792
Anaphylactic shock haloperidol PT C0002792
Angiopathy haloperidol LLT C0042373
Angiopathy haloperidol PT C0042373
Anorexia haloperidol LLT C0003123
Anxiety haloperidol LLT C0003467
Anxiety haloperidol PT C0003467
Argininosuccinate synthetase deficiency haloperidol LLT C0175683
Argininosuccinate synthetase deficiency haloperidol PT C0175683
Blood and lymphatic system disorders haloperidol - C0851353
Body temperature decreased haloperidol LLT C0020672
Body temperature decreased haloperidol PT C0020672
Body temperature increased haloperidol LLT C0015967
Body temperature increased haloperidol PT C0015967
Bradykinesia haloperidol LLT C0233565
Bradykinesia haloperidol PT C0233565
Breast discomfort haloperidol LLT C0877338
Breast discomfort haloperidol PT C0877338
Breast disorder haloperidol LLT C0006145
Breast disorder haloperidol PT C0006145
Breast engorgement haloperidol LLT C0085688
Breast engorgement haloperidol PT C0085688
Breast pain haloperidol LLT C0024902
Breast pain haloperidol PT C0024902
Bronchospasm haloperidol LLT C0006266
Bronchospasm haloperidol PT C0006266
Cardiac arrest haloperidol LLT C0018790
Cardiac arrest haloperidol PT C0018790
Cardiac disorder haloperidol LLT C0018799
Cardiac disorder haloperidol PT C0018799
Cataract haloperidol LLT C0086543
Cataract haloperidol PT C0086543
Catatonia haloperidol LLT C0007398
Catatonia haloperidol PT C0007398
Cholestasis haloperidol LLT C0008370
Cholestasis haloperidol PT C0008370
Cogwheel rigidity haloperidol LLT C0151564
Cogwheel rigidity haloperidol PT C0151564
Confusional state haloperidol LLT C0009676
Confusional state haloperidol PT C0009676
Connective tissue disorder haloperidol LLT C0009782
Connective tissue disorder haloperidol PT C0009782
Constipation haloperidol LLT C0009806
Constipation haloperidol PT C0009806
Convulsion haloperidol LLT C0036572
Convulsion haloperidol PT C0036572
Decreased appetite haloperidol PT C0232462
Depression haloperidol LLT C0011570
Depression haloperidol PT C0011570
Dermatitis haloperidol PT C0011603
Dermatitis exfoliative haloperidol LLT C0011606
Dermatitis exfoliative haloperidol PT C0011606
Diarrhoea haloperidol LLT C0011991
Diarrhoea haloperidol PT C0011991
Disturbance in sexual arousal haloperidol PT C0855242
Disturbance in sexual arousal haloperidol PT C0855242
Dizziness haloperidol LLT C0012833
Dizziness haloperidol PT C0012833
Drowsiness haloperidol LLT C0013144
Drug withdrawal syndrome neonatal haloperidol LLT C0027609
Drug withdrawal syndrome neonatal haloperidol PT C0027609
Dry mouth haloperidol LLT C0043352
SOURCE Rendered pharma page rows FAQPage JSON-LD

Frequently Asked Questions

Short answers generated only from the same visible source-linked rows on this page.

What is Haloperidol used for in pharmaceutical contexts?

Haloperidol (CAS 52-86-8) is rendered as a pharmaceutical compound from the matched source rows; no DailyMed product-name rows are present in this page query.

What are the known adverse events for Haloperidol?

Haloperidol has 2,675 DrugCentral/FAERS adverse event associations. Rendered reaction terms include Neuroleptic malignant syndrome, Extrapyramidal disorder, Intentional self-injury, Akathisia, Dystonia. Signal rows are source-linked records and should not be read as incidence rates or causality conclusions.

Is Haloperidol also used in cosmetics?

No same-CAS cosmetics profile is rendered from the ingredients-table cross-reference for Haloperidol.

What clinical phase is Haloperidol in?

Haloperidol is rendered with ChEMBL max phase 4 (approved).

What bioactivity targets are documented for Haloperidol?

Haloperidol has 93 bioactivity rows in this page query. Rendered target entries include Calmodulin, 5-hydroxytryptamine receptor 5A, 5-hydroxytryptamine receptor 1F, 5-hydroxytryptamine receptor 1E, Beta-2 adrenergic receptor.