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
Structure for Tolterodine (DB01036)
- 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).
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Urinary urge incontinence •••••••••••• •••••••• •••••••• ••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
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.
Target Actions Organism AMuscarinic acetylcholine receptor M3 antagonistHumans AMuscarinic acetylcholine receptor M2 antagonistHumans AMuscarinic acetylcholine receptor M5 antagonistHumans AMuscarinic acetylcholine receptor M1 antagonistHumans AMuscarinic acetylcholine receptor M4 antagonistHumans - 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
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
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, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes. Details Cytochrome P450 2D6 CYP2D6*4 Not Available C allele Effect Inferred Poor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes. Details Cytochrome P450 2D6 CYP2D6*5 Not Available Whole-gene deletion Effect Inferred Poor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes. Details Cytochrome P450 2D6 CYP2D6*6 Not Available 1707delT Effect Inferred Poor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes. Details Cytochrome P450 2D6 CYP2D6*7 Not Available 2935A>C Effect Inferred Poor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes. Details Cytochrome P450 2D6 CYP2D6*8 Not Available 1758G>T Effect Inferred Poor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes. Details Cytochrome P450 2D6 CYP2D6*11 Not Available 883G>C Effect Inferred Poor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes. Details Cytochrome P450 2D6 CYP2D6*12 Not Available 124G>A Effect Inferred Poor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes. Details Cytochrome P450 2D6 CYP2D6*13 Not Available CYP2D7/2D6 hybrid gene structure Effect Inferred Poor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes. Details Cytochrome P450 2D6 CYP2D6*14A Not Available 1758G>A Effect Inferred Poor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes. Details Cytochrome P450 2D6 CYP2D6*15 Not Available 137insT, 137_138insT Effect Inferred Poor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes. Details Cytochrome P450 2D6 CYP2D6*19 Not Available 2539_2542delAACT Effect Inferred Poor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes. Details Cytochrome P450 2D6 CYP2D6*20 Not Available 1973_1974insG Effect Inferred Poor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes. Details Cytochrome P450 2D6 CYP2D6*21 Not Available 2573insC Effect Inferred Poor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes. Details Cytochrome P450 2D6 CYP2D6*31 Not Available -1770G>A / -1584C>G … show all Effect Inferred Poor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes. Details Cytochrome P450 2D6 CYP2D6*36 Not Available 100C>T / -1426C>T … show all Effect Inferred Poor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes. Details Cytochrome P450 2D6 CYP2D6*38 Not Available 2587_2590delGACT Effect Inferred Poor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes. Details Cytochrome P450 2D6 CYP2D6*40 Not Available 1863_1864ins(TTT CGC CCC)2 Effect Inferred Poor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes. Details Cytochrome P450 2D6 CYP2D6*42 Not Available 3259_3260insGT Effect Inferred Poor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes. Details Cytochrome P450 2D6 CYP2D6*44 Not Available 2950G>C Effect Inferred Poor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes. Details Cytochrome P450 2D6 CYP2D6*47 Not Available 100C>T / -1426C>T … show all Effect Inferred Poor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes. Details Cytochrome P450 2D6 CYP2D6*51 Not Available -1584C>G / -1235A>G … show all Effect Inferred Poor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes. Details Cytochrome P450 2D6 CYP2D6*56 Not Available 3201C>T Effect Inferred Poor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes. Details Cytochrome P450 2D6 CYP2D6*57 Not Available 100C>T / 310G>T … show all Effect Inferred Poor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes. Details Cytochrome P450 2D6 CYP2D6*62 Not Available 4044C>T Effect Inferred Poor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes. Details Cytochrome P450 2D6 CYP2D6*68A Not Available -1426C>T / -1235A>G … show all Effect Inferred Poor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes. 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, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes. Details Cytochrome P450 2D6 CYP2D6*69 Not Available 2988G>A / -1426C>T … show all Effect Inferred Poor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes. Details Cytochrome P450 2D6 CYP2D6*92 Not Available 1995delC Effect Inferred Poor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes. Details Cytochrome P450 2D6 CYP2D6*100 Not Available -1426C>T / -1235A>G … show all Effect Inferred Poor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes. Details Cytochrome P450 2D6 CYP2D6*101 Not Available -1426C>T / -1235A>G … show all Effect Inferred Poor drug metabolizer, greater QTc interval increase in poor metabolizers, but no association of drug with Torsade de Pointes. Details
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbacavir Tolterodine may decrease the excretion rate of Abacavir which could result in a higher serum level. Abametapir The serum concentration of Tolterodine can be increased when it is combined with Abametapir. Abatacept The metabolism of Tolterodine can be increased when combined with Abatacept. Abiraterone The metabolism of Tolterodine can be decreased when combined with Abiraterone. Abrocitinib The metabolism of Abrocitinib can be decreased when combined with Tolterodine. - Food Interactions
- Take with food.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Tolterodine tartrate 5T619TQR3R 124937-52-6 TWHNMSJGYKMTRB-KXYUELECSA-N - Product Images
- International/Other Brands
- Detrusitol
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Detrol Tablet, film coated 1 mg/1 Oral Pharmacia & Upjohn Company LLC 1998-03-25 Not applicable US 
Detrol Tablet, film coated 2 mg/1 Oral Physicians Total Care, Inc. 1998-03-25 2012-06-30 US Detrol Tablet 1 mg Oral Bgp Pharma Ulc 1998-11-26 Not applicable Canada 
Detrol Tablet, film coated 1 mg/1 Oral Physicians Total Care, Inc. 1998-03-25 2010-06-30 US Detrol Tablet, film coated 2 mg/1 Oral Pharmacia & Upjohn Company LLC 1998-03-25 Not applicable US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Ach-tolterodine Tartrate Extended Release Capsule, extended release 4 mg Oral Accord Healthcare Inc Not applicable Not applicable Canada Ach-tolterodine Tartrate Extended Release Capsule, extended release 2 mg Oral Accord Healthcare Inc Not applicable Not applicable Canada Apo-tolterodine Tablet 1 mg Oral Apotex Corporation 2016-03-03 Not applicable Canada Apo-tolterodine Tablet 2 mg Oral Apotex Corporation 2016-03-03 Not applicable Canada Gd-tolterodine Tablet 2 mg Oral Genmed A Division Of Pfizer Canada Ulc Not applicable Not applicable Canada
Categories
- ATC Codes
- G04BD07 — Tolterodine
- Drug Categories
- Agents producing tachycardia
- Alcohols
- Amines
- Amino Alcohols
- Anticholinergic Agents
- Benzene Derivatives
- Benzhydryl Compounds
- Cholinergic Agents
- Cresols
- Cytochrome P-450 CYP2C19 Substrates
- Cytochrome P-450 CYP2C9 Substrates
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Substrates
- Drugs for Urinary Frequency and Incontinence
- Drugs that are Mainly Renally Excreted
- Genito Urinary System and Sex Hormones
- Genitourinary Agents
- Genitourinary Smooth Muscle Relaxants
- Muscarinic Antagonists
- Neurotransmitter Agents
- Phenols
- Potential QTc-Prolonging Agents
- Propanolamines
- Propanols
- QTc Prolonging Agents
- Urological Agents
- Urologicals
- 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
- External Links
- Human Metabolome Database
- HMDB0015170
- KEGG Drug
- D00646
- KEGG Compound
- C07750
- PubChem Compound
- 443879
- PubChem Substance
- 46508059
- ChemSpider
- 391967
- BindingDB
- 50165008
- 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 Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Not Available Healthy Subjects (HS) / Pharmacokinetics of Mirabegron and Tolterodine 1 4 Completed Treatment Benign Prostatic Hyperplasia (BPH) 1 4 Completed Treatment Benign Prostatic Hyperplasia (BPH) / Overactive Bladder Syndrome (OABS) 1 4 Completed Treatment Bladder Outlet Obstruction 1 4 Completed Treatment Chronic Pain 2
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
Form Route Strength Tablet Oral 2.00 mg Tablet, film coated, extended release Tablet Oral 1 mg Tablet Oral 2 mg Tablet, film coated Oral 1 mg/1 Tablet, film coated Oral 2 mg/1 Capsule, extended release Oral 2 mg/1 Capsule, extended release Oral 4 mg/1 Tablet, film coated Oral Tablet Oral Capsule Oral 4.00 mg Capsule, extended release Oral 2 mg Capsule, extended release Oral 4 mg Capsule Oral 2 mg Capsule Oral 4 mg Tablet Oral 2.000 mg Capsule, extended release Oral 400000 mg Tablet, film coated Oral 1 mg Tablet, film coated Oral 2 mg Tablet, coated Oral 1 mg Capsule Oral Tablet, film coated, extended release 2 mg Capsule, extended release Oral Tablet, coated Oral 2 mg Tablet, film coated Oral 1.00 mg Tablet, film coated Oral 2.00 mg Tablet Oral 2 mg/1 Tablet Oral 1 mg/1 Tablet, extended release Oral 1 mg/1 Tablet, extended release Oral 2 mg/1 Tablet, film coated, extended release 4 mg Tablet Oral 2.0000 mg - Prices
Unit description Cost Unit Detrol LA 2 mg 24 Hour Capsule 5.01USD capsule Detrol LA 4 mg 24 Hour Capsule 4.84USD capsule Detrol la 4 mg capsule 4.82USD capsule Detrol la 2 mg capsule 4.81USD capsule Detrol 2 mg tablet 2.85USD tablet Detrol 1 mg tablet 2.77USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US5382600 No 1995-01-17 2012-03-25 US CA2311755 No 2010-03-23 2019-08-26 Canada CA1340223 No 1998-12-15 2015-12-15 Canada US6630162 Yes 2003-10-07 2020-05-11 US US6770295 Yes 2004-08-03 2020-02-26 US US6911217 Yes 2005-06-28 2020-05-11 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source logP 5.6 Not Available - Predicted Properties
Property Value Source Water Solubility 0.00534 mg/mL ALOGPS logP 5.39 ALOGPS logP 5.12 Chemaxon logS -4.8 ALOGPS pKa (Strongest Acidic) 10.28 Chemaxon pKa (Strongest Basic) 11.01 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 2 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 23.47 Å2 Chemaxon Rotatable Bond Count 7 Chemaxon Refractivity 103.96 m3·mol-1 Chemaxon Polarizability 39.29 Å3 Chemaxon Number of Rings 2 Chemaxon Bioavailability 1 Chemaxon Rule of Five No Chemaxon Ghose Filter Yes Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.958 Blood Brain Barrier + 0.9194 Caco-2 permeable + 0.8286 P-glycoprotein substrate Substrate 0.5 P-glycoprotein inhibitor I Non-inhibitor 0.6727 P-glycoprotein inhibitor II Non-inhibitor 0.8305 Renal organic cation transporter Inhibitor 0.6904 CYP450 2C9 substrate Non-substrate 0.6235 CYP450 2D6 substrate Substrate 0.8918 CYP450 3A4 substrate Substrate 0.7408 CYP450 1A2 substrate Inhibitor 0.8139 CYP450 2C9 inhibitor Non-inhibitor 0.6965 CYP450 2D6 inhibitor Inhibitor 0.7456 CYP450 2C19 inhibitor Non-inhibitor 0.5853 CYP450 3A4 inhibitor Non-inhibitor 0.8575 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.5259 Ames test Non AMES toxic 0.6658 Carcinogenicity Non-carcinogens 0.7967 Biodegradation Not ready biodegradable 0.9959 Rat acute toxicity 2.5503 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.8014 hERG inhibition (predictor II) Inhibitor 0.6875
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 194.6461435 predictedDarkChem Lite v0.1.0 [M-H]- 195.2610435 predictedDarkChem Lite v0.1.0 [M-H]- 183.21559 predictedDeepCCS 1.0 (2019) [M+H]+ 195.4828435 predictedDarkChem Lite v0.1.0 [M+H]+ 195.7198435 predictedDarkChem Lite v0.1.0 [M+H]+ 185.57358 predictedDeepCCS 1.0 (2019) [M+Na]+ 194.5233435 predictedDarkChem Lite v0.1.0 [M+Na]+ 195.3221435 predictedDarkChem Lite v0.1.0 [M+Na]+ 192.49144 predictedDeepCCS 1.0 (2019)
Targets
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Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- 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
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- 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]
- 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]
- 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
- 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]
- 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]
- 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]
- 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
- 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
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- 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]
- 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
- 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
- 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
- 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]
- 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]
- 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
- 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]
- 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
- 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]
- 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]
- 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
- 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
- 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 at June 13, 2005 13:24 / Updated at February 20, 2024 23:55