DGIdb - THIORIDAZINE Drug Record

THIORIDAZINE chembl:CHEMBL479

Alternate Names:

MELLERIL
MELLARIL
RIDERIL
TP-21
MELLARIL-S
THIORIDAZINE
THIORIDAZIN
MEL269
TIORIDAZINA
THIORIDAZINUM
3-METHYLMERCAPTO-N-(2'-(N-METHYL-2-PIPERIDYL)ETHYL)PHENOTHIAZINE
MELLARIL®
10-[2-(1-METHYL-2-PIPERIDYL)ETHYL]-2-METHYLSULFANYL-PHENOTHIAZINE
2-METHYLMERCAPTO-10-(2-(N-METHYL-2-PIPERIDYL)ETHYL)PHENOTHIAZINE
chemidplus:50-52-2
chembl:CHEMBL479
drugbank:00679
rxcui:10502
pubchem.compound:5452

Drug Info:

Drug Class	antipsychotic agents
Year of Approval	1962
FDA Approval	1962
Drug Class	small molecule
Drug Indications	Antipsychotic Agents
Drug Categories	psycholeptics
Drug Groups	withdrawn
Drug Categories	adrenergic alpha-1 receptor antagonists
Drug Categories	adrenergic alpha-antagonists
Drug Categories	adrenergic antagonists
Drug Categories	agents that produce hypertension
Drug Categories	antidepressive agents
Drug Categories	cytochrome p-450 cyp2e1 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 enzyme inhibitors
Drug Categories	cytochrome p-450 substrates
Drug Categories	dopamine d2 receptor antagonists
Drug Categories	drugs causing inadvertant photosensitivity
Drug Categories	heterocyclic compounds, fused-ring
Drug Categories	neurotoxic agents
Drug Categories	photosensitizing agents
Drug Categories	qtc prolonging agents
Drug Categories	serotonergic drugs shown to increase risk of serotonin syndrome
Drug Categories	serotonin 5-ht2 receptor antagonists
Drug Categories	serotonin agents
Drug Categories	serotonin receptor antagonists

(6 More Sources)

Publications:

Cahir et al., 2005, Antipsychotics lack alpha 1A/B adrenoceptor subtype selectivity in the rat., Eur Neuropsychopharmacol
Tay JK et al., 2007, Functional polymorphisms of the cytochrome P450 1A2 (CYP1A2) gene and prolonged QTc interval in schizophrenia., Prog Neuropsychopharmacol Biol Psychiatry
Lee CA et al., 2010, Identification of novel substrates for human cytochrome P450 2J2., Drug Metab Dispos
Dorado P et al., 2009, Relevance of CYP2D6 -1584C>G polymorphism for thioridazine:mesoridazine plasma concentration ratio in psychiatric patients., Pharmacogenomics
von Bahr C et al., 1991, Plasma levels of thioridazine and metabolites are influenced by the debrisoquin hydroxylation phenotype., Clin Pharmacol Ther
Hammock et al., 1995, The effect of clozapine on self-injurious behavior., J Autism Dev Disord
Katchman AN et al., 2006, Comparative evaluation of HERG currents and QT intervals following challenge with suspected torsadogenic and nontorsadogenic drugs., J Pharmacol Exp Ther
Milnes et al., 2006, hERG K+ channel blockade by the antipsychotic drug thioridazine: An obligatory role for the S6 helix residue F656., Biochem. Biophys. Res. Commun.
Costall et al., 1995, Behavioural interactions between 5-hydroxytryptophan, neuroleptic agents and 5-HT receptor antagonists in modifying rodent responding to aversive situations., Br. J. Pharmacol.
Morisset et al., 1999, Atypical neuroleptics enhance histamine turnover in brain via 5-Hydroxytryptamine2A receptor blockade., J. Pharmacol. Exp. Ther.
Canton et al., 1994, Competitive antagonism of serotonin (5-HT)2C and 5-HT2A receptor-mediated phosphoinositide (PI) turnover by clozapine in the rat: a comparison to other antipsychotics., Neurosci. Lett.
Andree et al., 1986, Differential effect of subchronic treatment with various neuroleptic agents on serotonin2 receptors in rat cerebral cortex., J. Neurochem.
Burki, 1986, Binding of psychoactive drugs to rat brain amine receptors, measured ex vivo, and their effects on the metabolism of biogenic amines., Naunyn Schmiedebergs Arch. Pharmacol.
Sleight et al., 1993, Binding of antipsychotic drugs at alpha 1A- and alpha 1B-adrenoceptors: risperidone is selective for the alpha 1B-adrenoceptors., Eur. J. Pharmacol.
Assié et al., 1993, Biphasic displacement of [3H]YM-09151-2 binding in the rat brain by thioridazine, risperidone and clozapine, but not by other antipsychotics., Eur. J. Pharmacol.
Carey et al., 1997, Discriminative-stimulus effects of clozapine in squirrel monkeys: comparison with conventional and novel antipsychotic drugs., Psychopharmacology (Berl.)
Seeman, 1990, Atypical neuroleptics: role of multiple receptors, endogenous dopamine, and receptor linkage., Acta Psychiatr Scand Suppl
Barth et al., 2006, Comparison of rat dopamine D2 receptor occupancy for a series of antipsychotic drugs measured using radiolabeled or nonlabeled raclopride tracer., Life Sci.
Dimpfel et al., 1992, Different neuroleptics show common dose and time dependent effects in quantitative field potential analysis in freely moving rats., Psychopharmacology (Berl.)

THIORIDAZINE CYP2J2

Interaction Score: 0.54

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19923256

Sources:
PharmGKB
THIORIDAZINE HTR2A

Interaction Score: 0.14

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
8680734 9918563 7898773 2866233 2423886

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology ChemblInteractions
THIORIDAZINE DRD2

Interaction Score: 0.13

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Mechanism of Interaction D2-like dopamine receptor antagonist

PMIDs:
7689973 9292626 1978482 16434058 1352051

Sources:
TEND TdgClinicalTrial TTD DrugBank ChemblInteractions
THIORIDAZINE DRD1

Interaction Score: 0.09

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Endogenous Drug? False

PMIDs:
8720030

Sources:
TEND DTC TdgClinicalTrial DrugBank GuideToPharmacology
THIORIDAZINE ADRA1A

Interaction Score: 0.08

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
7691623 15695070

Sources:
TEND TdgClinicalTrial DrugBank
THIORIDAZINE DRD5

Interaction Score: 0.07

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
THIORIDAZINE HTR6

Interaction Score: 0.05

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Inverse agonist

PMIDs:
None found

Sources:
GuideToPharmacology
THIORIDAZINE ADRA1B

Interaction Score: 0.05

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
15695070

Sources:
DrugBank
THIORIDAZINE HTR2C

Interaction Score: 0.04

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
None found

Sources:
GuideToPharmacology ChemblInteractions
THIORIDAZINE HTR7

Interaction Score: 0.04

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Inverse agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
THIORIDAZINE DRD4

Interaction Score: 0.04

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction D2-like dopamine receptor antagonist

PMIDs:
None found

Sources:
ChemblInteractions
THIORIDAZINE KCNH2

Interaction Score: 0.03

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
16278312 17056009

Sources:
PharmGKB DrugBank
THIORIDAZINE DRD3

Interaction Score: 0.03

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction D2-like dopamine receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
THIORIDAZINE PPARD

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
THIORIDAZINE CYP2D6

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19604081 2007317

Sources:
FDA PharmGKB
THIORIDAZINE HTR1A

Interaction Score: 0.02

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
GuideToPharmacology
THIORIDAZINE HRH1

Interaction Score: 0.01

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
THIORIDAZINE CBX1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
THIORIDAZINE ATXN2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
THIORIDAZINE CYP1A2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17611010

Sources:
PharmGKB
THIORIDAZINE EHMT2

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

DrugBank: DB00679

Version: 5.1.7

Alternate Names:

THIORIDAZINE DrugBank Drug Name

50-52-2 CAS Number

Aldazine Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups withdrawn

Publications:

Milnes et al., 2006, hERG K+ channel blockade by the antipsychotic drug thioridazine: An obligatory role for the S6 helix residue F656., Biochem. Biophys. Res. Commun.

Assié et al., 1993, Biphasic displacement of [3H]YM-09151-2 binding in the rat brain by thioridazine, risperidone and clozapine, but not by other antipsychotics., Eur. J. Pharmacol.

Carey et al., 1997, Discriminative-stimulus effects of clozapine in squirrel monkeys: comparison with conventional and novel antipsychotic drugs., Psychopharmacology (Berl.)

TEND: THIORIDAZINE
- Version: 01-August-2011
Alternate Names:

THIORIDAZINE Primary Drug Name

Drug Info:

Year of Approval 1962

Drug Class antipsychotic agents

Publications:
TdgClinicalTrial: THIORIDAZINE
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications Antipsychotic Agents

Drug Class small molecule

FDA Approval 1962

Publications:

PharmGKB: thioridazine

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Tay JK et al., 2007, Functional polymorphisms of the cytochrome P450 1A2 (CYP1A2) gene and prolonged QTc interval in schizophrenia., Prog Neuropsychopharmacol Biol Psychiatry

Lee CA et al., 2010, Identification of novel substrates for human cytochrome P450 2J2., Drug Metab Dispos

Dorado P et al., 2009, Relevance of CYP2D6 -1584C>G polymorphism for thioridazine:mesoridazine plasma concentration ratio in psychiatric patients., Pharmacogenomics

DTC: THIORIDAZINE
- Version: 02-September-2020
Alternate Names:

CHEMBL479 ChEMBL Drug ID

Drug Info:

Publications:
TTD: Thioridazine
- Version: 2020.06.01
Alternate Names:

D0U1OE TTD Drug ID

Drug Info:

Publications:
GuideToPharmacology: 135651259
- Version: 29-September-2020
Alternate Names:

THIORIDAZINE GuideToPharmacology Ligand Name

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL479
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
FDA: Thioridazine
- Version: 04-September-2020
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL479
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:

Direct Interaction?	True
Endogenous Drug?	False
Specific Action of the Ligand	Antagonist

Trial Name	-
Novel drug target	Established target
Mechanism of Interaction	D2-like dopamine receptor antagonist

Specific Action of the Ligand	Inverse agonist
Endogenous Drug?	False

Direct Interaction	yes
Mechanism of Interaction	D2-like dopamine receptor antagonist

THIORIDAZINE	DrugBank Drug Name
50-52-2	CAS Number
Aldazine	Drug Brand

Drug Type	small molecule
Drug Groups	approved
Drug Groups	withdrawn

THIORIDAZINE Drug Record

THIORIDAZINE chembl:CHEMBL479

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 19923256

Sources: PharmGKB

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Direct Interaction? True Endogenous Drug? False Specific Action of the Ligand Antagonist

PMIDs: 8680734 9918563 7898773 2866233 2423886

Sources: TEND TdgClinicalTrial DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target Mechanism of Interaction D2-like dopamine receptor antagonist

PMIDs: 7689973 9292626 1978482 16434058 1352051

Sources: TEND TdgClinicalTrial TTD DrugBank ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name - Endogenous Drug? False

PMIDs: 8720030

Sources: TEND DTC TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 7691623 15695070

Sources: TEND TdgClinicalTrial DrugBank

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Endogenous Drug? False Specific Action of the Ligand Inverse agonist

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info:

PMIDs: 15695070

Sources: DrugBank

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False Direct Interaction? True

PMIDs: None found

Sources: GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Inverse agonist Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction D2-like dopamine receptor antagonist

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 16278312 17056009

Sources: PharmGKB DrugBank

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction D2-like dopamine receptor antagonist Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 19604081 2007317

Sources: FDA PharmGKB

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Endogenous Drug? False Specific Action of the Ligand Antagonist

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Interaction Types & Directionality:

n/a

PMIDs:
19923256

Sources:
PharmGKB

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
8680734 9918563 7898773 2866233 2423886

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Mechanism of Interaction D2-like dopamine receptor antagonist

PMIDs:
7689973 9292626 1978482 16434058 1352051

Sources:
TEND TdgClinicalTrial TTD DrugBank ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Endogenous Drug? False

PMIDs:
8720030

Sources:
TEND DTC TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
7691623 15695070

Sources:
TEND TdgClinicalTrial DrugBank

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Inverse agonist

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

PMIDs:
15695070

Sources:
DrugBank

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
None found

Sources:
GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Inverse agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction D2-like dopamine receptor antagonist

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
16278312 17056009

Sources:
PharmGKB DrugBank

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction D2-like dopamine receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
19604081 2007317

Sources:
FDA PharmGKB

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
17611010

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Alternate Names:

THIORIDAZINE DrugBank Drug Name

50-52-2 CAS Number

Aldazine Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups withdrawn

Alternate Names:

THIORIDAZINE Primary Drug Name

Drug Info:

Year of Approval 1962

Drug Class antipsychotic agents

Drug Info:

Drug Indications Antipsychotic Agents

Drug Class small molecule

FDA Approval 1962