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Identification
- Summary
Paliperidone is an atypical antipsychotic used in the treatment of schizophrenia and other schizoaffective or delusional disorders.
- Brand Names
- Invega, Invega Hafyera, Xeplion
- Generic Name
- Paliperidone
- DrugBank Accession Number
- DB01267
- Background
Paliperidone is the primary active metabolite of risperidone. The mechanism of action is unknown but it is likely to act via a similar pathway to risperidone. It has been proposed that the drug's therapeutic activity in schizophrenia is mediated through a combination of central dopamine Type 2 (D2) and serotonin Type 2 (5HT2A) receptor antagonism. Paliperidone is also active as an antagonist at alpha 1 and alpha 2 adrenergic receptors and H1 histaminergic receptors, which may explain some of the other effects of the drug. Paliperidone was approved by the FDA for treatment of schizophrenia on December 20, 2006. It is available as an extended-release tablet, a once-monthly intramuscular injection, an every-three-month intramuscular injection, and a twice-yearly gluteal injection.3,5,4,6
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Paliperidone (DB01267)
- Weight
- Average: 426.4839
Monoisotopic: 426.206718955 - Chemical Formula
- C23H27FN4O3
- Synonyms
- 9-hydroxyrisperidone
- Paliperidona
- Paliperidone
- External IDs
- R-76477
- RO-76477
- RO76477
Pharmacology
- Indication
As an oral extended-release tablet and a once-monthly extended-release suspension for intramuscular injection, paliperidone is indicated for the treatment of adults and adolescents with schizophrenia and in the treatment of schizoaffective disorder in combination with antidepressants or mood stabilizers.3,5 Paliperidone is also available in both an every-three-month and twice-yearly extended-release suspension for intramuscular injection for the treatment of schizophrenia.4,6
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Adjunct therapy in treatment of Schizoaffective disorders •••••••••••• ••••••••• Adjunct therapy in treatment of Schizoaffective disorders •••••••••••• ••••••••• Adjunct therapy in treatment of Schizoaffective disorders •••••••••••• ••••••• •••••••• ••••••• Treatment of Schizoaffective disorders •••••••••••• ••••••• •••••••• ••••••• Treatment of Schizophrenia •••••••••••• ••••• ••••• ••••••••• •••• ••••••••••••••••• •••••••••••• ••••••••• •••••••••• ••••••••••• •••••••• ••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Paliperidone is an atypical antipsychotic developed by Janssen Pharmaceutica. Chemically, paliperidone is primary active metabolite of the older antipsychotic risperidone (paliperidone is 9-hydroxyrisperidone). The mechanism of action is unknown but it is likely to act via a similar pathway to risperidone.
- Mechanism of action
Paliperidone is the major active metabolite of risperidone. The mechanism of action of paliperidone, as with other drugs having efficacy in schizophrenia, is unknown, but it has been proposed that the drug's therapeutic activity in schizophrenia is mediated through a combination of central dopamine Type 2 (D2) and serotonin Type 2 (5HT2A) receptor antagonism.
Target Actions Organism A5-hydroxytryptamine receptor 2A antagonistHumans AD(2) dopamine receptor antagonistHumans AD(4) dopamine receptor antagonistHumans AD(3) dopamine receptor antagonistHumans A5-hydroxytryptamine receptor 2C antagonistHumans UHistamine H1 receptor antagonistHumans UAlpha-1A adrenergic receptor antagonistHumans UAlpha-1B adrenergic receptor antagonistHumans U5-hydroxytryptamine receptor 1D antagonistHumans UAlpha-2A adrenergic receptor antagonistHumans UAlpha-2B adrenergic receptor antagonistHumans UAlpha-2C adrenergic receptor agonistHumans U5-hydroxytryptamine receptor 1A antagonistHumans UD(1A) dopamine receptor antagonistHumans U5-hydroxytryptamine receptor 7 Not Available Humans - Absorption
The absolute oral bioavailability of paliperidone following paliperidone administration is 28%.
- Volume of distribution
- 487 L
- Protein binding
The plasma protein binding of racemic paliperidone is 74%.
- Metabolism
Although in vitro studies suggested a role for CYP2D6 and CYP3A4 in the metabolism of paliperidone, in vivo results indicate that these isozymes play a limited role in the overall elimination of paliperidone. Four primary metabolic pathways have been identified in vivo, none of which could be shown to account for more than 10% of the dose: dealkylation, hydroxylation, dehydrogenation, and benzisoxazole scission. Paliperidone does not undergo extensive metabolism and a significant portion of its metabolism occurs in the kidneys.
- Route of elimination
One week following administration of a single oral dose of 1 mg immediate-release 14C-paliperidone to 5 healthy volunteers, 59% (range 51% – 67%) of the dose was excreted unchanged into urine, 32% (26% – 41%) of the dose was recovered as metabolites, and 6% – 12% of the dose was not recovered.
- Half-life
The terminal elimination half-life of paliperidone is approximately 23 hours.
- Clearance
Not Available
- Adverse Effects
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The possibility of obtundation, seizures, or dystonic reaction of the head and neck following overdose may create a risk of aspiration with induced emesis.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine The risk or severity of CNS depression can be increased when Paliperidone is combined with 1,2-Benzodiazepine. Abacavir Abacavir may decrease the excretion rate of Paliperidone which could result in a higher serum level. Abametapir The serum concentration of Paliperidone can be increased when it is combined with Abametapir. Abatacept The metabolism of Paliperidone can be increased when combined with Abatacept. Abemaciclib The serum concentration of Abemaciclib can be increased when it is combined with Paliperidone. - Food Interactions
- Avoid alcohol.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Paliperidone palmitate R8P8USM8FR 199739-10-1 VOMKSBFLAZZBOW-UHFFFAOYSA-N - Product Images
- International/Other Brands
- Invega Hafyera (Janssen Pharmaceutical Companies of Johnson & Johnson)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Byannli 1000 mg Intramuscular Janssen Cilag International Nv 2022-05-04 Not applicable EU 
Byannli 700 mg Intramuscular Janssen Cilag International Nv 2022-05-04 Not applicable EU Invega Tablet, extended release 6 mg Oral Janssen Cilag International Nv 2016-09-08 Not applicable EU Invega Tablet, extended release 12 mg Oral Janssen Cilag International Nv 2016-09-08 Not applicable EU Invega Tablet, extended release 12 mg Oral Janssen Cilag International Nv 2016-09-08 Not applicable EU - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Mar-paliperidone Tablet, extended release 3 mg Oral Marcan Pharmaceuticals Inc 2021-06-29 Not applicable Canada 
Mar-paliperidone Tablet, extended release 9 mg Oral Marcan Pharmaceuticals Inc Not applicable Not applicable Canada Mar-paliperidone Tablet, extended release 6 mg Oral Marcan Pharmaceuticals Inc 2021-06-29 Not applicable Canada Mylan-paliperidone Tablet, extended release 6 mg Oral Mylan Pharmaceuticals Inc. Not applicable Not applicable Canada Mylan-paliperidone Tablet, extended release 3 mg Oral Mylan Pharmaceuticals Inc. Not applicable Not applicable Canada - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image XEPLION Paliperidone (150 MG/1ml) + Paliperidone (100 MG/1ml) Injection, solution Intramuscular Janssen Cilag International Nv 2014-07-08 Not applicable Italy 
XEPLION Paliperidone (150 MG/1ml) + Paliperidone (100 MG/1ml) Injection, solution Intramuscular Janssen Cilag International Nv 2014-07-08 Not applicable Italy
Categories
- ATC Codes
- N05AX13 — Paliperidone
- Drug Categories
- Adrenergic alpha-1 Receptor Antagonists
- Adrenergic alpha-Antagonists
- Adrenergic Antagonists
- Agents that produce hypertension
- Antidepressive Agents
- Antipsychotic Agents
- Antipsychotic Agents (Second Generation [Atypical])
- Central Nervous System Agents
- Central Nervous System Depressants
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A5 Substrates
- Cytochrome P-450 Substrates
- Dopamine Agents
- Dopamine Antagonists
- Dopamine D2 Receptor Antagonists
- Drugs that are Mainly Renally Excreted
- Highest Risk QTc-Prolonging Agents
- Hyperglycemia-Associated Agents
- Isoxazoles
- Nervous System
- Neurotoxic agents
- Neurotransmitter Agents
- P-glycoprotein inhibitors
- P-glycoprotein substrates
- Psycholeptics
- Psychotropic Drugs
- Pyrimidines
- QTc Prolonging Agents
- Serotonergic Drugs Shown to Increase Risk of Serotonin Syndrome
- Serotonin 5-HT1 Receptor Antagonists
- Serotonin 5-HT1A Receptor Antagonists
- Serotonin 5-HT1D Receptor Antagonists
- Serotonin 5-HT2 Receptor Antagonists
- Serotonin 5-HT2A Receptor Antagonists
- Serotonin 5-HT2C Receptor Antagonists
- Serotonin Agents
- Serotonin Receptor Antagonists
- Tranquilizing Agents
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as pyridopyrimidines. These are compounds containing a pyridopyrimidine, which consists of a pyridine fused to a pyrimidine. Pyridine is 6-membered ring consisting of five carbon atoms and a nitrogen atom. Pyrimidine is a 6-membered ring consisting of four carbon atoms and two nitrogen centers at the 1- and 3- ring positions.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Pyridopyrimidines
- Sub Class
- Not Available
- Direct Parent
- Pyridopyrimidines
- Alternative Parents
- Benzisoxazoles / Aralkylamines / Pyrimidones / Aryl fluorides / Benzenoids / Piperidines / Pyridines and derivatives / Isoxazoles / Heteroaromatic compounds / Lactams show 8 more
- Substituents
- Alcohol / Amine / Aralkylamine / Aromatic heteropolycyclic compound / Aryl fluoride / Aryl halide / Azacycle / Azole / Benzenoid / Benzisoxazole show 21 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- organofluorine compound, secondary alcohol, pyridopyrimidine, 1,2-benzoxazoles, heteroarylpiperidine (CHEBI:83804)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 838F01T721
- CAS number
- 144598-75-4
- InChI Key
- PMXMIIMHBWHSKN-UHFFFAOYSA-N
- InChI
- InChI=1S/C23H27FN4O3/c1-14-17(23(30)28-9-2-3-19(29)22(28)25-14)8-12-27-10-6-15(7-11-27)21-18-5-4-16(24)13-20(18)31-26-21/h4-5,13,15,19,29H,2-3,6-12H2,1H3
- IUPAC Name
- 3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-9-hydroxy-2-methyl-4H,6H,7H,8H,9H-pyrido[1,2-a]pyrimidin-4-one
- SMILES
- CC1=C(CCN2CCC(CC2)C2=NOC3=C2C=CC(F)=C3)C(=O)N2CCCC(O)C2=N1
References
- Synthesis Reference
Santiago Ini, Naama Chasid, Kobi Chen, Osnat Porter-Kleks, "Pure paliperidone and processes for preparing thereof." U.S. Patent US20080171876, issued July 17, 2008.
US20080171876- General References
- Jones MP, Nicholl D, Trakas K: Efficacy and tolerability of paliperidone ER and other oral atypical antipsychotics in schizophrenia. Int J Clin Pharmacol Ther. 2010 Jun;48(6):383-99. [Article]
- 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. [Article]
- FDA Approved Drug Products: Invega (paliperidone) extended-release tablets [Link]
- FDA Approved Drug Products: Invega Trinza (paliperidone palmitate) extended-release suspension for intramuscular injection [Link]
- FDA Approved Drug Products: Invega Sustenna (paliperidone palmitate) extended-release suspension for intramuscular injection [Link]
- FDA Approved Drug Products: Invega Hafyera (paliperidone palmitate) extended-release suspension for gluteal intramuscular injection [Link]
- External Links
- Human Metabolome Database
- HMDB0015396
- KEGG Drug
- D05339
- PubChem Compound
- 115237
- PubChem Substance
- 46506296
- ChemSpider
- 103109
- BindingDB
- 50252513
- 679314
- ChEBI
- 83804
- ChEMBL
- CHEMBL1621
- Therapeutic Targets Database
- DAP000847
- PharmGKB
- PA163518919
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Paliperidone
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Completed Not Available Bipolar Disorder (BD) 1 somestatus stop reason just information to hide Not Available Completed Not Available Bipolar Disorder (BD) / Psychosis / Schizoaffective Disorders / Schizophrenia / Type 2 Diabetes Mellitus 1 somestatus stop reason just information to hide Not Available Completed Not Available Bipolar Disorder (BD) / Schizophrenia 1 somestatus stop reason just information to hide Not Available Completed Not Available Schizophrenia 6 somestatus stop reason just information to hide Not Available Completed Treatment Methamphetamine Dependence 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Alza Corp.
- Interquim SA
- Janssen-Ortho Inc.
- Murfreesboro Pharmaceutical Nursing Supply
- Ortho Mcneil Janssen Pharmaceutical Inc.
- Physician Partners Ltd.
- Quality Care
- Rebel Distributors Corp.
- Dosage Forms
Form Route Strength Injection, suspension Intramuscular 100 MG Injection, suspension Intramuscular 1000 mg Injection, suspension Intramuscular 150 MG/100MG Injection, suspension Intramuscular 150 MG Injection, suspension Intramuscular 25 MG Injection, suspension Intramuscular 50 MG Injection, suspension Intramuscular 700 mg Injection, suspension Intramuscular 75 MG Tablet 3 MG Tablet 6 MG Tablet 9 MG Suspension Intramuscular 312.00 mg Suspension Intramuscular 78.000 mg Tablet, extended release Oral 1.5 mg Tablet, extended release Oral 12 mg Tablet, extended release Oral 3 mg/1 Tablet, extended release Oral 6 mg/1 Injection, suspension, extended release Intramuscular 1092 mg/3.5mL Injection, suspension, extended release Intramuscular 1560 mg/5mL Injection Intramuscular 100 MG/ML Injection Intramuscular 117 mg/0.75mL Injection Intramuscular 150 MG/1.5ML Injection Intramuscular 156 mg/1mL Injection Intramuscular 234 mg/1.5mL Injection Intramuscular 25 MG/0.25ML Injection Intramuscular 39 mg/0.25mL Injection Intramuscular 50 MG/0.5ML Injection Intramuscular 75 MG/0.75ML Injection Intramuscular 78 mg/0.5mL Suspension, extended release Intramuscular 100 mg / 1 mL Suspension, extended release Intramuscular 150 mg / 1.5 mL Suspension, extended release Intramuscular 156 mg/1ml Suspension, extended release Intramuscular 25 mg / 0.25 mL Suspension, extended release Intramuscular 50 mg / 0.5 mL Suspension, extended release Intramuscular 75 mg / 0.75 mL Suspension Intramuscular 150 mg Suspension Intramuscular 50 mg Injection, suspension, extended release Intramuscular 100 mg/1ml Injection, suspension, extended release Intramuscular 150 mg/1.5ml Injection, suspension, extended release Intramuscular 25 mg/0.25ml Injection, suspension, extended release Intramuscular 50 mg/0.5ml Injection, suspension, extended release Intramuscular 75 mg/0.75ml Suspension Intramuscular 25 mg Suspension Intramuscular 100 mg Injection Intramuscular 350 mg/1.75ml Injection Intramuscular 525 mg/2.625ml Injection, suspension, extended release Intramuscular 273 mg/0.88mL Injection, suspension, extended release Intramuscular 312 mg/1ml Injection, suspension, extended release Intramuscular 410 mg/1.32mL Injection, suspension, extended release Intramuscular 546 mg/1.75mL Injection, suspension, extended release Intramuscular 819 mg/2.63mL Suspension, extended release Intramuscular 175 mg / 0.875 mL Suspension, extended release Intramuscular 263 mg / 1.315 mL Suspension, extended release Intramuscular 350 mg / 1.75 mL Suspension, extended release Intramuscular 525 mg / 2.625 mL Suspension Intramuscular 175 mg/0.875mL Suspension Intramuscular 263 mg/1.315mL Suspension Intramuscular 350 mg/1.750mL Suspension Intramuscular 525 mg/2.625mL Injection, suspension, extended release Intramuscular 175 mg/0.875ml Injection, suspension, extended release Intramuscular 263 mg/1.315ml Injection, suspension, extended release Intramuscular 350 mg/1.75ml Injection, suspension, extended release Intramuscular 525 mg/2.625ml Suspension Intramuscular 200 mg Suspension Intramuscular 75 mg Injection, suspension Parenteral 100 mg Injection, suspension Parenteral 150 mg Injection, suspension Parenteral 25 mg Injection, suspension Parenteral 50 mg Injection, suspension Parenteral 75 mg Tablet, extended release Oral 1.5 mg/1 Tablet, extended release Oral 9 mg/1 Tablet, film coated, extended release Oral 1.5 mg/1 Tablet, film coated, extended release Oral 3 mg/1 Tablet, film coated, extended release Oral 6 mg/1 Tablet, film coated, extended release Oral 9 mg/1 Injection, suspension, extended release; kit Intramuscular 117 mg/0.75mL Injection, suspension, extended release; kit Intramuscular 156 mg/1mL Injection, suspension, extended release; kit Intramuscular 234 mg/1.5mL Injection, suspension, extended release; kit Intramuscular 39 mg/0.25mL Injection, suspension, extended release; kit Intramuscular 78 mg/0.5mL Injection, suspension 100 MG Injection, suspension 150 MG Injection, suspension 25 MG Injection, suspension 50 MG Injection, suspension 75 MG Injection, suspension Intramuscular; Parenteral 150 MG/100MG Injection, suspension Intramuscular; Parenteral 175 MG Injection, suspension Intramuscular; Parenteral 263 MG Injection, suspension Intramuscular; Parenteral 350 MG Injection, suspension Intramuscular; Parenteral 525 MG Injection, suspension, extended release Intramuscular 175 mg Injection, suspension, extended release Intramuscular 263 mg Injection, suspension, extended release Intramuscular 350 mg Injection, suspension, extended release Intramuscular 525 mg Injection, solution Intramuscular Injection, suspension Intramuscular; Parenteral 100 MG Injection, suspension Intramuscular; Parenteral 150 MG Injection, suspension Intramuscular; Parenteral 25 MG Injection, suspension Intramuscular; Parenteral 50 MG Injection, suspension Intramuscular; Parenteral 75 MG Injection, suspension, extended release Intramuscular 100 mg Injection, suspension, extended release Intramuscular 150 mg Injection, suspension, extended release Intramuscular 25 mg Injection, suspension, extended release Intramuscular 50 mg Injection, suspension, extended release Intramuscular 75 mg Injection, suspension, extended release Intramuscular Injection, suspension, extended release Intramuscular 50 mg/0.50ml Tablet, extended release Oral 3 mg Tablet, extended release Oral 6 mg Tablet, extended release Oral 9 mg - Prices
Unit description Cost Unit Invega sustenna 39 mg pref syringe 296.45USD syringe Invega er 6 mg tablet 28.62USD tablet Invega er 9 mg tablet 23.59USD tablet Invega er 3 mg tablet 23.09USD tablet Invega er 1.5 mg tablet 15.72USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US5254556 No 1993-10-19 2010-10-27 US 
CA2494234 No 2009-10-27 2023-07-28 Canada CA2000786 No 1999-01-26 2009-10-16 Canada US6077843 Yes 2000-06-20 2017-11-12 US US6555544 Yes 2003-04-29 2019-05-10 US US9439906 No 2016-09-13 2031-01-26 US US10143693 No 2018-12-04 2036-04-05 US US11304951 No 2021-05-07 2041-05-07 US US11324751 No 2021-05-07 2041-05-07 US US11666697 No 2021-11-24 2041-11-24 US US11666573 No 2019-09-24 2039-09-24 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility Practically insoluble in water Not Available logP 1.8 Not Available - Predicted Properties
Property Value Source Water Solubility 0.297 mg/mL ALOGPS logP 2.3 ALOGPS logP 1.76 Chemaxon logS -3.2 ALOGPS pKa (Strongest Acidic) 13.74 Chemaxon pKa (Strongest Basic) 8.76 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 82.17 Å2 Chemaxon Rotatable Bond Count 4 Chemaxon Refractivity 116.04 m3·mol-1 Chemaxon Polarizability 45.95 Å3 Chemaxon Number of Rings 5 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 1.0 Blood Brain Barrier + 0.7928 Caco-2 permeable - 0.5496 P-glycoprotein substrate Substrate 0.7449 P-glycoprotein inhibitor I Inhibitor 0.7011 P-glycoprotein inhibitor II Inhibitor 0.8229 Renal organic cation transporter Non-inhibitor 0.6231 CYP450 2C9 substrate Non-substrate 0.7721 CYP450 2D6 substrate Substrate 0.5131 CYP450 3A4 substrate Substrate 0.7154 CYP450 1A2 substrate Non-inhibitor 0.7379 CYP450 2C9 inhibitor Non-inhibitor 0.7395 CYP450 2D6 inhibitor Non-inhibitor 0.5326 CYP450 2C19 inhibitor Non-inhibitor 0.7815 CYP450 3A4 inhibitor Non-inhibitor 0.6468 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.7558 Ames test Non AMES toxic 0.518 Carcinogenicity Non-carcinogens 0.7995 Biodegradation Not ready biodegradable 0.9908 Rat acute toxicity 3.7859 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.8366 hERG inhibition (predictor II) Inhibitor 0.7061
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 199.877896 predictedDarkChem Lite v0.1.0 [M-H]- 201.10147 predictedDeepCCS 1.0 (2019) [M-H]- 199.877896 predictedDarkChem Lite v0.1.0 [M-H]- 201.10147 predictedDeepCCS 1.0 (2019) [M+H]+ 200.325696 predictedDarkChem Lite v0.1.0 [M+H]+ 203.45949 predictedDeepCCS 1.0 (2019) [M+H]+ 200.325696 predictedDarkChem Lite v0.1.0 [M+H]+ 203.45949 predictedDeepCCS 1.0 (2019) [M+Na]+ 199.658696 predictedDarkChem Lite v0.1.0 [M+Na]+ 210.13396 predictedDeepCCS 1.0 (2019) [M+Na]+ 199.658696 predictedDarkChem Lite v0.1.0 [M+Na]+ 210.13396 predictedDeepCCS 1.0 (2019)
Targets
Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin) (PubMed:1330647, PubMed:18703043, PubMed:19057895, PubMed:21645528, PubMed:22300836, PubMed:35084960, PubMed:38552625). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and lysergic acid diethylamide (LSD) (PubMed:28129538, PubMed:35084960). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors (PubMed:28129538, PubMed:35084960). HTR2A is coupled to G(q)/G(11) G alpha proteins and activates phospholipase C-beta, releasing diacylglycerol (DAG) and inositol 1,4,5-trisphosphate (IP3) second messengers that modulate the activity of phosphatidylinositol 3-kinase and promote the release of Ca(2+) ions from intracellular stores, respectively (PubMed:18703043, PubMed:28129538, PubMed:35084960). Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways (PubMed:28129538, PubMed:35084960). Affects neural activity, perception, cognition and mood (PubMed:18297054). Plays a role in the regulation of behavior, including responses to anxiogenic situations and psychoactive substances. Plays a role in intestinal smooth muscle contraction, and may play a role in arterial vasoconstriction (By similarity)
- Specific Function
- 1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding
- Gene Name
- HTR2A
- Uniprot ID
- P28223
- Uniprot Name
- 5-hydroxytryptamine receptor 2A
- Molecular Weight
- 52602.58 Da
References
- Cohen LJ: Risperidone. Pharmacotherapy. 1994 May-Jun;14(3):253-65. [Article]
- He H, Richardson JS: A pharmacological, pharmacokinetic and clinical overview of risperidone, a new antipsychotic that blocks serotonin 5-HT2 and dopamine D2 receptors. Int Clin Psychopharmacol. 1995 Mar;10(1):19-30. [Article]
- Leysen JE, Janssen PM, Megens AA, Schotte A: Risperidone: a novel antipsychotic with balanced serotonin-dopamine antagonism, receptor occupancy profile, and pharmacologic activity. J Clin Psychiatry. 1994 May;55 Suppl:5-12. [Article]
- Megens AA, Awouters FH, Schotte A, Meert TF, Dugovic C, Niemegeers CJ, Leysen JE: Survey on the pharmacodynamics of the new antipsychotic risperidone. Psychopharmacology (Berl). 1994 Feb;114(1):9-23. [Article]
- 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. [Article]
- Yamada Y, Ohno Y, Nakashima Y, Fukuda M, Takayanagi R, Sato H, Tsuchiya F, Sawada Y, Iga T: Prediction and assessment of extrapyramidal side effects induced by risperidone based on dopamine D(2) receptor occupancy. Synapse. 2002 Oct;46(1):32-7. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase (PubMed:21645528). Positively regulates postnatal regression of retinal hyaloid vessels via suppression of VEGFR2/KDR activity, downstream of OPN5 (By similarity)
- Specific Function
- dopamine binding
- Gene Name
- DRD2
- Uniprot ID
- P14416
- Uniprot Name
- D(2) dopamine receptor
- Molecular Weight
- 50618.91 Da
References
- Cohen LJ: Risperidone. Pharmacotherapy. 1994 May-Jun;14(3):253-65. [Article]
- Megens AA, Awouters FH, Schotte A, Meert TF, Dugovic C, Niemegeers CJ, Leysen JE: Survey on the pharmacodynamics of the new antipsychotic risperidone. Psychopharmacology (Berl). 1994 Feb;114(1):9-23. [Article]
- Regenthal R, Kunstler U, Hesse S, Sabri O, Preiss R: D2 dopamine receptor occupancy, risperidone plasma level and extrapyramidal motor symptoms in previously drug-free schizophrenic patients. Int J Clin Pharmacol Ther. 2005 Aug;43(8):370-8. [Article]
- Remington G, Mamo D, Labelle A, Reiss J, Shammi C, Mannaert E, Mann S, Kapur S: A PET study evaluating dopamine D2 receptor occupancy for long-acting injectable risperidone. Am J Psychiatry. 2006 Mar;163(3):396-401. [Article]
- 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. [Article]
- Yamada Y, Ohno Y, Nakashima Y, Fukuda M, Takayanagi R, Sato H, Tsuchiya F, Sawada Y, Iga T: Prediction and assessment of extrapyramidal side effects induced by risperidone based on dopamine D(2) receptor occupancy. Synapse. 2002 Oct;46(1):32-7. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General 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. Activated by dopamine, but also by epinephrine and norepinephrine, and by numerous synthetic agonists and drugs (PubMed:16423344, PubMed:27659709, PubMed:29051383, PubMed:9003072). Agonist binding triggers signaling via G proteins that inhibit adenylyl cyclase (PubMed:16423344, PubMed:27659709, PubMed:29051383, PubMed:7512953, PubMed:7643093). Modulates the circadian rhythm of contrast sensitivity by regulating the rhythmic expression of NPAS2 in the retinal ganglion cells (By similarity)
- Specific Function
- dopamine binding
- Gene Name
- DRD4
- Uniprot ID
- P21917
- Uniprot Name
- D(4) dopamine receptor
- Molecular Weight
- 43900.84 Da
References
- Leysen JE, Janssen PM, Megens AA, Schotte A: Risperidone: a novel antipsychotic with balanced serotonin-dopamine antagonism, receptor occupancy profile, and pharmacologic activity. J Clin Psychiatry. 1994 May;55 Suppl:5-12. [Article]
- Megens AA, Awouters FH, Schotte A, Meert TF, Dugovic C, Niemegeers CJ, Leysen JE: Survey on the pharmacodynamics of the new antipsychotic risperidone. Psychopharmacology (Berl). 1994 Feb;114(1):9-23. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation
- Specific Function
- dopamine neurotransmitter receptor activity, coupled via Gi/Go
- Gene Name
- DRD3
- Uniprot ID
- P35462
- Uniprot Name
- D(3) dopamine receptor
- Molecular Weight
- 44194.315 Da
References
- Leysen JE, Janssen PM, Megens AA, Schotte A: Risperidone: a novel antipsychotic with balanced serotonin-dopamine antagonism, receptor occupancy profile, and pharmacologic activity. J Clin Psychiatry. 1994 May;55 Suppl:5-12. [Article]
- Megens AA, Awouters FH, Schotte A, Meert TF, Dugovic C, Niemegeers CJ, Leysen JE: Survey on the pharmacodynamics of the new antipsychotic risperidone. Psychopharmacology (Berl). 1994 Feb;114(1):9-23. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin) (PubMed:12970106, PubMed:18703043, PubMed:19057895, PubMed:29398112, PubMed:7895773). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-iodophenyl-2-aminopropane (DOI) and lysergic acid diethylamide (LSD) (PubMed:19057895, PubMed:29398112). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors (PubMed:18703043, PubMed:29398112). HTR2C is coupled to G(q)/G(11) G alpha proteins and activates phospholipase C-beta, releasing diacylglycerol (DAG) and inositol 1,4,5-trisphosphate (IP3) second messengers that modulate the activity of phosphatidylinositol 3-kinase and promote the release of Ca(2+) ions from intracellular stores, respectively (PubMed:18703043, PubMed:29398112). Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways (PubMed:29398112). Regulates neuronal activity via the activation of short transient receptor potential calcium channels in the brain, and thereby modulates the activation of pro-opiomelanocortin neurons and the release of CRH that then regulates the release of corticosterone (By similarity). Plays a role in the regulation of appetite and eating behavior, responses to anxiogenic stimuli and stress (By similarity). Plays a role in insulin sensitivity and glucose homeostasis (By similarity)
- Specific Function
- 1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding
- Gene Name
- HTR2C
- Uniprot ID
- P28335
- Uniprot Name
- 5-hydroxytryptamine receptor 2C
- Molecular Weight
- 51804.645 Da
References
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- G-protein-coupled receptor for histamine, a biogenic amine that functions as an immune modulator and a neurotransmitter (PubMed:33828102, PubMed:8280179). Through the H1 receptor, histamine mediates the contraction of smooth muscles and increases capillary permeability due to contraction of terminal venules. Also mediates neurotransmission in the central nervous system and thereby regulates circadian rhythms, emotional and locomotor activities as well as cognitive functions (By similarity)
- Specific Function
- G protein-coupled serotonin receptor activity
- Gene Name
- HRH1
- Uniprot ID
- P35367
- Uniprot Name
- Histamine H1 receptor
- Molecular Weight
- 55783.61 Da
References
- Cicek E, Cicek IE, Uguz F: Bilateral Pretibial Edema Associated with Paliperidone Palmitate Long-acting Injectable: A Case Report. Clin Psychopharmacol Neurosci. 2017 May 31;15(2):184-186. doi: 10.9758/cpn.2017.15.2.184. [Article]
- Gilday E, Nasrallah HA: Clinical pharmacology of paliperidone palmitate a parenteral long-acting formulation for the treatment of schizophrenia. Rev Recent Clin Trials. 2012 Feb;7(1):2-9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General 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) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine(PE)-stimulated ERK signaling in cardiac myocytes
- Specific Function
- alpha1-adrenergic receptor activity
- Gene Name
- ADRA1A
- Uniprot ID
- P35348
- Uniprot Name
- Alpha-1A adrenergic receptor
- Molecular Weight
- 51486.005 Da
References
- Cohen LJ: Risperidone. Pharmacotherapy. 1994 May-Jun;14(3):253-65. [Article]
- Eltze M: In functional experiments, risperidone is selective, not for the B, but for the A subtype of alpha 1-adrenoceptors. Eur J Pharmacol. 1996 Jan 4;295(1):69-73. [Article]
- Fenton C, Scott LJ: Risperidone: a review of its use in the treatment of bipolar mania. CNS Drugs. 2005;19(5):429-44. [Article]
- Keks NA, Culhane C: Risperidone (Risperdal): clinical experience with a new antipsychosis drug. Expert Opin Investig Drugs. 1999 Apr;8(4):443-52. [Article]
- Megens AA, Awouters FH, Schotte A, Meert TF, Dugovic C, Niemegeers CJ, Leysen JE: Survey on the pharmacodynamics of the new antipsychotic risperidone. Psychopharmacology (Berl). 1994 Feb;114(1):9-23. [Article]
- Nourian Z, Mow T, Muftic D, Burek S, Pedersen ML, Matz J, Mulvany MJ: Orthostatic hypotensive effect of antipsychotic drugs in Wistar rats by in vivo and in vitro studies of alpha1-adrenoceptor function. Psychopharmacology (Berl). 2008 Jul;199(1):15-27. doi: 10.1007/s00213-007-1064-9. Epub 2008 Jun 10. [Article]
- 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. [Article]
- Sleight AJ, Koek W, Bigg DC: Binding of antipsychotic drugs at alpha 1A- and alpha 1B-adrenoceptors: risperidone is selective for the alpha 1B-adrenoceptors. Eur J Pharmacol. 1993 Jul 20;238(2-3):407-10. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General 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) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine (PE)-stimulated ERK signaling in cardiac myocytes
- Specific Function
- alpha1-adrenergic receptor activity
- Gene Name
- ADRA1B
- Uniprot ID
- P35368
- Uniprot Name
- Alpha-1B adrenergic receptor
- Molecular Weight
- 56835.375 Da
References
- Cohen LJ: Risperidone. Pharmacotherapy. 1994 May-Jun;14(3):253-65. [Article]
- Eltze M: In functional experiments, risperidone is selective, not for the B, but for the A subtype of alpha 1-adrenoceptors. Eur J Pharmacol. 1996 Jan 4;295(1):69-73. [Article]
- Fenton C, Scott LJ: Risperidone: a review of its use in the treatment of bipolar mania. CNS Drugs. 2005;19(5):429-44. [Article]
- Keks NA, Culhane C: Risperidone (Risperdal): clinical experience with a new antipsychosis drug. Expert Opin Investig Drugs. 1999 Apr;8(4):443-52. [Article]
- Megens AA, Awouters FH, Schotte A, Meert TF, Dugovic C, Niemegeers CJ, Leysen JE: Survey on the pharmacodynamics of the new antipsychotic risperidone. Psychopharmacology (Berl). 1994 Feb;114(1):9-23. [Article]
- Nourian Z, Mow T, Muftic D, Burek S, Pedersen ML, Matz J, Mulvany MJ: Orthostatic hypotensive effect of antipsychotic drugs in Wistar rats by in vivo and in vitro studies of alpha1-adrenoceptor function. Psychopharmacology (Berl). 2008 Jul;199(1):15-27. doi: 10.1007/s00213-007-1064-9. Epub 2008 Jun 10. [Article]
- 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. [Article]
- Sleight AJ, Koek W, Bigg DC: Binding of antipsychotic drugs at alpha 1A- and alpha 1B-adrenoceptors: risperidone is selective for the alpha 1B-adrenoceptors. Eur J Pharmacol. 1993 Jul 20;238(2-3):407-10. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin) (PubMed:10452531, PubMed:1565658, PubMed:1652050, PubMed:33762731). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances (PubMed:10452531, PubMed:1565658, PubMed:1652050, PubMed:33762731). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors, such as adenylate cyclase (PubMed:10452531, PubMed:1565658, PubMed:1652050, PubMed:33762731). HTR1D is coupled to G(i)/G(o) G alpha proteins and mediates inhibitory neurotransmission by inhibiting adenylate cyclase activity (PubMed:33762731). Regulates the release of 5-hydroxytryptamine in the brain, and thereby affects neural activity (PubMed:18476671, PubMed:20945968). May also play a role in regulating the release of other neurotransmitters (PubMed:18476671, PubMed:20945968). May play a role in vasoconstriction (PubMed:18476671, PubMed:20945968)
- Specific Function
- G protein-coupled serotonin receptor activity
- Gene Name
- HTR1D
- Uniprot ID
- P28221
- Uniprot Name
- 5-hydroxytryptamine receptor 1D
- Molecular Weight
- 41906.38 Da
References
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General 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 oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianserine > chlorpromazine = spiperone = prazosin > propanolol > alprenolol = pindolol
- Specific Function
- alpha-1B adrenergic receptor binding
- Gene Name
- ADRA2A
- Uniprot ID
- P08913
- Uniprot Name
- Alpha-2A adrenergic receptor
- Molecular Weight
- 50646.17 Da
References
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General 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 > norepinephrine > epinephrine = oxymetazoline > dopamine > p-tyramine = phenylephrine > serotonin > p-synephrine / p-octopamine. For antagonists, the rank order is yohimbine > chlorpromazine > phentolamine > mianserine > spiperone > prazosin > alprenolol > propanolol > pindolol
- Specific Function
- alpha2-adrenergic receptor activity
- Gene Name
- ADRA2B
- Uniprot ID
- P18089
- Uniprot Name
- Alpha-2B adrenergic receptor
- Molecular Weight
- 49953.145 Da
References
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Agonist
- General Function
- Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins
- Specific Function
- alpha-2A adrenergic receptor binding
- Gene Name
- ADRA2C
- Uniprot ID
- P18825
- Uniprot Name
- Alpha-2C adrenergic receptor
- Molecular Weight
- 49521.585 Da
References
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin) (PubMed:22957663, PubMed:3138543, PubMed:33762731, PubMed:37935376, PubMed:37935377, PubMed:8138923, PubMed:8393041). Also functions as a receptor for various drugs and psychoactive substances (PubMed:22957663, PubMed:3138543, PubMed:33762731, PubMed:38552625, PubMed:8138923, PubMed:8393041). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors, such as adenylate cyclase (PubMed:22957663, PubMed:3138543, PubMed:33762731, PubMed:8138923, PubMed:8393041). HTR1A is coupled to G(i)/G(o) G alpha proteins and mediates inhibitory neurotransmission: signaling inhibits adenylate cyclase activity and activates a phosphatidylinositol-calcium second messenger system that regulates the release of Ca(2+) ions from intracellular stores (PubMed:33762731, PubMed:35610220). Beta-arrestin family members regulate signaling by mediating both receptor desensitization and resensitization processes (PubMed:18476671, PubMed:20363322, PubMed:20945968). Plays a role in the regulation of 5-hydroxytryptamine release and in the regulation of dopamine and 5-hydroxytryptamine metabolism (PubMed:18476671, PubMed:20363322, PubMed:20945968). Plays a role in the regulation of dopamine and 5-hydroxytryptamine levels in the brain, and thereby affects neural activity, mood and behavior (PubMed:18476671, PubMed:20363322, PubMed:20945968). Plays a role in the response to anxiogenic stimuli (PubMed:18476671, PubMed:20363322, PubMed:20945968)
- Specific Function
- G protein-coupled serotonin receptor activity
- Gene Name
- HTR1A
- Uniprot ID
- P08908
- Uniprot Name
- 5-hydroxytryptamine receptor 1A
- Molecular Weight
- 46106.335 Da
References
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase
- Specific Function
- arrestin family protein binding
- Gene Name
- DRD1
- Uniprot ID
- P21728
- Uniprot Name
- D(1A) dopamine receptor
- Molecular Weight
- 49292.765 Da
References
- Leysen JE, Janssen PM, Megens AA, Schotte A: Risperidone: a novel antipsychotic with balanced serotonin-dopamine antagonism, receptor occupancy profile, and pharmacologic activity. J Clin Psychiatry. 1994 May;55 Suppl:5-12. [Article]
- Megens AA, Awouters FH, Schotte A, Meert TF, Dugovic C, Niemegeers CJ, Leysen JE: Survey on the pharmacodynamics of the new antipsychotic risperidone. Psychopharmacology (Berl). 1994 Feb;114(1):9-23. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Curator comments
- Acts as an inactivating antagonist competing for the ligand binding site and producing lasting inactivation of the receptor.
- General Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone and a mitogen (PubMed:35714614, PubMed:8226867). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors (PubMed:35714614, PubMed:8226867). HTR7 is coupled to G(s) G alpha proteins and mediates activation of adenylate cyclase activity (PubMed:35714614)
- Specific Function
- G protein-coupled serotonin receptor activity
- Gene Name
- HTR7
- Uniprot ID
- P34969
- Uniprot Name
- 5-hydroxytryptamine receptor 7
- Molecular Weight
- 53554.43 Da
References
- Knight JA, Smith C, Toohey N, Klein MT, Teitler M: Pharmacological analysis of the novel, rapid, and potent inactivation of the human 5-Hydroxytryptamine7 receptor by risperidone, 9-OH-Risperidone, and other inactivating antagonists. Mol Pharmacol. 2009 Feb;75(2):374-80. doi: 10.1124/mol.108.052084. Epub 2008 Nov 7. [Article]
- Toohey N, Klein MT, Knight J, Smith C, Teitler M: Human 5-HT7 receptor-induced inactivation of forskolin-stimulated adenylate cyclase by risperidone, 9-OH-risperidone and other "inactivating antagonists". Mol Pharmacol. 2009 Sep;76(3):552-9. doi: 10.1124/mol.109.056283. Epub 2009 Jun 9. [Article]
- Teitler M, Toohey N, Knight JA, Klein MT, Smith C: Clozapine and other competitive antagonists reactivate risperidone-inactivated h5-HT7 receptors: radioligand binding and functional evidence for GPCR homodimer protomer interactions. Psychopharmacology (Berl). 2010 Dec;212(4):687-97. doi: 10.1007/s00213-010-2001-x. Epub 2010 Sep 9. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of sterols, steroid hormones, retinoids and fatty acids (PubMed:10681376, PubMed:11093772, PubMed:11555828, PubMed:12865317, PubMed:14559847, PubMed:15373842, PubMed:15764715, PubMed:19965576, PubMed:20702771, PubMed:21490593, PubMed:21576599). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase). Catalyzes the hydroxylation of carbon-hydrogen bonds (PubMed:12865317, PubMed:14559847, PubMed:15373842, PubMed:15764715, PubMed:21490593, PubMed:21576599, PubMed:2732228). Exhibits high catalytic activity for the formation of hydroxyestrogens from estrone (E1) and 17beta-estradiol (E2), namely 2-hydroxy E1 and E2, as well as D-ring hydroxylated E1 and E2 at the C-16 position (PubMed:11555828, PubMed:12865317, PubMed:14559847). Plays a role in the metabolism of androgens, particularly in oxidative deactivation of testosterone (PubMed:15373842, PubMed:15764715, PubMed:22773874, PubMed:2732228). Metabolizes testosterone to less biologically active 2beta- and 6beta-hydroxytestosterones (PubMed:15373842, PubMed:15764715, PubMed:2732228). Contributes to the formation of hydroxycholesterols (oxysterols), particularly A-ring hydroxylated cholesterol at the C-4beta position, and side chain hydroxylated cholesterol at the C-25 position, likely contributing to cholesterol degradation and bile acid biosynthesis (PubMed:21576599). Catalyzes bisallylic hydroxylation of polyunsaturated fatty acids (PUFA) (PubMed:9435160). Catalyzes the epoxidation of double bonds of PUFA with a preference for the last double bond (PubMed:19965576). Metabolizes endocannabinoid arachidonoylethanolamide (anandamide) to 8,9-, 11,12-, and 14,15-epoxyeicosatrienoic acid ethanolamides (EpETrE-EAs), potentially modulating endocannabinoid system signaling (PubMed:20702771). Plays a role in the metabolism of retinoids. Displays high catalytic activity for oxidation of all-trans-retinol to all-trans-retinal, a rate-limiting step for the biosynthesis of all-trans-retinoic acid (atRA) (PubMed:10681376). Further metabolizes atRA toward 4-hydroxyretinoate and may play a role in hepatic atRA clearance (PubMed:11093772). Responsible for oxidative metabolism of xenobiotics. Acts as a 2-exo-monooxygenase for plant lipid 1,8-cineole (eucalyptol) (PubMed:11159812). Metabolizes the majority of the administered drugs. Catalyzes sulfoxidation of the anthelmintics albendazole and fenbendazole (PubMed:10759686). Hydroxylates antimalarial drug quinine (PubMed:8968357). Acts as a 1,4-cineole 2-exo-monooxygenase (PubMed:11695850). Also involved in vitamin D catabolism and calcium homeostasis. Catalyzes the inactivation of the active hormone calcitriol (1-alpha,25-dihydroxyvitamin D(3)) (PubMed:29461981)
- Specific Function
- 1,8-cineole 2-exo-monooxygenase activity
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Gunes A, Spina E, Dahl ML, Scordo MG: ABCB1 polymorphisms influence steady-state plasma levels of 9-hydroxyrisperidone and risperidone active moiety. Ther Drug Monit. 2008 Oct;30(5):628-33. doi: 10.1097/FTD.0b013e3181858ca9. [Article]
- Invega (Paliperidone) FDA label [Link]
- FDA Approved Drug Products: Invega Trinza (paliperidone palmitate) extended-release suspension for intramuscular injection [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of fatty acids, steroids and retinoids (PubMed:18698000, PubMed:19965576, PubMed:20972997, PubMed:21289075, PubMed:21576599). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:18698000, PubMed:19965576, PubMed:20972997, PubMed:21289075, PubMed:21576599). Catalyzes the epoxidation of double bonds of polyunsaturated fatty acids (PUFA) (PubMed:19965576, PubMed:20972997). Metabolizes endocannabinoid arachidonoylethanolamide (anandamide) to 20-hydroxyeicosatetraenoic acid ethanolamide (20-HETE-EA) and 8,9-, 11,12-, and 14,15-epoxyeicosatrienoic acid ethanolamides (EpETrE-EAs), potentially modulating endocannabinoid system signaling (PubMed:18698000, PubMed:21289075). Catalyzes the hydroxylation of carbon-hydrogen bonds. Metabolizes cholesterol toward 25-hydroxycholesterol, a physiological regulator of cellular cholesterol homeostasis (PubMed:21576599). Catalyzes the oxidative transformations of all-trans retinol to all-trans retinal, a precursor for the active form all-trans-retinoic acid (PubMed:10681376). Also involved in the oxidative metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants
- Specific Function
- anandamide 11,12 epoxidase activity
- Gene Name
- CYP2D6
- Uniprot ID
- P10635
- Uniprot Name
- Cytochrome P450 2D6
- Molecular Weight
- 55768.94 Da
References
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of steroid hormones and vitamins (PubMed:10681376, PubMed:11093772, PubMed:12865317, PubMed:2732228). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase). Catalyzes the hydroxylation of carbon-hydrogen bonds (PubMed:10681376, PubMed:11093772, PubMed:12865317, PubMed:2732228). Exhibits high catalytic activity for the formation of catechol estrogens from 17beta-estradiol (E2) and estrone (E1), namely 2-hydroxy E1 and E2 (PubMed:12865317). Catalyzes 6beta-hydroxylation of the steroid hormones testosterone, progesterone, and androstenedione (PubMed:2732228). Catalyzes the oxidative conversion of all-trans-retinol to all-trans-retinal, a rate-limiting step for the biosynthesis of all-trans-retinoic acid (atRA) (PubMed:10681376). Further metabolizes all trans-retinoic acid (atRA) to 4-hydroxyretinoate and may play a role in hepatic atRA clearance (PubMed:11093772). Also involved in the oxidative metabolism of xenobiotics, including calcium channel blocking drug nifedipine and immunosuppressive drug cyclosporine (PubMed:2732228)
- Specific Function
- aromatase activity
- Gene Name
- CYP3A5
- Uniprot ID
- P20815
- Uniprot Name
- Cytochrome P450 3A5
- Molecular Weight
- 57108.065 Da
References
- Yasui-Furukori N, Hidestrand M, Spina E, Facciola G, Scordo MG, Tybring G: Different enantioselective 9-hydroxylation of risperidone by the two human CYP2D6 and CYP3A4 enzymes. Drug Metab Dispos. 2001 Oct;29(10):1263-8. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Translocates drugs and phospholipids across the membrane (PubMed:2897240, PubMed:35970996, PubMed:8898203, PubMed:9038218). Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins (PubMed:8898203). Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells (PubMed:2897240, PubMed:35970996, PubMed:9038218)
- Specific Function
- ABC-type xenobiotic transporter activity
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- ATP-dependent translocase ABCB1
- Molecular Weight
- 141477.255 Da
References
Drug created at May 16, 2007 20:09 / Updated at October 20, 2024 02:07