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 works by blocking the M3 muscarinic acetylcholine receptor, which is primarily responsible for bladder muscle contractions. It thereby decreases the urgency to urinate. It should not be used in people with urinary retention.

It is not known whether this selectivity for the M3 receptor translates into any clinical advantage when treating symptoms of overactive bladder syndrome.

Structure
Thumb
Synonyms
  • (S)-1-(2-(2,3-dihydro-5-Benzofuranyl)ethyl)-alpha,alpha-diphenyl-3-pyrrolidineacetamide
  • Darifenacin
  • Darifenacina
  • Darifénacine
  • Darifenacinum
External IDs
UK 88525 / UK 88525-04
Product Ingredients
IngredientUNIICASInChI Key
Darifenacin HydrobromideCR02EYQ8GV133099-07-7UQAVIASOPREUIT-VQIWEWKSSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
DarifenacinTablet, extended release15 mg/1OralActavis Pharma Company2016-03-15Not applicableUs
DarifenacinTablet, extended release7.5 mg/1OralActavis Pharma Company2016-03-15Not applicableUs
EnablexTablet, extended release15 mg/1OralPhysicians Total Care, Inc.2005-07-20Not applicableUs
EnablexTablet, extended release7.5 mgOralMerus Labs Luxco S. A R.L.2006-04-06Not applicableCanada
EnablexTablet, extended release15 mg/1OralLake Erie Medical &Surgical Supply Dba Quality Care Products Llc2012-03-052014-12-31Us
EnablexTablet, extended release15 mg/1OralNovartis2004-12-222014-06-30Us
EnablexTablet, extended release7.5 mg/1OralPhysicians Total Care, Inc.2006-11-06Not applicableUs
EnablexTablet, extended release15 mg/1OralAllergan2004-12-22Not applicableUs00430 0171 15 nlmimage10 153a0af0
EnablexTablet, extended release7.5 mg/1OralNovartis2004-12-222014-06-30Us
EnablexTablet, extended release15 mgOralMerus Labs Luxco S. A R.L.2006-04-06Not applicableCanada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-darifenacinTablet, extended release15 mgOralApotex CorporationNot applicableNot applicableCanada
Apo-darifenacinTablet, extended release7.5 mgOralApotex CorporationNot applicableNot applicableCanada
DarifenacinTablet, extended release15 mg/1OralTorrent Pharmaceuticals Limited2016-11-18Not applicableUs
DarifenacinTablet, extended release7.5 mg/1OralJubilant Cadista Pharmaceuticals Inc.2016-10-12Not applicableUs
DarifenacinTablet, extended release15 mg/1OralCipla Limited2016-09-01Not applicableUs
DarifenacinTablet, film coated, extended release15 mg/1OralAurobindo Pharma Limited2016-09-19Not applicableUs
DarifenacinTablet, extended release15 mg/1OralAlembic Pharmaceuticals Limited2017-12-12Not applicableUs
DarifenacinTablet, extended release7.5 mg/1OralAlembic Pharmaceuticals Inc.2017-12-12Not applicableUs
DarifenacinTablet, extended release7.5 mg/1OralTorrent Pharmaceuticals Limited2016-11-18Not applicableUs
DarifenacinTablet, extended release15 mg/1OralMacleods Pharmaceuticals Limited2017-07-29Not applicableUs
International/Other Brands
Emselex (Novartis) / Xelena (Dr. Reddy's)
Categories
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.

TargetActionsOrganism
AMuscarinic acetylcholine receptor M3
antagonist
Human
UMuscarinic acetylcholine receptor M1
antagonist
Human
UMuscarinic acetylcholine receptor M2
antagonist
Human
UMuscarinic acetylcholine receptor M4
antagonist
Human
UMuscarinic acetylcholine receptor M5
antagonist
Human
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/EnzymeAllele nameGenotype(s)Defining Change(s)Type(s)DescriptionDetails
Cytochrome P450 2D6CYP2D6*3Not AvailableC alleleEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*4Not AvailableC alleleEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*5Not AvailableWhole-gene deletionEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*6Not Available1707delTEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*7Not Available2935A>CEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*8Not Available1758G>TEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*11Not Available883G>CEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*12Not Available124G>AEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*13Not AvailableCYP2D7/2D6 hybrid gene structureEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*14ANot Available1758G>AEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*15Not Available137insT, 137_138insTEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*19Not Available2539_2542delAACTEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*20Not Available1973_1974insGEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*21Not Available2573insCEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*31Not Available-1770G>A / -1584C>G  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*36Not Available100C>T / -1426C>T  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*38Not Available2587_2590delGACTEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*40Not Available1863_1864ins(TTT CGC CCC)2Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*42Not Available3259_3260insGTEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*44Not Available2950G>CEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*47Not Available100C>T / -1426C>T  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*51Not Available-1584C>G / -1235A>G  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*56Not Available3201C>TEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*57Not Available100C>T / 310G>T  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*62Not Available4044C>TEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*68ANot Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*68BNot AvailableSimilar but not identical switch region compared to CYP2D6*68A. Found in tandem arrangement with CYP2D6*4.Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*69Not Available2988G>A / -1426C>T  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*92Not Available1995delCEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*100Not Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2D6CYP2D6*101Not Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 3A4CYP3A4*20Not Available1461_1462insAEffect InferredPoor drug metabolizer.Details
Cytochrome P450 3A4CYP3A4*26Not Available802C>TEffect InferredPoor drug metabolizer.Details

Interactions

Drug Interactions
DrugInteraction
(2-benzhydryloxyethyl)diethyl-methylammonium iodideThe risk or severity of adverse effects can be increased when Darifenacin is combined with (2-benzhydryloxyethyl)diethyl-methylammonium iodide.
(R)-warfarinThe metabolism of Darifenacin can be decreased when combined with (R)-warfarin.
(S)-WarfarinThe metabolism of Darifenacin can be decreased when combined with (S)-Warfarin.
1,10-PhenanthrolineThe therapeutic efficacy of Darifenacin can be decreased when used in combination with 1,10-Phenanthroline.
3,5-diiodothyropropionic acidThe metabolism of Darifenacin can be decreased when combined with 3,5-diiodothyropropionic acid.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be decreased when combined with Darifenacin.
4-MethoxyamphetamineThe metabolism of 4-Methoxyamphetamine can be decreased when combined with Darifenacin.
5-androstenedioneThe metabolism of Darifenacin can be decreased when combined with 5-androstenedione.
6-O-benzylguanineThe metabolism of Darifenacin can be decreased when combined with 6-O-benzylguanine.
AbemaciclibThe metabolism of Darifenacin can be decreased when combined with Abemaciclib.
Food Interactions
  • Take without regard to meals.

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
ChEBI
391960
ChEMBL
CHEMBL1346
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
PhaseStatusPurposeConditionsCount
1CompletedTreatmentHealthy Volunteers2
1Unknown StatusNot AvailableBioequivalency2
2CompletedTreatmentHealthy Volunteers1
2TerminatedTreatmentDisseminated Sclerosis / Overactive Detrusor1
2TerminatedTreatmentNeurogenic Detrusor Overactivity1
3CompletedTreatmentUrinary Bladder, Overactive3
4CompletedNot AvailableUrinary Bladder, Overactive1
4CompletedNot AvailableUrinary Incontinence (UI)1
4CompletedTreatmentHealthy Volunteers1
4CompletedTreatmentNeurogenic Detrusor Overactivity / Spinal Cord Injuries (SCI)1
4CompletedTreatmentUrinary Bladder, Overactive2
4WithdrawnNot AvailableNocturia1
Not AvailableActive Not RecruitingNot AvailableUrinary Bladder, Overactive1
Not AvailableCompletedNot AvailableUrinary Bladder Diseases / Urinary Bladder, Overactive / Urologic Diseases1
Not AvailableCompletedNot AvailableUrinary Bladder, Overactive1
Not AvailableCompletedTreatmentParkinson's Disease (PD) / Urinary Bladder, Overactive1
Not AvailableRecruitingNot AvailableUrinary Bladder, Overactive1
Not AvailableTerminatedTreatmentBladder Spasms / Postoperative / Postoperative pain / Renal Colic / Ureteral Stent Pain / Urinary Bladder, Overactive1

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
FormRouteStrength
Tablet, film coated, extended releaseOral15 mg/1
Tablet, film coated, extended releaseOral7.5 mg/1
Tablet, extended releaseOral15 mg/1
Tablet, extended releaseOral15 mg
Tablet, extended releaseOral7.5 mg
Tablet, extended releaseOral7.5 mg/1
Prices
Unit descriptionCostUnit
Enablex 15 mg 24 Hour tablet5.22USD tablet
Enablex 7.5 mg 24 Hour tablet5.22USD tablet
Enablex 15 mg tablet5.02USD tablet
Enablex 7.5 mg tablet5.02USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5096890No1995-03-132015-03-13Us
CA2469702No2010-07-062022-03-05Canada
CA2230314No2003-06-242016-08-21Canada
US6106864No1996-08-212016-08-21Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
logP4.5Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.000298 mg/mLALOGPS
logP4.35ALOGPS
logP4.54ChemAxon
logS-6.2ALOGPS
pKa (Strongest Acidic)16.21ChemAxon
pKa (Strongest Basic)10.11ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area55.56 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity128.37 m3·mol-1ChemAxon
Polarizability48.54 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9966
Blood Brain Barrier+0.9989
Caco-2 permeable-0.5256
P-glycoprotein substrateSubstrate0.6385
P-glycoprotein inhibitor INon-inhibitor0.6329
P-glycoprotein inhibitor IIInhibitor0.5374
Renal organic cation transporterInhibitor0.6441
CYP450 2C9 substrateNon-substrate0.8774
CYP450 2D6 substrateNon-substrate0.5946
CYP450 3A4 substrateSubstrate0.6046
CYP450 1A2 substrateNon-inhibitor0.696
CYP450 2C9 inhibitorNon-inhibitor0.8253
CYP450 2D6 inhibitorInhibitor0.5816
CYP450 2C19 inhibitorInhibitor0.5399
CYP450 3A4 inhibitorInhibitor0.5
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.6168
Ames testNon AMES toxic0.7145
CarcinogenicityNon-carcinogens0.8847
BiodegradationNot ready biodegradable0.9599
Rat acute toxicity3.0008 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.907
hERG inhibition (predictor II)Inhibitor0.6703
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

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
Human
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
  1. 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]
  2. 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]
  3. 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]
  4. 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
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. 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]
  2. 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
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. 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]
  2. 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
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. 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]
  2. 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
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. 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]
  2. 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
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. Skerjanec A: The clinical pharmacokinetics of darifenacin. Clin Pharmacokinet. 2006;45(4):325-50. [PubMed:16584282]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
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. 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 October 21, 2018 20:23