Drug Information

Drug (ID: DG00162) and It's Reported Resistant Information

Name	Haloperidol
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] Click to Show/Hide
Indication	In total 1 Indication(s) Schizophrenia [ICD-11: 6A20] Approved [1]
Structure
Target	Dopamine D2 receptor (D2R)	DRD2_HUMAN	[1]
Click to Show/Hide the Molecular Information and External Link(s) of This Drug
Formula	C21H23ClFNO2
IsoSMILES	C1CN(CCC1(C2=CC=C(C=C2)Cl)O)CCCC(=O)C3=CC=C(C=C3)F
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
InChIKey	LNEPOXFFQSENCJ-UHFFFAOYSA-N
PubChem CID	3559
ChEBI ID	CHEBI:5613
TTD Drug ID	D0D1AL
VARIDT ID	DR00426
DrugBank ID	DB00502

Type(s) of Resistant Mechanism of This Drug

IDUE: Irregularity in Drug Uptake and Drug Efflux

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-06: Mental/behavioural/neurodevelopmental disorders

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Psychosis [ICD-11: 6D8Z]

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Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
Irregularity in Drug Uptake and Drug Efflux (IDUE)			Click to Show/Hide
Key Molecule: Multidrug resistance protein 1 (ABCB1)				[1]
Molecule Alteration	Expression		Down-regulation	Molecule Info
Sensitive Disease	Psychosis [ICD-11: 6D8Z.0]			Disease Info
Experimental Note	Revealed Based on the Cell Line Data
In Vitro Model	L-MDR1 cells(Sus scrofa (Pig))	Kidney	Homo sapiens (Human)	CVCL_0391
	LLC-Pk1 cells(Sus scrofa (Pig))	Kidney	Homo sapiens (Human)	CVCL_0391
Experiment for Drug Resistance	Flow cytometric assay
Mechanism Description	The multidrug resistance transporter, P-glycoprotein (P-gp), is involved in efflux transport of several antipsychotics in the blood-brain barrier (BBB). All the antipsychotics showed various degrees of inhibitory effects on P-gp activity at concentrations ranging from 1 to 100 uM. However, risperidone and olanzapine are the most likely agents that may inhibit P-gp activity.

References

Ref 1	Evaluation of antipsychotic drugs as inhibitors of multidrug resistance transporter P-glycoprotein. Psychopharmacology (Berl). 2006 Sep;187(4):415-23. doi: 10.1007/s00213-006-0437-9. Epub 2006 Jun 30.