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

Similar Structures

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
Darifenacin	Tablet, extended release	15 mg/1	Oral	Actavis Pharma, Inc.	2016-03-15	Not applicable
Darifenacin	Tablet, extended release	7.5 mg/1	Oral	Actavis Pharma, Inc.	2016-03-15	Not applicable
Enablex	Tablet, extended release	7.5 mg/1	Oral	Novartis	2004-12-22	2014-06-30
Enablex	Tablet, extended release	7.5 mg	Oral	Merus Labs Luxco S. A R.L.	2006-04-06	Not applicable
Enablex	Tablet, extended release	7.5 mg/1	Oral	Allergan	2004-12-22	Not applicable
Enablex	Tablet, extended release	15 mg/1	Oral	Physicians Total Care, Inc.	2005-07-20	Not applicable
Enablex	Tablet, extended release	15 mg/1	Oral	Lake Erie Medical &Surgical Supply Dba Quality Care Products Llc	2012-03-05	2014-12-31
Enablex	Tablet, extended release	7.5 mg/1	Oral	Physicians Total Care, Inc.	2006-11-06	Not applicable
Enablex	Tablet, extended release	15 mg/1	Oral	Novartis	2004-12-22	2014-06-30
Enablex	Tablet, extended release	15 mg	Oral	Merus Labs Luxco S. A R.L.	2006-04-06	Not applicable

Generic Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Apo-darifenacin	Tablet, extended release	15 mg	Oral	Apotex Corporation	Not applicable	Not applicable
Apo-darifenacin	Tablet, extended release	7.5 mg	Oral	Apotex Corporation	Not applicable	Not applicable
Darifenacin	Tablet, film coated, extended release	15 mg/1	Oral	Aurobindo Pharma Limited	2016-09-19	Not applicable
Darifenacin	Tablet, extended release	7.5 mg/1	Oral	Alembic Pharmaceuticals Limited	2017-12-12	Not applicable
Darifenacin	Tablet, extended release	15 mg/1	Oral	Macleods Pharmaceuticals Limited	2017-07-29	Not applicable
Darifenacin	Tablet, film coated, extended release	7.5 mg/1	Oral	Aurobindo Pharma Limited	2016-09-19	Not applicable
Darifenacin	Tablet, extended release	15 mg/1	Oral	Cipla USA Inc.	2016-09-01	Not applicable
Darifenacin	Tablet, extended release	15 mg/1	Oral	Torrent Pharmaceuticals Limited	2016-11-18	Not applicable
Darifenacin	Tablet, extended release	15 mg/1	Oral	Alembic Pharmaceuticals Inc.	2017-12-12	Not applicable
Darifenacin	Tablet, extended release	7.5 mg/1	Oral	Macleods Pharmaceuticals Limited	2017-07-29	Not applicable

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

Urinary Bladder, Overactive

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	antagonist	Humans
UMuscarinic acetylcholine receptor M1	antagonist	Humans
UMuscarinic acetylcholine receptor M2	antagonist	Humans
UMuscarinic acetylcholine receptor M4	antagonist	Humans
UMuscarinic acetylcholine receptor M5	antagonist	Humans

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 CYP2D668A. Found in tandem arrangement with CYP2D64.	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

Interactions

Drug Interactions

Drug	Interaction
(R)-warfarin	The metabolism of Darifenacin can be decreased when combined with (R)-warfarin.
(S)-Warfarin	The metabolism of Darifenacin can be decreased when combined with (S)-Warfarin.
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	The risk or severity of Tachycardia can be increased when Darifenacin is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3,4-Methylenedioxyamphetamine	The risk or severity of Tachycardia can be increased when Darifenacin is combined with 3,4-Methylenedioxyamphetamine.
3,5-diiodothyropropionic acid	The metabolism of Darifenacin can be decreased when combined with 3,5-diiodothyropropionic acid.
4-Bromo-2,5-dimethoxyamphetamine	The risk or severity of Tachycardia can be increased when Darifenacin is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-hydroxycoumarin	The metabolism of 4-hydroxycoumarin can be decreased when combined with Darifenacin.
4-Methoxyamphetamine	The metabolism of 4-Methoxyamphetamine can be decreased when combined with Darifenacin.

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

Phase	Status	Purpose	Conditions	Count
1	Completed	Treatment	Healthy Volunteers	2
1	Unknown Status	Not Available	Bioequivalency	2
2	Completed	Treatment	Healthy Volunteers	1
2	Terminated	Treatment	Disseminated Sclerosis / Overactive Detrusor	1
2	Terminated	Treatment	Neurogenic Detrusor Overactivity	1
3	Completed	Treatment	Urinary Bladder, Overactive	3
4	Completed	Not Available	Urinary Bladder, Overactive	1
4	Completed	Not Available	Urinary Incontinence (UI)	1
4	Completed	Treatment	Healthy Volunteers	1
4	Completed	Treatment	Neurogenic Detrusor Overactivity / Spinal Cord Injuries (SCI)	1
4	Completed	Treatment	Urinary Bladder, Overactive	2
4	Withdrawn	Not Available	Nocturia	1
Not Available	Active Not Recruiting	Not Available	Urinary Bladder, Overactive	1
Not Available	Completed	Not Available	Urinary Bladder Diseases / Urinary Bladder, Overactive / Urologic Diseases	1
Not Available	Completed	Not Available	Urinary Bladder, Overactive	1
Not Available	Completed	Treatment	Parkinson's Disease (PD) / Urinary Bladder, Overactive	1
Not Available	Recruiting	Not Available	Urinary Bladder, Overactive	1
Not Available	Terminated	Treatment	Bladder Spasms / Postoperative / Postoperative pain / Renal Colic / Ureteral Stent Pain / Urinary Bladder, Overactive	1

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, 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)
US5096890	No	1992-03-17	2015-03-13
CA2469702	No	2010-07-06	2022-03-05
CA2230314	No	2003-06-24	2016-08-21
US6106864	No	2000-08-22	2016-08-21

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

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

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

Property	Measurement	pH	Temperature (°C)	References
Ki (nM)	0.84	N/A	N/A	11303071 / 11831911
Ki (nM)	1.3	N/A	N/A	16275087

Details1. Muscarinic acetylcholine receptor M3

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]

Property	Measurement	pH	Temperature (°C)	References
Ki (nM)	5.5	N/A	N/A	11303071 / 11831911

Details2. Muscarinic acetylcholine receptor M1

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]

Property	Measurement	pH	Temperature (°C)	References
Ki (nM)	47	N/A	N/A	11303071 / 11831911
Ki (nM)	50	N/A	N/A	16275087

Details3. Muscarinic acetylcholine receptor M2

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]

Property	Measurement	pH	Temperature (°C)	References
Ki (nM)	8.6	N/A	N/A	11303071 / 11831911

Details4. Muscarinic acetylcholine receptor M4

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]

Property	Measurement	pH	Temperature (°C)	References
Ki (nM)	2.3	N/A	N/A	11831911

Details5. Muscarinic acetylcholine receptor M5

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

Details1. Cytochrome P450 3A4

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]

Details2. Cytochrome P450 2D6

Kind: Protein
Organism: Humans
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

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 February 16, 2019 03:22

Darifenacin

Identification

Structure for Darifenacin (DB00496)

Pharmacology

Interactions

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Clinical Trials

Pharmacoeconomics

Properties

Spectra

Taxonomy

Targets

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Enzymes

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