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Identification
NameTolterodine
Accession NumberDB01036  (APRD00146)
TypeSmall Molecule
GroupsApproved, Investigational
Description

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

Structure
Thumb
Synonyms
(+)-(R)-2-(alpha-(2-(Diisopropylamino)ethyl)benzyl)-p-cresol
(+)-Tolterodine
Tolterodina
Tolterodine
Tolterodinum
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Detroltablet, film coated2 mg/1oralSTAT Rx USA LLC1998-03-25Not applicableUs
Detroltablet, film coated1 mg/1oralPharmacia and Upjohn Company1998-03-25Not applicableUs
Detroltablet2 mgoralPfizer Canada Inc1998-11-23Not applicableCanada
Detroltablet1 mgoralPfizer Canada Inc1998-11-26Not applicableCanada
Detroltablet, film coated2 mg/1oralPharmacia and Upjohn Company1998-03-25Not applicableUs
Detrol LAcapsule, extended release4 mg/1oralPd Rx Pharmaceuticals, Inc.2000-02-22Not applicableUs
Detrol LAcapsule (extended release)4 mgoralPfizer Canada Inc2002-03-26Not applicableCanada
Detrol LAcapsule, extended release2 mg/1oralCardinal Health2000-12-22Not applicableUs
Detrol LAcapsule, extended release4 mg/1oralCardinal Health2000-12-22Not applicableUs
Detrol LAcapsule (extended release)2 mgoralPfizer Canada Inc2002-03-26Not applicableCanada
Detrol LAcapsule, extended release2 mg/1oralPhysicians Total Care, Inc.2004-09-03Not applicableUs
Detrol LAcapsule, extended release4 mg/1oralPharmacia and Upjohn Company2000-02-22Not applicableUs
Detrol LAcapsule, extended release4 mg/1oralPhysicians Total Care, Inc.2004-09-03Not applicableUs
Detrol LAcapsule, extended release2 mg/1oralPharmacia and Upjohn Company2000-02-22Not applicableUs
Detrol LAcapsule, extended release4 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-02-28Not applicableUs
Gd-tolterodinetablet2 mgoralGenmed A Division Of Pfizer Canada IncNot applicableNot applicableCanada
Gd-tolterodinetablet1 mgoralGenmed A Division Of Pfizer Canada IncNot applicableNot applicableCanada
Gd-tolterodine LAcapsule (extended release)4 mgoralGenmed A Division Of Pfizer Canada IncNot applicableNot applicableCanada
Gd-tolterodine LAcapsule (extended release)2 mgoralGenmed A Division Of Pfizer Canada IncNot applicableNot applicableCanada
Mint-tolterodinetablet2 mgoralMint Pharmaceuticals Inc2015-12-16Not applicableCanada
Mint-tolterodinetablet1 mgoralMint Pharmaceuticals Inc2015-12-16Not applicableCanada
Mylan-tolterodine ERcapsule (extended release)4 mgoralMylan Pharmaceuticals Ulc2015-10-23Not applicableCanada
Mylan-tolterodine ERcapsule (extended release)2 mgoralMylan Pharmaceuticals Ulc2015-10-23Not applicableCanada
Ran-tolterodinetablet2 mgoralRanbaxy Pharmaceuticals Canada Inc.Not applicableNot applicableCanada
Ran-tolterodinetablet1 mgoralRanbaxy Pharmaceuticals Canada Inc.Not applicableNot applicableCanada
Sandoz Tolterodine LAcapsule (extended release)2 mgoralSandoz Canada Incorporated2015-12-16Not applicableCanada
Sandoz Tolterodine LAcapsule (extended release)4 mgoralSandoz Canada Incorporated2015-12-16Not applicableCanada
Teva-tolterodinetablet2 mgoralTeva Canada Limited2015-12-16Not applicableCanada
Teva-tolterodinetablet1 mgoralTeva Canada Limited2015-12-16Not applicableCanada
Teva-tolterodine LAcapsule (extended release)4 mgoralTeva Canada Limited2015-12-16Not applicableCanada
Teva-tolterodine LAcapsule (extended release)2 mgoralTeva Canada Limited2015-12-16Not applicableCanada
Tolterodine Tartratetablet, film coated1 mg/1oralGreenstone LLC2014-01-21Not applicableUs
Tolterodine Tartratetablet, film coated1 mg/1oralTeva Pharmaceuticals USA Inc2012-05-11Not applicableUs
Tolterodine Tartratetablet, film coated2 mg/1oralTeva Pharmaceuticals USA Inc2012-05-11Not applicableUs
Tolterodine Tartratecapsule, extended release2 mg/1oralTeva Pharmaceuticals USA Inc2014-01-02Not applicableUs
Tolterodine Tartratecapsule, extended release4 mg/1oralTeva Pharmaceuticals USA Inc2014-01-02Not applicableUs
Tolterodine Tartratetablet, film coated2 mg/1oralGreenstone LLC2014-01-21Not applicableUs
Tolterodine Tartrate Extended Releasecapsule, extended release4 mg/1oralGreenstone LLC2000-02-22Not applicableUs
Tolterodine Tartrate Extended Releasecapsule, extended release2 mg/1oralGreenstone LLC2000-02-22Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-tolterodinetablet2 mgoralApotex Inc2016-03-03Not applicableCanada
Apo-tolterodinetablet1 mgoralApotex Inc2016-03-03Not applicableCanada
Tolterodine Tartratetablet, film coated1 mg/1oralMacleods Pharmaceuticals Limited2015-10-08Not applicableUs
Tolterodine Tartratetablet, film coated1 mg/1oralTeva Pharmaceuticals USA Inc2015-11-01Not applicableUs
Tolterodine Tartratecapsule, extended release4 mg/1oralTorrent Pharmaceuticals Limited2015-08-11Not applicableUs
Tolterodine Tartratetablet, film coated2 mg/1oralApotex Corp.2012-09-25Not applicableUs
Tolterodine Tartratecapsule, extended release2 mg/1oralTorrent Pharmaceuticals Limited2015-08-11Not applicableUs
Tolterodine Tartratetablet, film coated1 mg/1oralApotex Corp.2012-09-25Not applicableUs
Tolterodine Tartratetablet, film coated2 mg/1oralMylan Pharmaceuticals Inc.2012-11-28Not applicableUs
Tolterodine Tartratetablet, film coated2 mg/1oralMylan Institutional Inc.2013-03-26Not applicableUs
Tolterodine Tartratetablet, film coated1 mg/1oralMylan Pharmaceuticals Inc.2012-11-28Not applicableUs
Tolterodine Tartratecapsule, extended release4 mg/1oralMylan Institutional Inc.2014-01-29Not applicableUs
Tolterodine Tartratecapsule, extended release4 mg/1oralMylan Pharmaceuticals Inc.2014-01-06Not applicableUs
Tolterodine Tartratecapsule, extended release2 mg/1oralMylan Institutional Inc.2014-01-28Not applicableUs
Tolterodine Tartratecapsule, extended release2 mg/1oralMylan Pharmaceuticals Inc.2014-01-06Not applicableUs
Tolterodine Tartratetablet, film coated2 mg/1oralMacleods Pharmaceuticals Limited2015-10-08Not applicableUs
Tolterodine Tartratetablet, film coated2 mg/1oralTeva Pharmaceuticals USA Inc2015-11-01Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
DetrusitolNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Tolterodine Tartrate
Thumb
  • InChI Key: TWHNMSJGYKMTRB-KXYUELECSA-N
  • Monoisotopic Mass: 475.257002543
  • Average Mass: 475.5745
DBSALT000467
Categories
UNIIWHE7A56U7K
CAS number124937-51-5
WeightAverage: 325.4876
Monoisotopic: 325.240564619
Chemical FormulaC22H31NO
InChI KeyInChIKey=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[[email protected]](C1=CC=CC=C1)C1=C(O)C=CC(C)=C1)C(C)C
Taxonomy
DescriptionThis 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.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassDiphenylmethanes
Direct ParentDiphenylmethanes
Alternative Parents
Substituents
  • Diphenylmethane
  • Phenylpropylamine
  • P-cresol
  • Aralkylamine
  • Toluene
  • Phenol
  • Tertiary aliphatic amine
  • Tertiary amine
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Amine
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of overactive bladder (with symptoms of urinary frequency, urgency, or urge incontinence).
PharmacodynamicsTolterodine 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 actionBoth 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.
Related Articles
AbsorptionNot Available
Volume of distribution
  • 113 ± 26.7 L
Protein bindingApproximately 96.3%.
Metabolism
SubstrateEnzymesProduct
Tolterodine
N-Dealkylated tolterodineDetails
Tolterodine
5-Hydroxymethyl tolterodineDetails
N-Dealkylated tolterodine
Not Available
N-Dealkylated 5-hydroxymethyl tolterodineDetails
5-Hydroxymethyl tolterodine
Not Available
N-Dealkylated 5-hydroxymethyl tolterodineDetails
5-Hydroxymethyl tolterodine
Not Available
5-Carboxylic acid tolterodineDetails
Route of eliminationFollowing 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 life1.9-3.7 hours
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
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 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Tabletoral1 mg
Tabletoral2 mg
Tablet, film coatedoral1 mg/1
Tablet, film coatedoral2 mg/1
Capsule (extended release)oral2 mg
Capsule (extended release)oral4 mg
Capsule, extended releaseoral2 mg/1
Capsule, extended releaseoral4 mg/1
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)
CA1340223 No1998-12-152015-12-15Canada
CA2311755 No2010-03-232019-08-26Canada
US5382600 No1995-03-252012-03-25Us
US6630162 Yes2000-05-112020-05-11Us
US6770295 Yes2000-02-262020-02-26Us
US6911217 Yes2000-05-112020-05-11Us
Properties
StateSolid
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 FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

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

US20040249211
General ReferencesNot Available
External Links
ATC CodesG04BD07
AHFS Codes
  • 86:12.00
PDB EntriesNot Available
FDA labelDownload (94.9 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Tolterodine can be increased when it is combined with Abiraterone.
AclidiniumAclidinium may increase the anticholinergic activities of Tolterodine.
AprepitantThe serum concentration of Tolterodine can be increased when it is combined with Aprepitant.
AtazanavirThe serum concentration of Tolterodine can be increased when it is combined with Atazanavir.
BexaroteneThe serum concentration of Tolterodine can be decreased when it is combined with Bexarotene.
BoceprevirThe serum concentration of Tolterodine can be increased when it is combined with Boceprevir.
BosentanThe serum concentration of Tolterodine can be decreased when it is combined with Bosentan.
Botulinum Toxin Type ATolterodine may increase the anticholinergic activities of Botulinum Toxin Type A.
Botulinum Toxin Type BTolterodine may increase the anticholinergic activities of Botulinum Toxin Type B.
CeritinibThe serum concentration of Tolterodine can be increased when it is combined with Ceritinib.
Cimetropium BromideTolterodine may increase the anticholinergic activities of Cimetropium Bromide.
CitalopramTolterodine may increase the QTc-prolonging activities of Citalopram.
ClarithromycinThe serum concentration of Tolterodine can be increased when it is combined with Clarithromycin.
CobicistatThe serum concentration of Tolterodine can be increased when it is combined with Cobicistat.
ConivaptanThe serum concentration of Tolterodine can be increased when it is combined with Conivaptan.
DabrafenibThe serum concentration of Tolterodine can be decreased when it is combined with Dabrafenib.
DarunavirThe serum concentration of Tolterodine can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Tolterodine can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Tolterodine can be decreased when it is combined with Deferasirox.
DofetilideTolterodine may increase the QTc-prolonging activities of Dofetilide.
DronabinolTolterodine may increase the tachycardic activities of Dronabinol.
EluxadolineTolterodine may increase the activities of Eluxadoline.
FluconazoleThe metabolism of Tolterodine can be decreased when combined with Fluconazole.
FluoxetineThe metabolism of Tolterodine can be decreased when combined with Fluoxetine.
FosaprepitantThe serum concentration of Tolterodine can be increased when it is combined with Fosaprepitant.
Fusidic AcidThe serum concentration of Tolterodine can be increased when it is combined with Fusidic Acid.
Glucagon recombinantThe risk or severity of adverse effects can be increased when Tolterodine is combined with Glucagon recombinant.
GoserelinTolterodine may increase the QTc-prolonging activities of Goserelin.
IdelalisibThe serum concentration of Tolterodine can be increased when it is combined with Idelalisib.
IndinavirThe serum concentration of Tolterodine can be increased when it is combined with Indinavir.
Ipratropium bromideIpratropium bromide may increase the anticholinergic activities of Tolterodine.
ItoprideThe therapeutic efficacy of Itopride can be decreased when used in combination with Tolterodine.
ItraconazoleThe serum concentration of Tolterodine can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Tolterodine can be increased when it is combined with Ivacaftor.
KetoconazoleThe serum concentration of Tolterodine can be increased when it is combined with Ketoconazole.
LeuprolideTolterodine may increase the QTc-prolonging activities of Leuprolide.
LuliconazoleThe serum concentration of Tolterodine can be increased when it is combined with Luliconazole.
MianserinMianserin may increase the anticholinergic activities of Tolterodine.
MifepristoneThe serum concentration of Tolterodine can be increased when it is combined with Mifepristone.
MirabegronThe risk or severity of adverse effects can be increased when Tolterodine is combined with Mirabegron.
MitotaneThe serum concentration of Tolterodine can be decreased when it is combined with Mitotane.
MorphineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Morphine.
NefazodoneThe serum concentration of Tolterodine can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Tolterodine can be increased when it is combined with Nelfinavir.
NetupitantThe serum concentration of Tolterodine can be increased when it is combined with Netupitant.
PalbociclibThe serum concentration of Tolterodine can be increased when it is combined with Palbociclib.
PanobinostatThe serum concentration of Tolterodine can be increased when it is combined with Panobinostat.
Peginterferon alfa-2bThe serum concentration of Tolterodine can be decreased when it is combined with Peginterferon alfa-2b.
PhenytoinThe metabolism of Tolterodine can be increased when combined with Phenytoin.
PosaconazoleThe serum concentration of Tolterodine can be increased when it is combined with Posaconazole.
Potassium ChlorideTolterodine may increase the ulcerogenic activities of Potassium Chloride.
PramlintidePramlintide may increase the anticholinergic activities of Tolterodine.
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Tolterodine.
RamosetronTolterodine may increase the activities of Ramosetron.
RitonavirThe serum concentration of Tolterodine can be increased when it is combined with Ritonavir.
SaquinavirThe serum concentration of Tolterodine can be increased when it is combined with Saquinavir.
SecretinThe therapeutic efficacy of Secretin can be decreased when used in combination with Tolterodine.
SiltuximabThe serum concentration of Tolterodine can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Tolterodine can be increased when it is combined with Simeprevir.
St. John's WortThe serum concentration of Tolterodine can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Tolterodine can be increased when it is combined with Stiripentol.
SulpirideThe therapeutic efficacy of Sulpiride can be decreased when used in combination with Tolterodine.
TacrineThe therapeutic efficacy of Tolterodine can be decreased when used in combination with Tacrine.
TelaprevirThe serum concentration of Tolterodine can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Tolterodine can be increased when it is combined with Telithromycin.
TiclopidineThe metabolism of Tolterodine can be decreased when combined with Ticlopidine.
TiotropiumTolterodine may increase the anticholinergic activities of Tiotropium.
TocilizumabThe serum concentration of Tolterodine can be decreased when it is combined with Tocilizumab.
TopiramateThe risk or severity of adverse effects can be increased when Tolterodine is combined with Topiramate.
TrichlormethiazideThe serum concentration of Trichlormethiazide can be increased when it is combined with Tolterodine.
UmeclidiniumUmeclidinium may increase the anticholinergic activities of Tolterodine.
VinblastineThe serum concentration of Tolterodine can be increased when it is combined with Vinblastine.
VoriconazoleThe serum concentration of Tolterodine can be increased when it is combined with Voriconazole.
WarfarinTolterodine may increase the anticoagulant activities of Warfarin.
Food Interactions
  • Take with food.

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 action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM3
Uniprot ID:
P20309
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. [PubMed:11752352 ]
  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. [PubMed:14769832 ]
  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. [PubMed:19168050 ]
  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. [PubMed:11193006 ]
Kind
Protein
Organism
Human
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 action of G proteins. Primary transducing effect is adenylate cyclase inhibition. Signaling promotes phospholipase C activity, leading to the release of inositol trisphosphate (IP3); this then trigge...
Gene Name:
CHRM2
Uniprot ID:
P08172
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. [PubMed:16188951 ]
  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. [PubMed:14769832 ]
  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. [PubMed:19168050 ]
  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. [PubMed:11193006 ]
Kind
Protein
Organism
Human
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 action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM5
Uniprot ID:
P08912
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. [PubMed:16406943 ]
Kind
Protein
Organism
Human
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 action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM1
Uniprot ID:
P11229
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. [PubMed:17139284 ]
  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. [PubMed:17016423 ]
  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. [PubMed:14769832 ]
Kind
Protein
Organism
Human
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 action of G proteins. Primary transducing effect is inhibition of adenylate cyclase.
Gene Name:
CHRM4
Uniprot ID:
P08173
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. [PubMed:16406943 ]

Enzymes

Kind
Protein
Organism
Human
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 antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
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. [PubMed:19515014 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 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. [PubMed:19515014 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  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. [PubMed:9531513 ]
Kind
Protein
Organism
Human
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
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. [PubMed:19515014 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
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 imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
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. [PubMed:19515014 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
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Drug created on June 13, 2005 07:24 / Updated on July 01, 2016 03:05