Tolterodine

Identification

Summary

Tolterodine is a muscarinic receptor antagonist used to treat overactive bladder with urinary incontinence, urgency, and frequency.

Brand Names
Detrol, Detrusitol
Generic Name
Tolterodine
DrugBank Accession Number
DB01036
Background

Tolterodine is an antimuscarinic drug that is used to treat urinary incontinence. Tolterodine acts on M2 and M3 subtypes of muscarinic receptors.

Type
Small Molecule
Groups
Approved, Investigational
Structure
Thumb
Weight
Average: 325.4876
Monoisotopic: 325.240564619
Chemical Formula
C22H31NO
Synonyms
  • (+)-(R)-2-(alpha-(2-(Diisopropylamino)ethyl)benzyl)-p-cresol
  • (+)-Tolterodine
  • Tolterodina
  • Tolterodine
  • Tolterodinum

Pharmacology

Indication

For the treatment of overactive bladder (with symptoms of urinary frequency, urgency, or urge incontinence).

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Tolterodine is a competitive muscarinic receptor antagonist. Both urinary bladder contraction and salivation are mediated via cholinergic muscarinic receptors. After oral administration, tolterodine is metabolized in the liver, resulting in the formation of the 5-hydroxymethyl derivative, a major pharmacologically active metabolite. The 5-hydroxymethyl metabolite, which exhibits an antimuscarinic activity similar to that of tolterodine, contributes significantly to the therapeutic effect. Both tolterodine and the 5-hydroxymethyl metabolite exhibit a high specificity for muscarinic receptors, since both show negligible activity or affinity for other neurotransmitter receptors and other potential cellular targets, such as calcium channels. Tolterodine has a pronounced effect on bladder function. The main effects of tolterodine are an increase in residual urine, reflecting an incomplete emptying of the bladder, and a decrease in detrusor pressure, consistent with an antimuscarinic action on the lower urinary tract.

Mechanism of action

Both tolterodine and its active metabolite, 5-hydroxymethyltolterodine, act as competitive antagonists at muscarinic receptors. This antagonism results in inhibition of bladder contraction, decrease in detrusor pressure, and an incomplete emptying of the bladder.

TargetActionsOrganism
AMuscarinic acetylcholine receptor M3
antagonist
Humans
AMuscarinic acetylcholine receptor M2
antagonist
Humans
AMuscarinic acetylcholine receptor M5
antagonist
Humans
AMuscarinic acetylcholine receptor M1
antagonist
Humans
AMuscarinic acetylcholine receptor M4
antagonist
Humans
Absorption

Not Available

Volume of distribution
  • 113 ± 26.7 L
Protein binding

Approximately 96.3%.

Metabolism

Hover over products below to view reaction partners

Route of elimination

Following administration of a 5-mg oral dose of 14C-tolterodine solution to healthy volunteers, 77% of radioactivity was recovered in urine and 17% was recovered in feces in 7 days.

Half-life

1.9-3.7 hours

Clearance

Not Available

Adverse Effects
Adverseeffects
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Toxicity

Not Available

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, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*4Not AvailableC alleleEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*5Not AvailableWhole-gene deletionEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*6Not Available1707delTEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*7Not Available2935A>CEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*8Not Available1758G>TEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*11Not Available883G>CEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*12Not Available124G>AEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*13Not AvailableCYP2D7/2D6 hybrid gene structureEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*14ANot Available1758G>AEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*15Not Available137insT, 137_138insTEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*19Not Available2539_2542delAACTEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*20Not Available1973_1974insGEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*21Not Available2573insCEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*31Not Available-1770G>A / -1584C>G  … show all Effect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*36Not Available100C>T / -1426C>T  … show all Effect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*38Not Available2587_2590delGACTEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*40Not Available1863_1864ins(TTT CGC CCC)2Effect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*42Not Available3259_3260insGTEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*44Not Available2950G>CEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*47Not Available100C>T / -1426C>T  … show all Effect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*51Not Available-1584C>G / -1235A>G  … show all Effect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*56Not Available3201C>TEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*57Not Available100C>T / 310G>T  … show all Effect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*62Not Available4044C>TEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*68ANot Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.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, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*69Not Available2988G>A / -1426C>T  … show all Effect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*92Not Available1995delCEffect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*100Not Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details
Cytochrome P450 2D6CYP2D6*101Not Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes.Details

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.
DrugInteraction
1,2-Benzodiazepine1,2-Benzodiazepine may increase the central nervous system depressant (CNS depressant) activities of Tolterodine.
AbacavirTolterodine may decrease the excretion rate of Abacavir which could result in a higher serum level.
AbametapirThe serum concentration of Tolterodine can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Tolterodine can be increased when combined with Abatacept.
AbirateroneThe metabolism of Tolterodine can be decreased when combined with Abiraterone.
AcebutololThe metabolism of Tolterodine can be decreased when combined with Acebutolol.
AceclofenacAceclofenac may decrease the excretion rate of Tolterodine which could result in a higher serum level.
AcemetacinAcemetacin may decrease the excretion rate of Tolterodine which could result in a higher serum level.
AcenocoumarolThe metabolism of Acenocoumarol can be decreased when combined with Tolterodine.
AcetaminophenAcetaminophen may decrease the excretion rate of Tolterodine which could result in a higher serum level.
Interactions
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Food Interactions
  • Take with food.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Tolterodine tartrate5T619TQR3R124937-52-6TWHNMSJGYKMTRB-KXYUELECSA-N
Product Images
International/Other Brands
Detrusitol
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
DetrolTablet, film coated1 mg/1OralPhysicians Total Care, Inc.1998-03-252010-06-30US flag
DetrolTablet, film coated2 mg/1OralPharmacia & Upjohn Company LLC1998-03-25Not applicableUS flag
DetrolTablet2 mgOralUpjohn Canada Ulc1998-11-23Not applicableCanada flag
DetrolTablet, film coated2 mg/1OralStat Rx USA1998-03-25Not applicableUS flag
DetrolTablet1 mgOralUpjohn Canada Ulc1998-11-26Not applicableCanada flag
DetrolTablet, film coated1 mg/1OralPharmacia & Upjohn Company LLC1998-03-25Not applicableUS flag
DetrolTablet, film coated2 mg/1OralPhysicians Total Care, Inc.1998-03-252012-06-30US flag
Detrol LACapsule, extended release4 mg/1OralPharmacia and Upjohn Company LLC2000-02-22Not applicableUS flag0009 519120180812 28838 1vamki
Detrol LACapsule, extended release4 mg/1OralLake Erie Medical &Surgical Supply Dba Quality Care Products Llc2012-02-282016-06-01US flag
Detrol LACapsule, extended release4 mg/1OralPD-Rx Pharmaceuticals, Inc.2000-02-22Not applicableUS flag00009 5191 02 nlmimage10 3c159e1c
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Ach-tolterodine Tartrate Extended ReleaseCapsule, extended release2 mgOralAccord Healthcare IncNot applicableNot applicableCanada flag
Ach-tolterodine Tartrate Extended ReleaseCapsule, extended release4 mgOralAccord Healthcare IncNot applicableNot applicableCanada flag
Apo-tolterodineTablet2 mgOralApotex Corporation2016-03-03Not applicableCanada flag
Apo-tolterodineTablet1 mgOralApotex Corporation2016-03-03Not applicableCanada flag
Gd-tolterodineTablet2 mgOralGenmed A Division Of Pfizer Canada UlcNot applicableNot applicableCanada flag
Gd-tolterodineTablet1 mgOralGenmed A Division Of Pfizer Canada UlcNot applicableNot applicableCanada flag
Gd-tolterodine LACapsule, extended release4 mgOralGenmed A Division Of Pfizer Canada UlcNot applicableNot applicableCanada flag
Gd-tolterodine LACapsule, extended release2 mgOralGenmed A Division Of Pfizer Canada UlcNot applicableNot applicableCanada flag
Jamp TolterodineTablet2 mgOralJamp Pharma CorporationNot applicableNot applicableCanada flag
Jamp TolterodineTablet1 mgOralJamp Pharma CorporationNot applicableNot applicableCanada flag

Categories

ATC Codes
G04BD07 — Tolterodine
Drug Categories
Chemical TaxonomyProvided by Classyfire
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
Para cresols / Toluenes / Aralkylamines / 1-hydroxy-2-unsubstituted benzenoids / Trialkylamines / Organopnictogen compounds / Organooxygen compounds / Hydrocarbon derivatives
Substituents
1-hydroxy-2-unsubstituted benzenoid / Amine / Aralkylamine / Aromatic homomonocyclic compound / Diphenylmethane / Hydrocarbon derivative / Organic nitrogen compound / Organic oxygen compound / Organonitrogen compound / Organooxygen compound
Molecular Framework
Aromatic homomonocyclic compounds
External Descriptors
tertiary amine (CHEBI:9622)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
WHE7A56U7K
CAS number
124937-51-5
InChI Key
OOGJQPCLVADCPB-HXUWFJFHSA-N
InChI
InChI=1S/C22H31NO/c1-16(2)23(17(3)4)14-13-20(19-9-7-6-8-10-19)21-15-18(5)11-12-22(21)24/h6-12,15-17,20,24H,13-14H2,1-5H3/t20-/m1/s1
IUPAC Name
2-[(1R)-3-[bis(propan-2-yl)amino]-1-phenylpropyl]-4-methylphenol
SMILES
CC(C)N(CC[C@H](C1=CC=CC=C1)C1=C(O)C=CC(C)=C1)C(C)C

References

Synthesis Reference

Yatendra Kumar, "PROCESS FOR THE PREPARATION OF TOLTERODINE." U.S. Patent US20040249211, issued December 09, 2004.

US20040249211
General References
Not Available
Human Metabolome Database
HMDB0015170
KEGG Drug
D00646
KEGG Compound
C07750
PubChem Compound
443879
PubChem Substance
46508059
ChemSpider
391967
BindingDB
50165008
RxNav
119565
ChEBI
9622
ChEMBL
CHEMBL1382
ZINC
ZINC000000968336
Therapeutic Targets Database
DAP000376
PharmGKB
PA164746757
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Tolterodine
FDA label
Download (94.9 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedNot AvailableHealthy Subjects (HS) / Pharmacokinetics of Mirabegron and Tolterodine1
4CompletedTreatmentBenign Prostatic Hyperplasia (BPH)1
4CompletedTreatmentBenign Prostatic Hyperplasia (BPH) / Overactive Bladder Syndrome (OABS)1
4CompletedTreatmentBladder Outlet Obstruction1
4CompletedTreatmentCognition / Memory1
4CompletedTreatmentHealthy Subjects (HS)1
4CompletedTreatmentOveractive Bladder Syndrome (OABS)9
4CompletedTreatmentPain, Chronic2
4CompletedTreatmentUreteral Obstruction1
4CompletedTreatmentUrinary Incontinence (UI)5

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Cardinal Health
  • Catalent Pharma Solutions
  • Kaiser Foundation Hospital
  • Pfizer Inc.
  • Pharmacia Inc.
  • Physicians Total Care Inc.
  • Resource Optimization and Innovation LLC
  • Southwood Pharmaceuticals
  • Vangard Labs Inc.
Dosage Forms
FormRouteStrength
Tablet, film coated, extended release
TabletOral2 mg
Tablet, film coatedOral1 mg/1
Tablet, film coatedOral2 mg/1
Capsule, extended releaseOral2 mg/1
Capsule, extended releaseOral4 mg/1
Tablet, film coatedOral
TabletOral
CapsuleOral
Capsule, extended releaseOral2 mg
Capsule, extended releaseOral4 mg
CapsuleOral2 mg
CapsuleOral4 mg
Capsule, extended releaseOral
Tablet, film coatedOral1 mg
Tablet, film coatedOral2 mg
Tablet, coatedOral1 mg
Tablet, coatedOral2 mg
Tablet, film coatedOral1.00 mg
Tablet, film coatedOral2.00 mg
TabletOral2 mg/1
TabletOral1 mg/1
Tablet, extended releaseOral1 mg/1
Tablet, extended releaseOral2 mg/1
TabletOral1 mg
Prices
Unit descriptionCostUnit
Detrol LA 2 mg 24 Hour Capsule5.01USD capsule
Detrol LA 4 mg 24 Hour Capsule4.84USD capsule
Detrol la 4 mg capsule4.82USD capsule
Detrol la 2 mg capsule4.81USD capsule
Detrol 2 mg tablet2.85USD tablet
Detrol 1 mg tablet2.77USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US5382600No1995-01-172012-03-25US flag
CA2311755No2010-03-232019-08-26Canada flag
CA1340223No1998-12-152015-12-15Canada flag
US6630162Yes2003-10-072020-05-11US flag
US6770295Yes2004-08-032020-02-26US flag
US6911217Yes2005-06-282020-05-11US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
logP5.6Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00534 mg/mLALOGPS
logP5.39ALOGPS
logP5.12ChemAxon
logS-4.8ALOGPS
pKa (Strongest Acidic)10.28ChemAxon
pKa (Strongest Basic)11.01ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area23.47 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity103.96 m3·mol-1ChemAxon
Polarizability39.27 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.958
Blood Brain Barrier+0.9194
Caco-2 permeable+0.8286
P-glycoprotein substrateSubstrate0.5
P-glycoprotein inhibitor INon-inhibitor0.6727
P-glycoprotein inhibitor IINon-inhibitor0.8305
Renal organic cation transporterInhibitor0.6904
CYP450 2C9 substrateNon-substrate0.6235
CYP450 2D6 substrateSubstrate0.8918
CYP450 3A4 substrateSubstrate0.7408
CYP450 1A2 substrateInhibitor0.8139
CYP450 2C9 inhibitorNon-inhibitor0.6965
CYP450 2D6 inhibitorInhibitor0.7456
CYP450 2C19 inhibitorNon-inhibitor0.5853
CYP450 3A4 inhibitorNon-inhibitor0.8575
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.5259
Ames testNon AMES toxic0.6658
CarcinogenicityNon-carcinogens0.7967
BiodegradationNot ready biodegradable0.9959
Rat acute toxicity2.5503 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8014
hERG inhibition (predictor II)Inhibitor0.6875
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
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-000t-2911000000-6586d7c95e03f623dbf4

Targets

Drugtargets2
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insights and accelerate drug research.
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Learn more
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
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
  2. Schneider T, Fetscher C, Krege S, Michel MC: Signal transduction underlying carbachol-induced contraction of human urinary bladder. J Pharmacol Exp Ther. 2004 Jun;309(3):1148-53. Epub 2004 Feb 9. [Article]
  3. McNamara A, Pulido-Rios MT, Sweazey S, Obedencio GP, Thibodeaux H, Renner T, Armstrong SR, Steinfeld T, Hughes AD, Wilson RD, Jasper JR, Mammen M, Hegde SS: Pharmacological properties of TD-6301, a novel bladder selective muscarinic receptor antagonist. Eur J Pharmacol. 2009 Mar 1;605(1-3):145-52. doi: 10.1016/j.ejphar.2008.12.043. Epub 2009 Jan 10. [Article]
  4. Sellers DJ, Yamanishi T, Chapple CR, Couldwell C, Yasuda K, Chess-Williams R: M3 muscarinic receptors but not M2 mediate contraction of the porcine detrusor muscle in vitro. J Auton Pharmacol. 2000 Jun;20(3):171-6. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
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. Nelson CP, Nahorski SR, Challiss RA: Constitutive activity and inverse agonism at the M2 muscarinic acetylcholine receptor. J Pharmacol Exp Ther. 2006 Jan;316(1):279-88. Epub 2005 Sep 27. [Article]
  2. Schneider T, Fetscher C, Krege S, Michel MC: Signal transduction underlying carbachol-induced contraction of human urinary bladder. J Pharmacol Exp Ther. 2004 Jun;309(3):1148-53. Epub 2004 Feb 9. [Article]
  3. McNamara A, Pulido-Rios MT, Sweazey S, Obedencio GP, Thibodeaux H, Renner T, Armstrong SR, Steinfeld T, Hughes AD, Wilson RD, Jasper JR, Mammen M, Hegde SS: Pharmacological properties of TD-6301, a novel bladder selective muscarinic receptor antagonist. Eur J Pharmacol. 2009 Mar 1;605(1-3):145-52. doi: 10.1016/j.ejphar.2008.12.043. Epub 2009 Jan 10. [Article]
  4. Sellers DJ, Yamanishi T, Chapple CR, Couldwell C, Yasuda K, Chess-Williams R: M3 muscarinic receptors but not M2 mediate contraction of the porcine detrusor muscle in vitro. J Auton Pharmacol. 2000 Jun;20(3):171-6. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
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. Maruyama S, Oki T, Otsuka A, Shinbo H, Ozono S, Kageyama S, Mikami Y, Araki I, Takeda M, Masuyama K, Yamada S: Human muscarinic receptor binding characteristics of antimuscarinic agents to treat overactive bladder. J Urol. 2006 Jan;175(1):365-9. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
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. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
  3. Schneider T, Fetscher C, Krege S, Michel MC: Signal transduction underlying carbachol-induced contraction of human urinary bladder. J Pharmacol Exp Ther. 2004 Jun;309(3):1148-53. Epub 2004 Feb 9. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
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. Maruyama S, Oki T, Otsuka A, Shinbo H, Ozono S, Kageyama S, Mikami Y, Araki I, Takeda M, Masuyama K, Yamada S: Human muscarinic receptor binding characteristics of antimuscarinic agents to treat overactive bladder. J Urol. 2006 Jan;175(1):365-9. [Article]

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
  1. Postlind H, DanielsonA, Lindgren A, Andersson SH: Tolterodine, a new muscarinic receptor antagonist, is metabolized by cytochromes P450 2D6 and 3A in human liver microsomes. Drug Metab Dispos. 1998 Apr;26(4):289-93. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [Article]
  2. Brynne N, Dalen P, Alvan G, Bertilsson L, Gabrielsson J: Influence of CYP2D6 polymorphism on the pharmacokinetics and pharmacodynamic of tolterodine. Clin Pharmacol Ther. 1998 May;63(5):529-39. doi: 10.1016/S0009-9236(98)90104-7. [Article]
  3. Oishi M, Chiba K, Malhotra B, Suwa T: Effect of the CYP2D6*10 genotype on tolterodine pharmacokinetics. Drug Metab Dispos. 2010 Sep;38(9):1456-63. doi: 10.1124/dmd.110.033407. Epub 2010 Jun 7. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid 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 oxidizes a variety of structurally un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [Article]
  2. Rendic S: Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448. [Article]
  3. Postlind H, DanielsonA, Lindgren A, Andersson SH: Tolterodine, a new muscarinic receptor antagonist, is metabolized by cytochromes P450 2D6 and 3A in human liver microsomes. Drug Metab Dispos. 1998 Apr;26(4):289-93. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [Article]
  2. Postlind H, DanielsonA, Lindgren A, Andersson SH: Tolterodine, a new muscarinic receptor antagonist, is metabolized by cytochromes P450 2D6 and 3A in human liver microsomes. Drug Metab Dispos. 1998 Apr;26(4):289-93. [Article]

Drug created on June 13, 2005 13:24 / Updated on October 18, 2021 04:56