Identification

Name
Quetiapine
Accession Number
DB01224  (APRD00675)
Type
Small Molecule
Groups
Approved
Description

Quetiapine is indicated for the treatment of schizophrenia as well as for the treatment of acute manic episodes associated with bipolar I disorder. The antipsychotic effect of quetiapine is thought by some to be mediated through antagonist activity at dopamine and serotonin receptors. Specifically the D1 and D2 dopamine, the alpha 1 adrenoreceptor and alpha 2 adrenoreceptor, and 5-HT1A and 5-HT2 serotonin receptor subtypes are antagonized. Quetiapine also has an antagonistic effect on the histamine H1 receptor.

Structure
Thumb
Synonyms
  • 2-[2-(4-Dibenzo[b,f][1,4]thiazepin-11-yl-1-piperazinyl)ethoxy]ethanol
  • Quetiapina
  • Quétiapine
  • Quetiapinum
Product Ingredients
IngredientUNIICASInChI Key
Quetiapine fumarate2S3PL1B6UJ111974-72-2ZTHJULTYCAQOIJ-WXXKFALUSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Act QuetiapineTablet150 mgOralActavis Pharma CompanyNot applicableNot applicableCanada
Act QuetiapineTablet100 mgOralActavis Pharma Company2008-09-04Not applicableCanada
Act QuetiapineTablet300 mgOralActavis Pharma Company2008-09-04Not applicableCanada
Act QuetiapineTablet25 mgOralActavis Pharma Company2008-09-04Not applicableCanada
Act QuetiapineTablet200 mgOralActavis Pharma Company2008-09-04Not applicableCanada
QuetiapineTablet25 mgOralCobalt LaboratoriesNot applicableNot applicableCanada
QuetiapineTablet300 mgOralSanis Health Inc2010-07-26Not applicableCanada
QuetiapineTablet25 mgOralSanis Health Inc2010-07-26Not applicableCanada
QuetiapineTablet100 mgOralSivem Pharmaceuticals Ulc2009-02-26Not applicableCanada
QuetiapineTablet150 mgOralCobalt LaboratoriesNot applicableNot applicableCanada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Abbott-quetiapineTablet, multilayer, extended release200 mgOralBgp Pharma Ulc2014-06-132015-12-31Canada
Abbott-quetiapineTablet, multilayer, extended release100 mgOralBgp Pharma Ulc2014-06-092015-12-31Canada
Abbott-quetiapineTablet, multilayer, extended release300 mgOralBgp Pharma Ulc2014-06-092015-12-31Canada
Abbott-quetiapineTablet, multilayer, extended release25 mgOralBgp Pharma Ulc2014-06-092015-12-31Canada
Accel-quetiapineTablet300 mgOralAccel Pharma Inc2015-03-262017-01-27Canada
Accel-quetiapineTablet100 mgOralAccel Pharma Inc2015-03-262017-01-27Canada
Accel-quetiapineTablet200 mgOralAccel Pharma Inc2015-03-262017-01-27Canada
Accel-quetiapineTablet25 mgOralAccel Pharma Inc2015-03-262017-01-27Canada
Accel-quetiapineTablet150 mgOralAccel Pharma Inc2015-03-032017-01-27Canada
Ach-quetiapine Fumarate XRTablet, extended release300 mgOralAccord Healthcare LimitedNot applicableNot applicableCanada
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Seroquel XRQuetiapine fumarate (50 mg/1) + Quetiapine fumarate (200 mg/1) + Quetiapine fumarate (300 mg/1)KitAstraZeneca Pharmaceuticals LP2014-10-022019-08-31Us
Seroquel XRQuetiapine fumarate (50 mg/1) + Quetiapine fumarate (200 mg/1) + Quetiapine fumarate (300 mg/1)KitAstraZeneca Pharmaceuticals LP2014-10-022019-08-31Us
Seroquel XRQuetiapine fumarate (50 mg/1) + Quetiapine fumarate (200 mg/1) + Quetiapine fumarate (300 mg/1)KitAstraZeneca Pharmaceuticals LP2014-10-022019-08-31Us
Categories
UNII
BGL0JSY5SI
CAS number
111974-69-7
Weight
Average: 383.507
Monoisotopic: 383.166747749
Chemical Formula
C21H25N3O2S
InChI Key
URKOMYMAXPYINW-UHFFFAOYSA-N
InChI
InChI=1S/C21H25N3O2S/c25-14-16-26-15-13-23-9-11-24(12-10-23)21-17-5-1-3-7-19(17)27-20-8-4-2-6-18(20)22-21/h1-8,25H,9-16H2
IUPAC Name
2-[2-(4-{2-thia-9-azatricyclo[9.4.0.0³,⁸]pentadeca-1(15),3,5,7,9,11,13-heptaen-10-yl}piperazin-1-yl)ethoxy]ethan-1-ol
SMILES
OCCOCCN1CCN(CC1)C1=NC2=CC=CC=C2SC2=CC=CC=C12

Pharmacology

Indication

For the treatment of schizophrenia and related psychotic disorders.

Associated Conditions
Pharmacodynamics

Quetiapine is a psychotropic agent belonging to the chemical class of benzisoxazole derivatives and is indicated for the treatment of schizophrenia. Quetiapine is a selective monoaminergic antagonist with high affinity for the serotonin Type 2 (5HT2), and dopamine type 2 (D2) receptors. Quetiapine is an antagonist at serotonin 5-HT1A and 5HT2, dopamine D1 and D2, histamine H1, and adrenergic alpha 1 and alpha 2 receptors. Quetiapine has no significant affinity for cholinergic muscarinic or benzodiazepine receptors. Drowsiness and orthostatic hypotension associated with use of quetiapine may be explained by its antagonism of histamine H1 and adrenergic alpha 1 receptors, respectively. Quetiapine's antagonism of adrenergic a1 receptors may explain the orthostatic hypotension observed with this drug.

Mechanism of action

Quetiapine's antipsychotic activity is likely due to a combination of antagonism at D2 receptors in the mesolimbic pathway and 5HT2A receptors in the frontal cortex. Antagonism at D2 receptors relieves positive symptoms while antagonism at 5HT2A receptors relieves negative symptoms of schizophrenia.

TargetActionsOrganism
A5-hydroxytryptamine receptor 2A
antagonist
Human
AD(2) dopamine receptor
antagonist
Human
U5-hydroxytryptamine receptor 1A
antagonist
Human
U5-hydroxytryptamine receptor 1B
other/unknown
Human
U5-hydroxytryptamine receptor 1D
other/unknown
Human
U5-hydroxytryptamine receptor 1E
other/unknown
Human
U5-hydroxytryptamine receptor 2C
antagonist
Human
U5-hydroxytryptamine receptor 3A
other/unknown
Human
U5-hydroxytryptamine receptor 6
other/unknown
Human
U5-hydroxytryptamine receptor 7
antagonist
Human
UD(1A) dopamine receptor
antagonist
Human
UD(1B) dopamine receptor
antagonist
Human
UD(3) dopamine receptor
antagonist
Human
UD(4) dopamine receptor
antagonist
Human
UHistamine H1 receptor
antagonist
Human
UAlpha-1A adrenergic receptor
antagonist
Human
UAlpha-1B adrenergic receptor
antagonist
Human
UAlpha-1D adrenergic receptor
antagonist
Human
UAlpha-2A adrenergic receptor
antagonist
Human
UAlpha-2B adrenergic receptor
antagonist
Human
UAlpha-2C adrenergic receptor
antagonist
Human
UMuscarinic acetylcholine receptor M1
antagonist
Human
UMuscarinic acetylcholine receptor M2
antagonist
Human
UMuscarinic acetylcholine receptor M3
antagonist
Human
UMuscarinic acetylcholine receptor M4
antagonist
Human
UMuscarinic acetylcholine receptor M5
antagonist
Human
Absorption

Rapidly and well absorbed.

Volume of distribution
  • 10±4 L/kg
Protein binding

83%

Metabolism

Hepatic. The major metabolic pathways are sulfoxidation, mediated by cytochrome P450 3A4 (CYP3A4), and oxidation of the terminal alcohol to a carboxylic acid. The major sulfoxide metabolite of quetiapine is inactive. Quetiapine also undergoes hydroxylation of the dibenzothiazepine ring, O-deakylation, N-dealkylation, and phase II conjugation. The 7-hydroxy and 7-hydroxy- N-delakylated metabolites appear to be active, but are present in very low concentrations.

Route of elimination

Elimination of quetiapine is mainly via hepatic metabolism. Following a single oral dose of 14C-quetiapine, less than 1% of the administered dose was excreted as unchanged drug, indicating that quetiapine is highly metabolized. Approximately 73% and 20% of the dose was recovered in the urine and feces, respectively.

Half life

6 hours

Clearance
Not Available
Toxicity

Symptoms of overdose include drowsiness and sedation, tachycardia, and hypotension.

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Quetiapine H1-Antihistamine ActionDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(2-benzhydryloxyethyl)diethyl-methylammonium iodideThe risk or severity of adverse effects can be increased when Quetiapine is combined with (2-benzhydryloxyethyl)diethyl-methylammonium iodide.
(R)-warfarinThe metabolism of Quetiapine can be decreased when combined with (R)-warfarin.
(S)-WarfarinThe metabolism of Quetiapine can be decreased when combined with (S)-Warfarin.
1,10-PhenanthrolineThe therapeutic efficacy of Quetiapine can be decreased when used in combination with 1,10-Phenanthroline.
2,4-thiazolidinedioneThe therapeutic efficacy of 2,4-thiazolidinedione can be decreased when used in combination with Quetiapine.
2,5-Dimethoxy-4-ethylamphetamineThe risk or severity of serotonin syndrome can be increased when Quetiapine is combined with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamineThe risk or severity of serotonin syndrome can be increased when Quetiapine is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3,4-MethylenedioxyamphetamineThe risk or severity of serotonin syndrome can be increased when Quetiapine is combined with 3,4-Methylenedioxyamphetamine.
3,5-diiodothyropropionic acidThe metabolism of Quetiapine can be decreased when combined with 3,5-diiodothyropropionic acid.
3,5-DinitrocatecholThe therapeutic efficacy of 3,5-Dinitrocatechol can be decreased when used in combination with Quetiapine.
Food Interactions
  • Avoid alcohol.
  • Take without regard to meals.

References

Synthesis Reference
US4879288
General References
  1. Dev V, Raniwalla J: Quetiapine: a review of its safety in the management of schizophrenia. Drug Saf. 2000 Oct;23(4):295-307. [PubMed:11051217]
  2. Mukaddes NM, Abali O: Quetiapine treatment of children and adolescents with Tourette's disorder. J Child Adolesc Psychopharmacol. 2003 Fall;13(3):295-9. [PubMed:14642017]
  3. Tallerico T, Novak G, Liu IS, Ulpian C, Seeman P: Schizophrenia: elevated mRNA for dopamine D2(Longer) receptors in frontal cortex. Brain Res Mol Brain Res. 2001 Mar 5;87(2):160-5. [PubMed:11245917]
  4. Urichuk L, Prior TI, Dursun S, Baker G: Metabolism of atypical antipsychotics: involvement of cytochrome p450 enzymes and relevance for drug-drug interactions. Curr Drug Metab. 2008 Jun;9(5):410-8. [PubMed:18537577]
External Links
Human Metabolome Database
HMDB0005021
KEGG Drug
D08456
KEGG Compound
C07397
PubChem Compound
5002
PubChem Substance
46504800
ChemSpider
4827
BindingDB
50095890
ChEBI
8707
ChEMBL
CHEMBL716
Therapeutic Targets Database
DAP000001
PharmGKB
PA451201
IUPHAR
50
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Quetiapine
ATC Codes
N05AH04 — Quetiapine
AHFS Codes
  • 28:16.08.04 — Atypical Antipsychotics
FDA label
Download (273 KB)
MSDS
Download (57.1 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0TerminatedPreventionSocial Anxiety Disorder (SAD)1
0TerminatedTreatmentMethamphetamine Dependence1
1CompletedNot AvailableBipolar Disorder (BD)1
1CompletedNot AvailableSchizophrenic Disorders1
1CompletedBasic ScienceBipolar Disorder (BD) / Depressive Disorders / Psychotic Disorder NOS / Schizophrenic Disorders1
1CompletedBasic ScienceDepression1
1CompletedBasic ScienceHealthy Volunteers1
1CompletedTreatmentDyskinesia, Drug-Induced1
1CompletedTreatmentFasting State1
1CompletedTreatmentFed1
1CompletedTreatmentHealthy Volunteers3
1CompletedTreatmentSchizoaffective Disorders / Schizophrenic Disorders1
1CompletedTreatmentSchizophrenic Disorders1
1Unknown StatusTreatmentCocaine-Related Disorders1
1Unknown StatusTreatmentHealthy Volunteers1
1, 2RecruitingBasic ScienceSchizophrenic Disorders1
1, 2RecruitingTreatmentDisseminated Sclerosis1
1, 2TerminatedTreatmentDelirium1
2CompletedNot AvailableSpecific Phobias1
2CompletedBasic ScienceSmoking, Marijuana1
2CompletedTreatmentAlcohol Abuse / Alcohol Consumption / Alcohol Drinking / Alcohol Relapse Prevention / Alcoholism1
2CompletedTreatmentAlcohol Abuse / Alcoholism1
2CompletedTreatmentAlcohol Dependence1
2CompletedTreatmentAlcoholism1
2CompletedTreatmentAttention Deficit Disorder With Hyperactivity1
2CompletedTreatmentBorderline Personality Disorder (BPD)1
2CompletedTreatmentCannabis Dependence2
2CompletedTreatmentDepression, Bipolar1
2CompletedTreatmentMajor Depressive Disorder (MDD)2
2CompletedTreatmentObsessive Compulsive Disorder (OCD)1
2RecruitingTreatmentMajor Depressive Disorder (MDD)1
2RecruitingTreatmentSchizophrenic Disorders1
2TerminatedTreatmentAnorexia Nervosa (AN)1
2TerminatedTreatmentBipolar Disorder (BD)1
2TerminatedTreatmentDepression in Patients With Bipolar Disorder1
2TerminatedTreatmentNicotine Dependence / Nicotine Use Disorder / Smoking / Tobacco Use Disorders1
2TerminatedTreatmentPostpartum Depressive Disorder1
2TerminatedTreatmentSchizoaffective Disorders / Schizophrenic Disorders1
2WithdrawnTreatmentMajor Depressive Disorder (MDD)1
2, 3CompletedTreatmentBipolar Disorder (BD)1
2, 3CompletedTreatmentBipolar II Disorder1
2, 3CompletedTreatmentSchizoaffective Disorders / Schizophrenic Disorders1
2, 3CompletedTreatmentSleeplessness1
2, 3CompletedTreatmentSocial Anxiety Disorder (SAD)1
2, 3Not Yet RecruitingTreatmentDelirium1
2, 3TerminatedTreatmentSchizophrenic Disorders1
3Active Not RecruitingTreatmentPsychotic Disorder NOS / Schizophrenic Disorders1
3CompletedNot AvailableBipolar Disorder (BD)1
3CompletedPreventionBipolar I Disorder1
3CompletedTreatmentAcute Bipolar Depression1
3CompletedTreatmentAlcohol Dependence / Bipolar I Disorder1
3CompletedTreatmentAlcoholism1
3CompletedTreatmentAlcoholism / Sleep Initiation and Maintenance Disorders1
3CompletedTreatmentAlzheimer's Disease (AD) / Dementia, Vascular1
3CompletedTreatmentAnxiety Disorders1
3CompletedTreatmentAnxiety Disorders / Anxiety States / Feeling Anxious / Neuroses, Anxiety1
3CompletedTreatmentAnxiety Disorders / Bipolar Disorder (BD) / Feeling Anxious / Substance Use Disorder (SUD)1
3CompletedTreatmentBipolar Disorder (BD)6
3CompletedTreatmentBipolar Disorder (BD) / Depression, Bipolar2
3CompletedTreatmentBipolar Disorder (BD) / Depression / Depression, Bipolar1
3CompletedTreatmentBipolar Disorder (BD) / Elderly1
3CompletedTreatmentBipolar Disorder (BD) / Mania1
3CompletedTreatmentBipolar Disorder (BD) / Moods Disorders1
3CompletedTreatmentBipolar Disorder (BD) / Schizophrenic Disorders1
3CompletedTreatmentBipolar I Disorder1
3CompletedTreatmentBipolar I Disorder / Schizophrenic Disorders1
3CompletedTreatmentBipolar Youth Treated With Second-generation Antipsychotics1
3CompletedTreatmentBorderline Personality Disorder (BPD)2
3CompletedTreatmentChronic Schizophrenia1
3CompletedTreatmentCognition / Schizophrenic Disorders1
3CompletedTreatmentDelirium1
3CompletedTreatmentDepression, Bipolar3
3CompletedTreatmentDepression / Depressive Disorders / Major Depressive Disorder (MDD) / Moods Disorders / Psychiatric Disorder NOS1
3CompletedTreatmentDepression / Schizophrenic Disorders1
3CompletedTreatmentGeneralized Anxiety Disorder (GAD)3
3CompletedTreatmentMajor Depressive Disorder (MDD)8
3CompletedTreatmentMajor Depressive Disorder (MDD) / Treatment Resistant Depression (TRD)1
3CompletedTreatmentMoods Disorders1
3CompletedTreatmentObsessive Compulsive Disorder (OCD)1
3CompletedTreatmentPost-Traumatic Stress Disorder (PTSD)1
3CompletedTreatmentPsychosis1
3CompletedTreatmentPsychotic Depression1
3CompletedTreatmentPsychotic Disorder NOS1
3CompletedTreatmentPsychotic Disorder NOS / Schizophrenic Disorders1
3CompletedTreatmentSchizoaffective Disorders / Schizophrenic Disorders1
3CompletedTreatmentSchizophrenia and Schizoaffective Disorder1
3CompletedTreatmentSchizophrenic Disorders12
3CompletedTreatmentSleep1
3CompletedTreatmentSocial Anxiety Disorder (SAD)1
3CompletedTreatmentUnipolar Depression1
3RecruitingTreatmentSchizophrenic Disorders1
3TerminatedTreatmentAcute Agitation / Dementias1
3TerminatedTreatmentAnxiety Disorders / Dementias / Depression / Psychosomatic Disorders / Schizophrenic Disorders1
3TerminatedTreatmentBipolar Disorder (BD) / Psychotic Disorder NOS / Schizophrenic Disorders1
3TerminatedTreatmentDelirium1
3TerminatedTreatmentDepression With Prominent Agitation1
3TerminatedTreatmentGeneralized Anxiety Disorder (GAD) / Major Depressive Disorder (MDD)1
3TerminatedTreatmentMajor Depression With Psychotic Features1
3TerminatedTreatmentPsychotic Disorder NOS / Schizoaffective Disorders / Schizophrenic Disorders1
3TerminatedTreatmentSchizophrenic Disorders6
3TerminatedTreatmentSocial Anxiety Disorder (SAD)1
3Unknown StatusPreventionDelirium1
3Unknown StatusTreatmentBipolar Disorder (BD)1
3Unknown StatusTreatmentFeeling Anxious / Schizophrenic Disorders1
3Unknown StatusTreatmentPsychosis Nos/Other1
4Active Not RecruitingTreatmentBipolar Disorder (BD)1
4Active Not RecruitingTreatmentMajor Depressive Disorder (MDD)1
4CompletedNot AvailableBipolar Disorder (BD)1
4CompletedNot AvailableDepression, Bipolar1
4CompletedNot AvailableMajor Depressive Disorder (MDD)1
4CompletedNot AvailableSchizophrenic Disorders2
4CompletedNot AvailableSchizophrenic Disorders / Substance Use Disorder (SUD)1
4CompletedDiagnosticSchizophrenic Disorders1
4CompletedOtherAlcohol Abuse / Psychotic Disorder NOS / Schizoaffective Disorders / Schizophrenic Disorders / Substance Abuse1
4CompletedOtherHealthy Volunteers1
4CompletedPreventionSchizophrenic Disorders1
4CompletedTreatmentAcute Agitation1
4CompletedTreatmentAcute Mania1
4CompletedTreatmentAcute Mania in Bipolar Disorder1
4CompletedTreatmentAlcohol Abuse/Dependence / Bipolar Disorder (BD)1
4CompletedTreatmentAlcohol Abuse / Bipolar Disorder (BD)1
4CompletedTreatmentAlcohol Dependence / Bipolar Disorder (BD)1
4CompletedTreatmentAlcoholism / Anxiety Disorders / Generalized Anxiety Disorder (GAD) / Obsessive-Compulsive Disorder (OCD) / Panic Disorders / Post-Traumatic Stress Disorder (PTSD)1
4CompletedTreatmentAlzheimer's Disease (AD) / Dementia, Alzheimer Type / Dementias / Senile Dementia, Alzheimer Type1
4CompletedTreatmentAnxiety Disorders1
4CompletedTreatmentBipolar Affective Psychosis / Bipolar Disorder (BD) / Mania / Manic Disorder / Manic syndromes1
4CompletedTreatmentBipolar Disorder (BD)4
4CompletedTreatmentBipolar Disorder (BD) / Cannabis-Related Disorder1
4CompletedTreatmentBipolar Disorder (BD) / Dependence, Cocaine1
4CompletedTreatmentBipolar Disorder (BD) / Mania1
4CompletedTreatmentBipolar I Disorder / Bipolar II Disorder1
4CompletedTreatmentBipolar II Disorder1
4CompletedTreatmentBipolar Spectrum Disorder1
4CompletedTreatmentCocaine-Related Disorders / Substance-Related Disorders1
4CompletedTreatmentCombat Disorders / Stress Disorders, Post-Traumatic1
4CompletedTreatmentDementias / Parkinson's Disease (PD)1
4CompletedTreatmentDepression1
4CompletedTreatmentDepression / Feeling Anxious1
4CompletedTreatmentDepression / Healthy Volunteers1
4CompletedTreatmentFibromyalgia3
4CompletedTreatmentHyperglycemias / Schizoaffective Disorders / Schizophrenic Disorders / Type 2 Diabetes Mellitus1
4CompletedTreatmentMajor Depression With Comorbid Anxiety Symptoms1
4CompletedTreatmentMajor Depressive Disorder (MDD)3
4CompletedTreatmentMajor Depressive Disorder (MDD) / Menopausal Hot Flushes / Sleeplessness1
4CompletedTreatmentMood Disorders With Comorbid Anxiety Symptoms / Primary Anxiety Disorders1
4CompletedTreatmentObsessive Compulsive Disorder (OCD)2
4CompletedTreatmentPTSD1
4CompletedTreatmentPanic Disorders1
4CompletedTreatmentPsychomotor Agitation1
4CompletedTreatmentPsychotic Disorder NOS2
4CompletedTreatmentPsychotic Disorder NOS / Schizophrenic Disorders3
4CompletedTreatmentSchizoaffective Disorders / Schizophrenia and Disorders With Psychotic Features / Schizophrenic Disorders1
4CompletedTreatmentSchizoaffective Disorders / Schizophrenic Disorders5
4CompletedTreatmentSchizoaffective Disorders / Schizophrenic Disorders / Substance Abuse / Substance Dependence1
4CompletedTreatmentSchizophrenic Disorders17
4CompletedTreatmentSchizophrenic Disorders / Type 2 Diabetes Mellitus1
4CompletedTreatmentSocial Anxiety Disorder (SAD)1
4CompletedTreatmentSocial Phobia1
4RecruitingDiagnosticAsthma Bronchial / Asthma: [Nos] or [Attack] / Major Depressive Disorder (MDD)1
4RecruitingDiagnosticFirst Episode Psychosis / Schizoaffective Disorders / Schizophrenic Disorders1
4RecruitingTreatmentBipolar Disorder (BD)2
4RecruitingTreatmentBipolar Disorder (BD) / Substance Use Disorder (SUD)1
4RecruitingTreatmentDefect, Congenital Heart1
4RecruitingTreatmentDepressive Disorder, Treatment-Resistant1
4RecruitingTreatmentSchizophrenic Disorders1
4TerminatedNot AvailableHigh Risk MC4R Genotype / Low Risk MC4R Genotype / One Week or Less Antipsychotic Lifetime Exposure1
4TerminatedTreatmentAcute Bipolar Mania2
4TerminatedTreatmentBipolar Disorder (BD)2
4TerminatedTreatmentBipolar Disorder (BD) / Cognitive Impairments1
4TerminatedTreatmentComorbid Opiate Dependence in Remission / Generalized Anxiety Disorder (GAD) / Status Post Methadone-Maintenance Treatment1
4TerminatedTreatmentGeneralized Anxiety Disorder (GAD) / Major Depressive Disorder (MDD)1
4TerminatedTreatmentMajor Depressive Disorder With Psychotic Features1
4TerminatedTreatmentSchizoaffective Disorders / Schizophrenic Disorders / Schizophreniform Disorder1
4TerminatedTreatmentSchizophrenic Disorders1
4Unknown StatusBasic ScienceDepression, Bipolar1
4Unknown StatusTreatmentAbnormal Mental State / Schizophrenic Disorders1
4Unknown StatusTreatmentAcute Schizophrenia1
4Unknown StatusTreatmentBipolar Disorder (BD)1
4Unknown StatusTreatmentBipolar, Mania / Seroquel / Utapine1
4Unknown StatusTreatmentBipolar / Schizophrenic Disorders1
4Unknown StatusTreatmentMajor Depressive Disorder (MDD)1
4Unknown StatusTreatmentMental Health Disorder / Sleeplessness / Substance Use Disorder (SUD)1
4Unknown StatusTreatmentPsychosis1
4Unknown StatusTreatmentPsychosis / Schizophrenic Disorders1
4Unknown StatusTreatmentSchizophrenia or Schizoaffective Disorder1
4Unknown StatusTreatmentSchizophrenic Disorders1
4WithdrawnPreventionSchizophrenic Disorders1
4WithdrawnTreatmentAlzheimer's Disease (AD) / Behavioral Symptoms / Dementias1
4WithdrawnTreatmentDepression, Bipolar1
Not AvailableActive Not RecruitingTreatmentSchizophrenia Relapse1
Not AvailableCompletedNot AvailableBipolar Disorder (BD)1
Not AvailableCompletedNot AvailableBipolar Disorder (BD) / Metabolic Syndromes / Psychotic Disorder NOS1
Not AvailableCompletedNot AvailableBipolar Disorder (BD) / Psychotic Disorder NOS / Schizoaffective Disorders / Schizophrenic Disorders / Type 2 Diabetes Mellitus1
Not AvailableCompletedNot AvailableDelirium / Dementias1
Not AvailableCompletedNot AvailableSchizophrenic Disorders2
Not AvailableCompletedDiagnosticBipolar Disorder (BD) / Mania1
Not AvailableCompletedDiagnosticSchizophrenic Disorders1
Not AvailableCompletedTreatmentAlzheimer's Disease (AD)1
Not AvailableCompletedTreatmentAnxiety Disorders / Dysthymic Disorder / Generalized Anxiety Disorder (GAD) / Major Depressive Disorder (MDD) / Panic Disorders / Post-Traumatic Stress Disorder (PTSD) / Social Anxiety Disorder (SAD)1
Not AvailableCompletedTreatmentBipolar Disorder (BD)1
Not AvailableCompletedTreatmentBipolar Disorder (BD) / Dependence, Cocaine / Methamphetamine Dependence1
Not AvailableCompletedTreatmentBipolar I Disorder2
Not AvailableCompletedTreatmentCocaine Abuse / Dependence, Cocaine / Drug Abuse / Substance Abuse1
Not AvailableCompletedTreatmentFunctional Bowel Disorders1
Not AvailableCompletedTreatmentGeneralized Anxiety Disorder (GAD) / Major Depressive Disorder (MDD)1
Not AvailableCompletedTreatmentPhysiology, Ocular / Regional Blood Flow1
Not AvailableCompletedTreatmentPost-Traumatic Stress Disorder (PTSD)1
Not AvailableCompletedTreatmentPostpartum Depression1
Not AvailableCompletedTreatmentPrimary Insomnia1
Not AvailableCompletedTreatmentPsychotic Disorder NOS / Schizoaffective Disorders / Schizophrenic Disorders / Schizophreniform Disorders1
Not AvailableCompletedTreatmentSchizoaffective Disorders / Schizophrenic Disorders1
Not AvailableCompletedTreatmentSchizophrenic Disorders3
Not AvailableCompletedTreatmentTreatment for Bipolar I Disorder1
Not AvailableEnrolling by InvitationNot AvailableBipolar Disorder (BD)1
Not AvailableNot Yet RecruitingBasic ScienceBipolar Disorder (BD) / Depression1
Not AvailableRecruitingNot AvailableAcute Bacterial Exacerbation of Chronic Bronchitis (ABECB) / Acute Bacterial Sinusitis (ABS) / Acute Decompensated Heart Failure (ADHF) / Acute Pyelonephritis / Adenovirus / Adjunct to general anesthesia therapy / Adrenal Insufficiency / Airway Swelling / Anaesthesia therapy / Anxiolysis / Arterial Hypotension / Autism, Early Infantile / Autistic Disorder / Bartonellosis / Benzodiazepine Withdrawal / Benzodiazepines / Bipolar Disorder (BD) / Bloodstream Infections / Bone and Joint Infections / Brain Swelling / Bronchospasm / Brucellosis / Cardiac Arrest / Central Nervous System Infections / Cholera / Chronic Bacterial Prostatitis / Community Acquired Pneumonia (CAP) / Complicated Urinary Tract Infections / Convulsions / Cyanide Poisoning / Cytomegalovirus Retinitis / Drug hypersensitivity reaction / Early-onset Schizophrenia Spectrum Disorders / Edema / Epilepsies / Feeling Anxious / Flu caused by Influenza / Gastroparesis / Gynaecological infection / Headaches / Herpes Simplex Virus / High Blood Pressure (Hypertension) / High Cholesterol / Hospital-acquired bacterial pneumonia / Hyperlipidemias / Infantile Hemangiomas / Infection NOS / Inflammatory Conditions / Inflammatory Reaction / Influenza Treatment or Prophylaxis / Inhalational Anthrax (Post-Exposure) / Intra-Abdominal Infections / Life-threatening Fungal Infections / Lower Respiratory Tract Infection (LRTI) / Meningitis, Bacterial / Migraines / Muscle Spasms / Nausea / Opioid Addiction / Pain NOS / Plague / Pneumonia / Prophylaxis / Psittacosis / Q Fever / Reflux / Relapsing Fever / Rocky Mountain Spotted Fever / Schizophrenic Disorders / Sedation therapy / Seizures / Sepsis / Skeletal Muscle Spasms / Skin and Subcutaneous Tissue Bacterial Infections / Skin Structures and Soft Tissue Infections / Stable Angina (SA) / Thromboprophylaxis / Thrombosis / Trachoma / Treatment-resistant Schizophrenia / Tularemia / Typhus Fever / Uncomplicated Skin and Skin Structure Infections / Uncomplicated Urinary Tract Infections / Urinary Tract Infections (UTIs) / Vomiting / Withdrawal1
Not AvailableRecruitingNot AvailableBipolar Disorder (BD)1
Not AvailableRecruitingNot AvailableBipolar Disorder (BD) / Depression1
Not AvailableRecruitingNot AvailableMicrognathia / Schizophrenic Disorders1
Not AvailableRecruitingNot AvailableObesity, Morbid1
Not AvailableRecruitingNot AvailableSchizophrenic Disorders1
Not AvailableTerminatedTreatmentGeneralized Anxiety Disorder (GAD) / Seroquel XR1
Not AvailableUnknown StatusNot AvailableDissociative Disorders1
Not AvailableUnknown StatusEducational/Counseling/TrainingSmoking Behavior in Schizophrenia1
Not AvailableUnknown StatusPreventionPsychotic Disorder NOS1
Not AvailableUnknown StatusTreatmentAlzheimer's Disease (AD) / Sleeplessness1
Not AvailableUnknown StatusTreatmentAnorexia Nervosa (AN)1
Not AvailableUnknown StatusTreatmentBipolar Disorder (BD)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Advanced Pharmaceutical Services Inc.
  • AQ Pharmaceuticals Inc.
  • A-S Medication Solutions LLC
  • AstraZeneca Inc.
  • Atlantic Biologicals Corporation
  • Bryant Ranch Prepack
  • Cardinal Health
  • Comprehensive Consultant Services Inc.
  • Coupler Enterprises Inc.
  • Direct Dispensing Inc.
  • Heartland Repack Services LLC
  • Innoviant Pharmacy Inc.
  • Lake Erie Medical and Surgical Supply
  • Murfreesboro Pharmaceutical Nursing Supply
  • Neuman Distributors Inc.
  • Norwich Pharmaceuticals Inc.
  • Nucare Pharmaceuticals Inc.
  • PD-Rx Pharmaceuticals Inc.
  • Physicians Total Care Inc.
  • Prepackage Specialists
  • Prepak Systems Inc.
  • Rebel Distributors Corp.
  • Remedy Repack
  • Resource Optimization and Innovation LLC
  • Southwood Pharmaceuticals
  • Tya Pharmaceuticals
  • Vangard Labs Inc.
  • Wyeth Pharmaceuticals
Dosage forms
FormRouteStrength
Tablet, multilayer, extended releaseOral100 mg
Tablet, multilayer, extended releaseOral200 mg
Tablet, multilayer, extended releaseOral25 mg
Tablet, multilayer, extended releaseOral300 mg
TabletOral50 mg
Tablet, film coated, extended releaseOral150 mg/1
Tablet, film coated, extended releaseOral300 mg/1
Tablet, film coated, extended releaseOral400 mg/1
TabletOral100 mg/1
TabletOral150 mg/1
TabletOral200 mg/1
TabletOral25 mg/1
TabletOral300 mg/1
TabletOral400 mg/1
TabletOral50 mg/1
Tablet, film coatedOral150 mg/1
Tablet, film coated, extended releaseOral200 mg/1
Tablet, film coated, extended releaseOral50 mg/1
Tablet, film coatedOral100 mg/1
Tablet, film coatedOral200 mg/1
Tablet, film coatedOral25 mg/1
Tablet, film coatedOral300 mg/1
Tablet, film coatedOral400 mg/1
Tablet, film coatedOral50 mg/1
TabletOral300 mg
TabletOral100 mg
TabletOral200 mg
TabletOral25 mg
Kit
Tablet, extended releaseOral150 mg
Tablet, extended releaseOral150 mg/1
Tablet, extended releaseOral200 mg/1
Tablet, extended releaseOral200 mg
Tablet, extended releaseOral300 mg/1
Tablet, extended releaseOral300 mg
Tablet, extended releaseOral400 mg/1
Tablet, extended releaseOral400 mg
Tablet, extended releaseOral50 mg
Tablet, extended releaseOral50 mg/1
TabletOral150 mg
Prices
Unit descriptionCostUnit
Seroquel 400 mg tablet16.71USD tablet
Seroquel xr 400 mg tablet14.82USD tablet
Seroquel 300 mg tablet14.21USD tablet
Seroquel xr 300 mg tablet12.61USD tablet
Seroquel 200 mg tablet10.84USD tablet
SEROquel XR 200 mg 24 Hour tablet10.0USD tablet
Seroquel xr 200 mg tablet9.62USD tablet
SEROquel XR 150 mg 24 Hour tablet9.09USD tablet
Seroquel xr 150 mg tablet8.74USD tablet
Seroquel 100 mg tablet5.75USD tablet
Seroquel 50 mg tablet5.5USD tablet
SEROquel XR 50 mg 24 Hour tablet5.06USD tablet
Seroquel xr 50 mg tablet4.87USD tablet
Seroquel 300 mg Tablet4.35USD tablet
Seroquel 25 mg tablet3.35USD tablet
Seroquel 200 mg Tablet2.98USD tablet
Apo-Quetiapine 300 mg Tablet2.44USD tablet
Co Quetiapine 300 mg Tablet2.44USD tablet
Jamp-Quetiapine 300 mg Tablet2.44USD tablet
Mylan-Quetiapine 300 mg Tablet2.44USD tablet
Novo-Quetiapine 300 mg Tablet2.44USD tablet
Pms-Quetiapine 300 mg Tablet2.44USD tablet
Ratio-Quetiapine 300 mg Tablet2.44USD tablet
Sandoz Quetiapine 300 mg Tablet2.44USD tablet
Apo-Quetiapine 200 mg Tablet1.67USD tablet
Co Quetiapine 200 mg Tablet1.67USD tablet
Jamp-Quetiapine 200 mg Tablet1.67USD tablet
Mylan-Quetiapine 200 mg Tablet1.67USD tablet
Novo-Quetiapine 200 mg Tablet1.67USD tablet
Pms-Quetiapine 200 mg Tablet1.67USD tablet
Ratio-Quetiapine 200 mg Tablet1.67USD tablet
Sandoz Quetiapine 200 mg Tablet1.67USD tablet
Seroquel 100 mg Tablet1.48USD tablet
Novo-Quetiapine 150 mg Tablet1.42USD tablet
Apo-Quetiapine 100 mg Tablet0.83USD tablet
Co Quetiapine 100 mg Tablet0.83USD tablet
Jamp-Quetiapine 100 mg Tablet0.83USD tablet
Mylan-Quetiapine 100 mg Tablet0.83USD tablet
Novo-Quetiapine 100 mg Tablet0.83USD tablet
Pms-Quetiapine 100 mg Tablet0.83USD tablet
Ratio-Quetiapine 100 mg Tablet0.83USD tablet
Sandoz Quetiapine 100 mg Tablet0.83USD tablet
Seroquel 25 mg Tablet0.56USD tablet
Apo-Quetiapine 25 mg Tablet0.31USD tablet
Co Quetiapine 25 mg Tablet0.31USD tablet
Jamp-Quetiapine 25 mg Tablet0.31USD tablet
Mylan-Quetiapine 25 mg Tablet0.31USD tablet
Novo-Quetiapine 25 mg Tablet0.31USD tablet
Pms-Quetiapine 25 mg Tablet0.31USD tablet
Ratio-Quetiapine 25 mg Tablet0.31USD tablet
Sandoz Quetiapine 25 mg Tablet0.31USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US4879288No1994-09-262011-09-26Us
CA2251944No2007-04-102017-05-27Canada
US5948437Yes1997-11-282017-11-28Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubilityModerateNot Available
logP2.8Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0403 mg/mLALOGPS
logP2.93ALOGPS
logP2.81ChemAxon
logS-4ALOGPS
pKa (Strongest Acidic)15.12ChemAxon
pKa (Strongest Basic)7.06ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area48.3 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity114.09 m3·mol-1ChemAxon
Polarizability42.78 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9155
Blood Brain Barrier+0.9906
Caco-2 permeable-0.6037
P-glycoprotein substrateSubstrate0.8424
P-glycoprotein inhibitor IInhibitor0.9117
P-glycoprotein inhibitor IIInhibitor0.9325
Renal organic cation transporterInhibitor0.5554
CYP450 2C9 substrateNon-substrate0.6438
CYP450 2D6 substrateSubstrate0.8919
CYP450 3A4 substrateNon-substrate0.6049
CYP450 1A2 substrateInhibitor0.5744
CYP450 2C9 inhibitorNon-inhibitor0.6305
CYP450 2D6 inhibitorInhibitor0.588
CYP450 2C19 inhibitorNon-inhibitor0.7033
CYP450 3A4 inhibitorInhibitor0.7961
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.5375
Ames testNon AMES toxic0.7479
CarcinogenicityNon-carcinogens0.869
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.6537 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9483
hERG inhibition (predictor II)Inhibitor0.8684
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
MS/MS Spectrum - DI-ESI-qTof , NegativeLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-001i-0089000000-b7b1c7d0bf6bb604c5cb
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0uk9-1390000000-ce855b6e08dee583681b

Taxonomy

Description
This compound belongs to the class of organic compounds known as dibenzothiazepines. These are compounds containing a dibenzothiazepine moiety, which consists of two benzene connected by a thiazepine ring.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Benzothiazepines
Sub Class
Dibenzothiazepines
Direct Parent
Dibenzothiazepines
Alternative Parents
Diarylthioethers / N-alkylpiperazines / Imidolactams / Benzenoids / Trialkylamines / Propargyl-type 1,3-dipolar organic compounds / Dialkyl ethers / Carboxamidines / Azacyclic compounds / Primary alcohols
show 2 more
Substituents
Dibenzothiazepine / Diarylthioether / Aryl thioether / N-alkylpiperazine / 1,4-diazinane / Piperazine / Benzenoid / Imidolactam / Tertiary amine / Tertiary aliphatic amine
show 18 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
N-arylpiperazine, N-alkylpiperazine, dibenzothiazepine (CHEBI:8707)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Virus receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodop...
Gene Name
HTR2A
Uniprot ID
P28223
Uniprot Name
5-hydroxytryptamine receptor 2A
Molecular Weight
52602.58 Da
References
  1. Goldstein JM: Quetiapine fumarate (Seroquel): a new atypical antipsychotic. Drugs Today (Barc). 1999 Mar;35(3):193-210. [PubMed:12973385]
  2. McIntyre RS, Soczynska JK, Woldeyohannes HO, Alsuwaidan M, Konarski JZ: A preclinical and clinical rationale for quetiapine in mood syndromes. Expert Opin Pharmacother. 2007 Jun;8(9):1211-9. [PubMed:17563257]
  3. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [PubMed:11132243]
  4. Yatham LN, Goldstein JM, Vieta E, Bowden CL, Grunze H, Post RM, Suppes T, Calabrese JR: Atypical antipsychotics in bipolar depression: potential mechanisms of action. J Clin Psychiatry. 2005;66 Suppl 5:40-8. [PubMed:16038601]
  5. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Details
2. D(2) dopamine receptor
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Potassium channel regulator activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name
DRD2
Uniprot ID
P14416
Uniprot Name
D(2) dopamine receptor
Molecular Weight
50618.91 Da
References
  1. Kapur S, Zipursky R, Jones C, Shammi CS, Remington G, Seeman P: A positron emission tomography study of quetiapine in schizophrenia: a preliminary finding of an antipsychotic effect with only transiently high dopamine D2 receptor occupancy. Arch Gen Psychiatry. 2000 Jun;57(6):553-9. [PubMed:10839333]
  2. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [PubMed:11132243]
  3. Seeman P: Atypical antipsychotics: mechanism of action. Can J Psychiatry. 2002 Feb;47(1):27-38. [PubMed:11873706]
  4. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
  5. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers...
Gene Name
HTR1A
Uniprot ID
P08908
Uniprot Name
5-hydroxytryptamine receptor 1A
Molecular Weight
46106.335 Da
References
  1. Ichikawa J, Li Z, Dai J, Meltzer HY: Atypical antipsychotic drugs, quetiapine, iloperidone, and melperone, preferentially increase dopamine and acetylcholine release in rat medial prefrontal cortex: role of 5-HT1A receptor agonism. Brain Res. 2002 Nov 29;956(2):349-57. [PubMed:12445705]
  2. McIntyre RS, Soczynska JK, Woldeyohannes HO, Alsuwaidan M, Konarski JZ: A preclinical and clinical rationale for quetiapine in mood syndromes. Expert Opin Pharmacother. 2007 Jun;8(9):1211-9. [PubMed:17563257]
  3. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [PubMed:11132243]
  4. Wood MD, Scott C, Clarke K, Cato KJ, Patel N, Heath J, Worby A, Gordon L, Campbell L, Riley G, Davies CH, Gribble A, Jones DN: Pharmacological profile of antipsychotics at monoamine receptors: atypicality beyond 5-HT2A receptor blockade. CNS Neurol Disord Drug Targets. 2006 Aug;5(4):445-52. [PubMed:16918396]
  5. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Other/unknown
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive subst...
Gene Name
HTR1B
Uniprot ID
P28222
Uniprot Name
5-hydroxytryptamine receptor 1B
Molecular Weight
43567.535 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Other/unknown
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive subst...
Gene Name
HTR1D
Uniprot ID
P28221
Uniprot Name
5-hydroxytryptamine receptor 1D
Molecular Weight
41906.38 Da
References
  1. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [PubMed:11132243]
  2. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Other/unknown
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various alkaloids and psychoactive substances. Ligand binding causes a conformation change that trig...
Gene Name
HTR1E
Uniprot ID
P28566
Uniprot Name
5-hydroxytryptamine receptor 1E
Molecular Weight
41681.57 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-...
Gene Name
HTR2C
Uniprot ID
P28335
Uniprot Name
5-hydroxytryptamine receptor 2C
Molecular Weight
51820.705 Da
References
  1. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [PubMed:11132243]
  2. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Other/unknown
General Function
Voltage-gated potassium channel activity
Specific Function
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gate...
Gene Name
HTR3A
Uniprot ID
P46098
Uniprot Name
5-hydroxytryptamine receptor 3A
Molecular Weight
55279.835 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Other/unknown
General Function
Serotonin receptor activity
Specific Function
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor ...
Gene Name
HTR6
Uniprot ID
P50406
Uniprot Name
5-hydroxytryptamine receptor 6
Molecular Weight
46953.625 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Serotonin receptor activity
Specific Function
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor ...
Gene Name
HTR7
Uniprot ID
P34969
Uniprot Name
5-hydroxytryptamine receptor 7
Molecular Weight
53554.43 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Details
11. D(1A) dopamine receptor
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
G-protein coupled amine receptor activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
Gene Name
DRD1
Uniprot ID
P21728
Uniprot Name
D(1A) dopamine receptor
Molecular Weight
49292.765 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Details
12. D(1B) dopamine receptor
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
G-protein coupled amine receptor activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
Gene Name
DRD5
Uniprot ID
P21918
Uniprot Name
D(1B) dopamine receptor
Molecular Weight
52950.5 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Details
13. D(3) dopamine receptor
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
G-protein coupled amine receptor activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.
Gene Name
DRD3
Uniprot ID
P35462
Uniprot Name
D(3) dopamine receptor
Molecular Weight
44224.335 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Details
14. D(4) dopamine receptor
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Sh3 domain binding
Specific Function
Dopamine receptor responsible for neuronal signaling in the mesolimbic system of the brain, an area of the brain that regulates emotion and complex behavior. Its activity is mediated by G proteins ...
Gene Name
DRD4
Uniprot ID
P21917
Uniprot Name
D(4) dopamine receptor
Molecular Weight
48359.86 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Details
15. Histamine H1 receptor
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Histamine receptor activity
Specific Function
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamin...
Gene Name
HRH1
Uniprot ID
P35367
Uniprot Name
Histamine H1 receptor
Molecular Weight
55783.61 Da
References
  1. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [PubMed:11132243]
  2. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Protein heterodimerization activity
Specific Function
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
Gene Name
ADRA1A
Uniprot ID
P35348
Uniprot Name
Alpha-1A adrenergic receptor
Molecular Weight
51486.005 Da
References
  1. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [PubMed:11132243]
  2. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Protein heterodimerization activity
Specific Function
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
Gene Name
ADRA1B
Uniprot ID
P35368
Uniprot Name
Alpha-1B adrenergic receptor
Molecular Weight
56835.375 Da
References
  1. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [PubMed:11132243]
  2. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Alpha1-adrenergic receptor activity
Specific Function
This alpha-adrenergic receptor mediates its effect through the influx of extracellular calcium.
Gene Name
ADRA1D
Uniprot ID
P25100
Uniprot Name
Alpha-1D adrenergic receptor
Molecular Weight
60462.205 Da
References
  1. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [PubMed:11132243]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Thioesterase binding
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazo...
Gene Name
ADRA2A
Uniprot ID
P08913
Uniprot Name
Alpha-2A adrenergic receptor
Molecular Weight
48956.275 Da
References
  1. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [PubMed:11132243]
  2. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Epinephrine binding
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine...
Gene Name
ADRA2B
Uniprot ID
P18089
Uniprot Name
Alpha-2B adrenergic receptor
Molecular Weight
49565.8 Da
References
  1. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [PubMed:11132243]
  2. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Protein homodimerization activity
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins.
Gene Name
ADRA2C
Uniprot ID
P18825
Uniprot Name
Alpha-2C adrenergic receptor
Molecular Weight
49521.585 Da
References
  1. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [PubMed:11132243]
  2. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Phosphatidylinositol phospholipase c activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM1
Uniprot ID
P11229
Uniprot Name
Muscarinic acetylcholine receptor M1
Molecular Weight
51420.375 Da
References
  1. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [PubMed:11132243]
  2. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
G-protein coupled acetylcholine receptor activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM2
Uniprot ID
P08172
Uniprot Name
Muscarinic acetylcholine receptor M2
Molecular Weight
51714.605 Da
References
  1. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [PubMed:11132243]
  2. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Receptor activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM3
Uniprot ID
P20309
Uniprot Name
Muscarinic acetylcholine receptor M3
Molecular Weight
66127.445 Da
References
  1. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [PubMed:11132243]
  2. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Guanyl-nucleotide exchange factor activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM4
Uniprot ID
P08173
Uniprot Name
Muscarinic acetylcholine receptor M4
Molecular Weight
53048.65 Da
References
  1. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [PubMed:11132243]
  2. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Phosphatidylinositol phospholipase c activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM5
Uniprot ID
P08912
Uniprot Name
Muscarinic acetylcholine receptor M5
Molecular Weight
60073.205 Da
References
  1. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [PubMed:11132243]
  2. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A7
Uniprot ID
P24462
Uniprot Name
Cytochrome P450 3A7
Molecular Weight
57525.03 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Urichuk L, Prior TI, Dursun S, Baker G: Metabolism of atypical antipsychotics: involvement of cytochrome p450 enzymes and relevance for drug-drug interactions. Curr Drug Metab. 2008 Jun;9(5):410-8. [PubMed:18537577]
  2. DeVane CL, Nemeroff CB: Clinical pharmacokinetics of quetiapine: an atypical antipsychotic. Clin Pharmacokinet. 2001;40(7):509-22. [PubMed:11510628]
  3. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  4. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  2. Lin SN, Chang Y, Moody DE, Foltz RL: A liquid chromatographic-electrospray-tandem mass spectrometric method for quantitation of quetiapine in human plasma and liver microsomes: application to study in vitro metabolism. J Anal Toxicol. 2004 Sep;28(6):443-8. [PubMed:15516294]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Boulton DW, DeVane CL, Liston HL, Markowitz JS: In vitro P-glycoprotein affinity for atypical and conventional antipsychotics. Life Sci. 2002 May 31;71(2):163-9. [PubMed:12031686]

Drug created on June 13, 2005 07:24 / Updated on October 21, 2018 20:30