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IdentificationPharmacologyInteractionsReferencesTrialsEconomicsPropertiesSpectraTaxonomyDarifenacin
Identification
- Name
- Darifenacin
- Accession Number
- DB00496 (APRD00903)
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Description
Darifenacin (Enablex®, Novartis) is a medication used to treat urinary incontinence.
Darifenacin blocks M3 muscarinic acetylcholine receptors, which mediate bladder muscle contractions. This block reduces the urgency to urinate and so it should not be used in people with urinary retention.
It is unknown if M3 receptor selectivity is clinically advantageous in overactive bladder syndrome treatments.
- Structure
Structure for Darifenacin (DB00496)
- Synonyms
- (S)-1-(2-(2,3-dihydro-5-benzofuranyl)ethyl)-α,α-diphenyl-3-pyrrolidineacetamide
- Darifenacin
- Darifenacina
- Darifénacine
- Darifenacinum
- External IDs
- UK 88525 / UK 88525-04
- Product Ingredients
Ingredient UNII CAS InChI Key Darifenacin hydrobromide CR02EYQ8GV 133099-07-7 UQAVIASOPREUIT-VQIWEWKSSA-N - Product Images
- Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Unlock Additional DataDarifenacin Tablet, extended release 15 mg/1 Oral Actavis Pharma, Inc. 2016-03-15 Not applicable US 
Darifenacin Tablet, extended release 7.5 mg/1 Oral Actavis Pharma, Inc. 2016-03-15 Not applicable US Enablex Tablet, extended release 7.5 mg/1 Oral Physicians Total Care, Inc. 2006-11-06 Not applicable US Enablex Tablet, extended release 7.5 mg/1 Oral Allergan, Inc. 2004-12-22 Not applicable US 
Enablex Tablet, extended release 15 mg Oral Searchlight Pharma Inc 2006-04-06 Not applicable Canada 
Enablex Tablet, extended release 7.5 mg Oral Searchlight Pharma Inc 2006-04-06 Not applicable Canada Enablex Tablet, extended release 15 mg/1 Oral Novartis 2004-12-22 2014-06-30 US Enablex Tablet, extended release 15 mg/1 Oral Allergan, Inc. 2004-12-22 Not applicable US 
Enablex Tablet, extended release 15 mg/1 Oral Lake Erie Medical &Surgical Supply Dba Quality Care Products Llc 2012-03-05 2014-12-31 US Enablex Tablet, extended release 7.5 mg/1 Oral Novartis 2004-12-22 2014-06-30 US Additional Data Available- Application NumberApplication Number
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct Code
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
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- Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Unlock Additional DataApo-darifenacin Tablet, extended release Oral Apotex Corporation Not applicable Not applicable Canada Apo-darifenacin Tablet, extended release Oral Apotex Corporation Not applicable Not applicable Canada Darifenacin Tablet, extended release 15 mg/1 Oral Jubilant Cadista Pharmaceuticals Inc. 2016-10-12 Not applicable US Darifenacin Tablet, extended release 15 mg/1 Oral Cipla USA Inc. 2016-09-01 Not applicable US Darifenacin Tablet, extended release 15 mg/1 Oral Torrent Pharmaceuticals Limited 2016-11-18 Not applicable US Darifenacin Tablet, extended release 7.5 mg/1 Oral Jubilant Cadista Pharmaceuticals Inc. 2016-10-12 Not applicable US Darifenacin Tablet, extended release 7.5 mg/1 Oral Torrent Pharmaceuticals Limited 2016-11-18 Not applicable US Darifenacin Tablet, extended release 7.5 mg/1 Oral Cipla USA Inc. 2016-09-01 Not applicable US Darifenacin Tablet, extended release 15 mg/1 Oral Macleods Pharmaceuticals Limited 2017-07-29 Not applicable US Darifenacin Tablet, extended release 15 mg/1 Oral Alembic Pharmaceuticals Inc. 2017-12-12 Not applicable US Additional Data Available- Application NumberApplication Number
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct Code
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
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- International/Other Brands
- Emselex (Novartis) / Xelena (Dr. Reddy's)
- Categories
- Agents producing tachycardia
- Anticholinergic Agents
- Cholinergic Agents
- Cytochrome P-450 CYP2D6 Inhibitors
- Cytochrome P-450 CYP2D6 Inhibitors (moderate)
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Drugs for Urinary Frequency and Incontinence
- Genito Urinary System and Sex Hormones
- Heterocyclic Compounds, Fused-Ring
- Muscarinic Antagonists
- Neurotransmitter Agents
- Urological Agents
- Urologicals
- UNII
- APG9819VLM
- CAS number
- 133099-04-4
- Weight
- Average: 426.55
Monoisotopic: 426.230728214 - Chemical Formula
- C28H30N2O2
- InChI Key
- HXGBXQDTNZMWGS-RUZDIDTESA-N
- InChI
- InChI=1S/C28H30N2O2/c29-27(31)28(23-7-3-1-4-8-23,24-9-5-2-6-10-24)25-14-17-30(20-25)16-13-21-11-12-26-22(19-21)15-18-32-26/h1-12,19,25H,13-18,20H2,(H2,29,31)/t25-/m1/s1
- IUPAC Name
- 2-[(3S)-1-[2-(2,3-dihydro-1-benzofuran-5-yl)ethyl]pyrrolidin-3-yl]-2,2-diphenylacetamide
- SMILES
- NC(=O)C([C@@H]1CCN(CCC2=CC3=C(OCC3)C=C2)C1)(C1=CC=CC=C1)C1=CC=CC=C1
Pharmacology
- Indication
For the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency and frequency.
- Associated Conditions
- Pharmacodynamics
Darifenacin is a competitive muscarinic receptor antagonist. In vitro studies using human recombinant muscarinic receptor subtypes show that darifenacin has greater affinity for the M3 receptor than for the other known muscarinic receptors (9 and 12-fold greater affinity for M3 compared to M1 and M5, respectively, and 59-fold greater affinity for M3 compared to both M2 and M4). Muscarinic receptors play an important role in several major cholinergically mediated functions, including contractions of the urinary bladder smooth muscle and stimulation of salivary secretion. Adverse drug effects such as dry mouth, constipation and abnormal vision may be mediated through effects on M3 receptors in these organs.
- Mechanism of action
Darifenacin selectively antagonizes the muscarinic M3 receptor. M3 receptors are involved in contraction of human bladder and gastrointestinal smooth muscle, saliva production, and iris sphincter function.
Target Actions Organism AMuscarinic acetylcholine receptor M3 antagonistHumans UMuscarinic acetylcholine receptor M1 antagonistHumans UMuscarinic acetylcholine receptor M2 antagonistHumans UMuscarinic acetylcholine receptor M4 antagonistHumans UMuscarinic acetylcholine receptor M5 antagonistHumans - Absorption
The mean oral bioavailability at steady state is estimated to be 15% and 19% for 7.5 mg and 15 mg tablets, respectively.
- Volume of distribution
- 163 L
- Protein binding
Darifenacin is approximately 98% bound to plasma proteins (primarily to alpha-1-acid-glycoprotein).
- Metabolism
Hepatic. Primarily mediated by the cytochrome P450 enzymes CYP2D6 and CYP3A4.
- Route of elimination
- Not Available
- Half life
The elimination half-life of darifenacin following chronic dosing is approximately 13-19 hours.
- Clearance
- 40 L/h [extensive metabolizers]
- 32 L/h [poor metabolizers]
- Toxicity
Overdosage can potentially result in severe central anticholinergic effects.
- Affected organisms
- Humans and other mammals
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
Interacting Gene/Enzyme Allele name Genotype(s) Defining Change(s) Type(s) Description Details Cytochrome P450 2D6 CYP2D6*3 Not Available C allele Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*4 Not Available C allele Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*5 Not Available Whole-gene deletion Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*6 Not Available 1707delT Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*7 Not Available 2935A>C Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*8 Not Available 1758G>T Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*11 Not Available 883G>C Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*12 Not Available 124G>A Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*13 Not Available CYP2D7/2D6 hybrid gene structure Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*14A Not Available 1758G>A Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*15 Not Available 137insT, 137_138insT Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*19 Not Available 2539_2542delAACT Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*20 Not Available 1973_1974insG Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*21 Not Available 2573insC Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*31 Not Available -1770G>A / -1584C>G … show all Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*36 Not Available 100C>T / -1426C>T … show all Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*38 Not Available 2587_2590delGACT Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*40 Not Available 1863_1864ins(TTT CGC CCC)2 Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*42 Not Available 3259_3260insGT Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*44 Not Available 2950G>C Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*47 Not Available 100C>T / -1426C>T … show all Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*51 Not Available -1584C>G / -1235A>G … show all Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*56 Not Available 3201C>T Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*57 Not Available 100C>T / 310G>T … show all Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*62 Not Available 4044C>T Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*68A Not Available -1426C>T / -1235A>G … show all Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*68B Not Available Similar but not identical switch region compared to CYP2D6*68A. Found in tandem arrangement with CYP2D6*4. Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*69 Not Available 2988G>A / -1426C>T … show all Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*92 Not Available 1995delC Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*100 Not Available -1426C>T / -1235A>G … show all Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*101 Not Available -1426C>T / -1235A>G … show all Effect Inferred Poor drug metabolizer. Details Cytochrome P450 3A4 CYP3A4*20 Not Available 1461_1462insA Effect Inferred Poor drug metabolizer. Details Cytochrome P450 3A4 CYP3A4*26 Not Available 802C>T Effect Inferred Poor drug metabolizer. Details
Unlock Additional Data
Additional Data Available
Adverse Effects
Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.
Learn more Additional Data Available
Contraindications
Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.
Learn more Additional Data Available
Blackbox Warnings
Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.
Learn moreInteractions
- 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 Unlock Additional Data1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine The metabolism of Darifenacin can be decreased when combined with 1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine. 1,10-Phenanthroline The therapeutic efficacy of Darifenacin can be decreased when used in combination with 1,10-Phenanthroline. 2,5-Dimethoxy-4-ethylamphetamine The risk or severity of Tachycardia can be increased when Darifenacin is combined with 2,5-Dimethoxy-4-ethylamphetamine. 2,5-Dimethoxy-4-ethylthioamphetamine 2,5-Dimethoxy-4-ethylthioamphetamine may increase the central nervous system depressant (CNS depressant) activities of Darifenacin. 4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may increase the central nervous system depressant (CNS depressant) activities of Darifenacin. 4-Methoxyamphetamine The metabolism of 4-Methoxyamphetamine can be decreased when combined with Darifenacin. 5-methoxy-N,N-dimethyltryptamine The metabolism of Darifenacin can be decreased when combined with 5-methoxy-N,N-dimethyltryptamine. 7-Nitroindazole 7-Nitroindazole may increase the central nervous system depressant (CNS depressant) activities of Darifenacin. 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the central nervous system depressant (CNS depressant) activities of Darifenacin. Abatacept The metabolism of Darifenacin can be increased when combined with Abatacept. Additional Data Available- Extended DescriptionExtended Description
Extended description of the mechanism of action and particular properties of each drug interaction.
Learn more - Severity
- Evidence Level
- ActionAction
An effect category for each drug interaction. Know how this interaction affects the subject drug.
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- Food Interactions
- Take with or without food. The absorption is unaffected by food.
References
- Synthesis Reference
Valeriano Merli, Augusto Canavesi, Paola Daverio, "Processes for preparing darifenacin hydrobromide." U.S. Patent US20070197631, issued August 23, 2007.
US20070197631- General References
- Not Available
- External Links
- Human Metabolome Database
- HMDB0014639
- KEGG Drug
- D01699
- PubChem Compound
- 444031
- PubChem Substance
- 46508104
- ChemSpider
- 392054
- BindingDB
- 50109647
- RxNav
- 136198
- ChEBI
- 391960
- ChEMBL
- CHEMBL1346
- ZINC
- ZINC000001996117
- Therapeutic Targets Database
- DAP001131
- PharmGKB
- PA164774901
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Darifenacin
- ATC Codes
- G04BD10 — Darifenacin
- AHFS Codes
- 86:12.04 — Antimuscarinics
- FDA label
- Download (394 KB)
Clinical Trials
- Clinical Trials
Pharmacoeconomics
- Manufacturers
- Novartis pharmaceuticals corp
- Packagers
- Lake Erie Medical and Surgical Supply
- Murfreesboro Pharmaceutical Nursing Supply
- Novartis AG
- Pfizer Inc.
- Physicians Total Care Inc.
- Redpharm Drug
- Dosage forms
Form Route Strength Tablet, extended release Oral Tablet, film coated, extended release Oral 15 mg/1 Tablet, film coated, extended release Oral 7.5 mg/1 Tablet, extended release Oral 15 mg/1 Tablet, extended release Oral 15 mg Tablet, extended release Oral 7.5 mg/1 Tablet, extended release Oral 7.5 mg - Prices
Unit description Cost Unit Enablex 15 mg 24 Hour tablet 5.22USD tablet Enablex 7.5 mg 24 Hour tablet 5.22USD tablet Enablex 15 mg tablet 5.02USD tablet Enablex 7.5 mg tablet 5.02USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Unlock Additional DataUS5096890 No 1992-03-17 2015-03-13 US CA2469702 No 2010-07-06 2022-03-05 Canada CA2230314 No 2003-06-24 2016-08-21 Canada US6106864 No 2000-08-22 2016-08-21 US Additional Data Available- Filed On
Properties
- State
- Solid
- Experimental Properties
Property Value Source logP 4.5 Not Available - Predicted Properties
Property Value Source Water Solubility 0.000298 mg/mL ALOGPS logP 4.35 ALOGPS logP 4.54 ChemAxon logS -6.2 ALOGPS pKa (Strongest Acidic) 16.21 ChemAxon pKa (Strongest Basic) 10.11 ChemAxon Physiological Charge 1 ChemAxon Hydrogen Acceptor Count 3 ChemAxon Hydrogen Donor Count 1 ChemAxon Polar Surface Area 55.56 Å2 ChemAxon Rotatable Bond Count 7 ChemAxon Refractivity 128.37 m3·mol-1 ChemAxon Polarizability 48.54 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 Yes ChemAxon - Predicted ADMET features
Property Value Probability Human Intestinal Absorption + 0.9966 Blood Brain Barrier + 0.9989 Caco-2 permeable - 0.5256 P-glycoprotein substrate Substrate 0.6385 P-glycoprotein inhibitor I Non-inhibitor 0.6329 P-glycoprotein inhibitor II Inhibitor 0.5374 Renal organic cation transporter Inhibitor 0.6441 CYP450 2C9 substrate Non-substrate 0.8774 CYP450 2D6 substrate Non-substrate 0.5946 CYP450 3A4 substrate Substrate 0.6046 CYP450 1A2 substrate Non-inhibitor 0.696 CYP450 2C9 inhibitor Non-inhibitor 0.8253 CYP450 2D6 inhibitor Inhibitor 0.5816 CYP450 2C19 inhibitor Inhibitor 0.5399 CYP450 3A4 inhibitor Inhibitor 0.5 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.6168 Ames test Non AMES toxic 0.7145 Carcinogenicity Non-carcinogens 0.8847 Biodegradation Not ready biodegradable 0.9599 Rat acute toxicity 3.0008 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.907 hERG inhibition (predictor II) Inhibitor 0.6703
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS Not Available Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Taxonomy
- Description
- This compound belongs to the class of organic compounds known as diphenylmethanes. These are compounds containing a diphenylmethane moiety, which consists of a methane wherein two hydrogen atoms are replaced by two phenyl groups.
- Kingdom
- Organic compounds
- Super Class
- Benzenoids
- Class
- Benzene and substituted derivatives
- Sub Class
- Diphenylmethanes
- Direct Parent
- Diphenylmethanes
- Alternative Parents
- Phenylacetamides / Phenethylamines / Coumarans / Aralkylamines / Alkyl aryl ethers / N-alkylpyrrolidines / Trialkylamines / Primary carboxylic acid amides / Amino acids and derivatives / Oxacyclic compounds show 5 more
- Substituents
- Diphenylmethane / Phenylacetamide / Phenethylamine / Coumaran / Alkyl aryl ether / Aralkylamine / N-alkylpyrrolidine / Pyrrolidine / Amino acid or derivatives / Carboxamide group show 18 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- monocarboxylic acid amide, 1-benzofurans, pyrrolidines (CHEBI:391960)
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- 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
- Bharucha AE, Ravi K, Zinsmeister AR: Comparison of selective M3 and nonselective muscarinic receptor antagonists on gastrointestinal transit and bowel habits in humans. Am J Physiol Gastrointest Liver Physiol. 2010 Jul;299(1):G215-9. doi: 10.1152/ajpgi.00072.2010. Epub 2010 Apr 15. [PubMed:20395537]
- Bozkurt TE, Sahin-Erdemli I: M(1) and M(3) muscarinic receptors are involved in the release of urinary bladder-derived relaxant factor. Pharmacol Res. 2009 May;59(5):300-5. doi: 10.1016/j.phrs.2009.01.013. Epub 2009 Feb 5. [PubMed:19416629]
- Jha S, Parsons M: Treatment of overactive bladder in the aging population: focus on darifenacin. Clin Interv Aging. 2006;1(4):309-16. [PubMed:18046909]
- 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
- Humans
- 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
- Jha S, Parsons M: Treatment of overactive bladder in the aging population: focus on darifenacin. Clin Interv Aging. 2006;1(4):309-16. [PubMed:18046909]
- Moriya H, Takagi Y, Nakanishi T, Hayashi M, Tani T, Hirotsu I: Affinity profiles of various muscarinic antagonists for cloned human muscarinic acetylcholine receptor (mAChR) subtypes and mAChRs in rat heart and submandibular gland. Life Sci. 1999;64(25):2351-8. [PubMed:10374898]
- Kind
- Protein
- Organism
- Humans
- 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
- Jha S, Parsons M: Treatment of overactive bladder in the aging population: focus on darifenacin. Clin Interv Aging. 2006;1(4):309-16. [PubMed:18046909]
- Moriya H, Takagi Y, Nakanishi T, Hayashi M, Tani T, Hirotsu I: Affinity profiles of various muscarinic antagonists for cloned human muscarinic acetylcholine receptor (mAChR) subtypes and mAChRs in rat heart and submandibular gland. Life Sci. 1999;64(25):2351-8. [PubMed:10374898]
- Kind
- Protein
- Organism
- Humans
- 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
- Jha S, Parsons M: Treatment of overactive bladder in the aging population: focus on darifenacin. Clin Interv Aging. 2006;1(4):309-16. [PubMed:18046909]
- Moriya H, Takagi Y, Nakanishi T, Hayashi M, Tani T, Hirotsu I: Affinity profiles of various muscarinic antagonists for cloned human muscarinic acetylcholine receptor (mAChR) subtypes and mAChRs in rat heart and submandibular gland. Life Sci. 1999;64(25):2351-8. [PubMed:10374898]
- Kind
- Protein
- Organism
- Humans
- 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
- Moriya H, Takagi Y, Nakanishi T, Hayashi M, Tani T, Hirotsu I: Affinity profiles of various muscarinic antagonists for cloned human muscarinic acetylcholine receptor (mAChR) subtypes and mAChRs in rat heart and submandibular gland. Life Sci. 1999;64(25):2351-8. [PubMed:10374898]
- Jha S, Parsons M: Treatment of overactive bladder in the aging population: focus on darifenacin. Clin Interv Aging. 2006;1(4):309-16. [PubMed:18046909]
Enzymes
- Kind
- Protein
- Organism
- Humans
- 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
- Skerjanec A: The clinical pharmacokinetics of darifenacin. Clin Pharmacokinet. 2006;45(4):325-50. [PubMed:16584282]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- 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
- Skerjanec A: The clinical pharmacokinetics of darifenacin. Clin Pharmacokinet. 2006;45(4):325-50. [PubMed:16584282]
Drug created on June 13, 2005 07:24 / Updated on May 25, 2020 23:44
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