Details of the Drug-Related molecule(s) Expression Atlas

General Information of Drug (ID: DM96SE0)

Drug Name

Haloperidol Drug Info

Synonyms

Aldo; Aloperidin; Aloperidol; Aloperidolo; Aloperidon; Bioperidolo; Brotopon; Dozic; Dozix; Eukystol; Fortunan; Galoperidol; Haldol; Halidol; Halojust; Halol; Halopal; Haloperido; Haloperidolum; Halopidol; Halopoidol; Halosten; Keselan; Linton; Mixidol; Pekuces; Peluces; Peridol; Pernox; Serenace; Serenase; Serenelfi; Sernas; Sernel; Sigaperidol; Ulcolind; Uliolind; Vesalium; Aloperidolo [DCIT]; Aloperidolo [Italian]; Einalon S; Haldol La; Haldol Solutab; Lealgin compositum; Pms Haloperidol; H 1512; R 1625; Aloperidin (TN); Apo-Haloperidol; Bioperidolo (TN); Brotopon (TN); Dozic (TN); Duraperidol (TN); Einalon S (TN); Eukystol (TN); Haldol (TN); Haloperidolum [INN-Latin]; Halosten (TN); Keselan (TN); Linton (TN);Novo-Peridol; Peluces (TN); R-1625; Serenace (TN); Serenase (TN); Sigaperidol (TN); Haloperidol (JP15/USP); McN-JR-1625; Haloperidol (JP15/USP/INN); Haloperidol [USAN:INN:BAN:JAN]

Indication

Disease Entry	ICD 11	Status	REF
Delirium		Approved	[1]
Nausea	MD90	Approved	[1]
Psychotic disorder	6A20-6A25	Approved	[1]
Schizophrenia	6A20	Approved	[2]
Vomiting	MD90	Approved	[1]
Coronavirus Disease 2019 (COVID-19)	1D6Y	Investigative	[3]
Tourette syndrome	8A05.00	Investigative	[1]

Therapeutic Class

Antipsychotic Agents

Cross-matching ID

PubChem CID: 3559
ChEBI ID: CHEBI:5613
CAS Number: CAS 52-86-8
TTD Drug ID: DM96SE0
VARIDT Drug ID: DR00426
INTEDE Drug ID: DR0801
ACDINA Drug ID: D00310

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Dopamine D2 receptor (D2R)	TTEX248	DRD2_HUMAN	Antagonist	[4]
HUMAN opioid receptor sigma 1 (OPRS1)	TTTPE1L	SGMR1_HUMAN	Modulator	[5]
HUMAN sigma intracellular receptor 2 (TMEM97)	TTIS0R2	SGMR2_HUMAN	Modulator	[5]

------------------------------------------------------------------------------------

Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	Highest Status	REF
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Approved	[6]

------------------------------------------------------------------------------------

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	Highest Status	REF
Cytochrome P450 3A4 (CYP3A4)	DE4LYSA	CP3A4_HUMAN	Approved	[7]
Cytochrome P450 2D6 (CYP2D6)	DECB0K3	CP2D6_HUMAN	Approved	[8]
Cytochrome P450 2C9 (CYP2C9)	DE5IED8	CP2C9_HUMAN	Approved	[9]
Cytochrome P450 1A1 (CYP1A1)	DE6OQ3W	CP1A1_HUMAN	Approved	[9]
Mephenytoin 4-hydroxylase (CYP2C19)	DEGTFWK	CP2CJ_HUMAN	Approved	[9]
Cytochrome P450 1A2 (CYP1A2)	DEJGDUW	CP1A2_HUMAN	Approved	[9]
Cytochrome P450 3A5 (CYP3A5)	DEIBDNY	CP3A5_HUMAN	Approved	[7]
Cytochrome P450 3A7 (CYP3A7)	DERD86B	CP3A7_HUMAN	Approved	[10]
UDP-glucuronosyltransferase 1A9 (UGT1A9)	DE85D2P	UD19_HUMAN	Approved	[11]

------------------------------------------------------------------------------------

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule	Molecule Type	Gene Name	Liver	Colon	Kidney	Small Intestine
Dopamine D2 receptor (D2R)	DTT	DRD2	5.345	5.634	5.789	5.901
P-glycoprotein 1 (ABCB1)	DTP	P-GP	7.009	6.988	7.442	8.135
Cytochrome P450 1A2 (CYP1A2)	DME	CYP1A2	10.036	5.779	6.508	6.481
Cytochrome P450 3A5 (CYP3A5)	DME	CYP3A5	10.08	7.207	5.403	9.211
Mephenytoin 4-hydroxylase (CYP2C19)	DME	CYP2C19	7.867	5.142	5.52	7.08
Cytochrome P450 2D6 (CYP2D6)	DME	CYP2D6	3.307	5.005	3.921	5.327
Cytochrome P450 1A1 (CYP1A1)	DME	CYP1A1	5.952	6.384	4.897	6.293
Cytochrome P450 2C9 (CYP2C9)	DME	CYP2C9	11.76	5.931	6.164	9.423
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	11.692	6.58	4.984	9.089

Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

ICD Disease Classification

06 Mental, behavioural or neurodevelopmental disorder

Disease Class

ICD-11: 6A20 Schizophrenia

The Studied Tissue

Pre-frontal cortex

The Studied Disease

Schizophrenia [ICD-11:6A20]

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Dopamine D2 receptor (D2R)	DTT	DRD2	9.39E-01	-0.01	-0.05
Dopamine D2 receptor (D2R)	DTT	DRD2	9.91E-01	-0.02	-0.28
P-glycoprotein 1 (ABCB1)	DTP	P-GP	1.19E-01	-1.32E-01	-2.77E-01
P-glycoprotein 1 (ABCB1)	DTP	P-GP	1.65E-01	-1.47E-01	-4.48E-01
Cytochrome P450 1A2 (CYP1A2)	DME	CYP1A2	6.73E-02	6.49E-02	3.07E-01
Cytochrome P450 1A2 (CYP1A2)	DME	CYP1A2	6.45E-01	2.07E-02	1.74E-01
Cytochrome P450 3A5 (CYP3A5)	DME	CYP3A5	1.17E-01	-3.87E-02	-2.23E-01
Cytochrome P450 3A5 (CYP3A5)	DME	CYP3A5	9.74E-01	7.48E-03	1.37E-01
Mephenytoin 4-hydroxylase (CYP2C19)	DME	CYP2C19	7.39E-01	1.54E-02	4.74E-02
Mephenytoin 4-hydroxylase (CYP2C19)	DME	CYP2C19	4.64E-02	-8.21E-02	-7.11E-01
Cytochrome P450 2D6 (CYP2D6)	DME	CYP2D6	2.59E-01	6.29E-02	3.14E-01
Cytochrome P450 2D6 (CYP2D6)	DME	CYP2D6	4.84E-01	-8.38E-02	-8.46E-01
Cytochrome P450 1A1 (CYP1A1)	DME	CYP1A1	2.32E-01	-3.66E-02	-1.30E-01
Cytochrome P450 1A1 (CYP1A1)	DME	CYP1A1	6.55E-01	1.27E-02	8.44E-02
Cytochrome P450 2C9 (CYP2C9)	DME	CYP2C9	8.99E-01	-6.93E-03	-1.36E-02
Cytochrome P450 2C9 (CYP2C9)	DME	CYP2C9	9.21E-01	7.31E-03	6.10E-02
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	4.66E-01	4.25E-02	1.20E-01
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	4.75E-01	5.15E-02	3.64E-01

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	Haloperidol FDA Label
2	URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 86).
3	Sigma-1Rs are upregulated via PERK/eIF2/ATF4 pathway and execute protective function in ER stress. Biochem Biophys Res Commun. 2011 Nov 25;415(3):519-25.
4	Dopaminergic synapses in the matrix of the ventrolateral striatum after chronic haloperidol treatment. Synapse. 2002 Aug;45(2):78-85.
5	A SARS-CoV-2 protein interaction map reveals targets for drug repurposing
6	Identification of P-glycoprotein substrates and inhibitors among psychoactive compounds--implications for pharmacokinetics of selected substrates. J Pharm Pharmacol. 2004 Aug;56(8):967-75.
7	Assessment of the contributions of CYP3A4 and CYP3A5 in the metabolism of the antipsychotic agent haloperidol to its potentially neurotoxic pyridinium metabolite and effect of antidepressants on the bioactivation pathway. Drug Metab Dispos. 2003 Mar;31(3):243-9.
8	Use of antidepressant drugs in schizophrenic patients with depression. Encephale. 2006 Mar-Apr;32(2 Pt 1):263-9.
9	In vitro characterization of the metabolism of haloperidol using recombinant cytochrome p450 enzymes and human liver microsomes. Drug Metab Dispos. 2001 Dec;29(12):1638-43.
10	Drug Interactions Flockhart Table
11	Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.