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Identification
NameSolifenacin
Accession NumberDB01591  (APRD00168)
TypeSmall Molecule
GroupsApproved
Description

Solifenacin (rINN), marketed as solifenacin succinate under the trade name Vesicare, is a urinary antispasmodic of the anticholinergic class. It is used in the treatment of overactive bladder with urge incontinence. [Wikipedia]

Structure
Thumb
SynonymsNot Available
External Identifiers
  • YM-67905
  • YM-905
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Act Solifenacintablet10 mgoralActavis Pharma Company2015-09-30Not applicableCanada
Act Solifenacintablet5 mgoralActavis Pharma Company2015-09-30Not applicableCanada
Auro-solifenacintablet10 mgoralAuro Pharma Inc2016-01-04Not applicableCanada
Auro-solifenacintablet5 mgoralAuro Pharma Inc2016-01-04Not applicableCanada
Jamp-solifenacintablet10 mgoralJamp Pharma Corporation2015-12-29Not applicableCanada
Jamp-solifenacintablet5 mgoralJamp Pharma Corporation2015-12-29Not applicableCanada
Med-solifenacintablet5 mgoralGeneric Medical Partners Inc2016-04-18Not applicableCanada
Med-solifenacintablet10 mgoralGeneric Medical Partners Inc2016-04-18Not applicableCanada
Mint-solifenacintablet5 mgoralMint Pharmaceuticals Inc2016-04-20Not applicableCanada
Mint-solifenacintablet10 mgoralMint Pharmaceuticals Inc2016-04-20Not applicableCanada
PMS-solifenacintablet10 mgoralPharmascience Inc2015-10-28Not applicableCanada
PMS-solifenacintablet5 mgoralPharmascience Inc2015-10-28Not applicableCanada
Ran-solifenacintablet10 mgoralRanbaxy Pharmaceuticals Canada Inc.2015-12-29Not applicableCanada
Ran-solifenacintablet5 mgoralRanbaxy Pharmaceuticals Canada Inc.2015-12-29Not applicableCanada
Sandoz Solifenacintablet10 mgoralSandoz Canada Incorporated2015-09-30Not applicableCanada
Sandoz Solifenacintablet10 mgoralSandoz Canada Incorporated2015-09-30Not applicableCanada
Sandoz Solifenacintablet5 mgoralSandoz Canada Incorporated2015-09-30Not applicableCanada
Sandoz Solifenacintablet5 mgoralSandoz Canada Incorporated2015-09-30Not applicableCanada
Solifenacin Succinatetablet10 mgoralJubilant Generics LimitedNot applicableNot applicableCanada
Solifenacin Succinatetablet5 mgoralJubilant Generics LimitedNot applicableNot applicableCanada
Solifenacin Succinate Tabletstablet10 mgoralMda Inc.Not applicableNot applicableCanada
Solifenacin Succinate Tabletstablet5 mgoralMda Inc.Not applicableNot applicableCanada
Teva-solifenacintablet10 mgoralTeva Canada Limited2015-07-30Not applicableCanada
Teva-solifenacintablet5 mgoralTeva Canada Limited2015-07-30Not applicableCanada
Vesicaretablet, film coated5 mg/1oralAstellas Pharma Technologies, Inc.2005-01-05Not applicableUs
Vesicaretablet, film coated5 mg/1oralCardinal Health2005-01-05Not applicableUs
Vesicaretablet, film coated10 mg/1oralCardinal Health2005-01-05Not applicableUs
Vesicaretablet, film coated5 mg/1oralCardinal Health2005-01-05Not applicableUs
Vesicaretablet, film coated5 mg/1oralPhysicians Total Care, Inc.2005-08-29Not applicableUs
Vesicaretablet10 mgoralAstellas Pharma Canada Inc2006-06-23Not applicableCanada
Vesicaretablet, film coated10 mg/1oralPhysicians Total Care, Inc.2007-09-13Not applicableUs
Vesicaretablet5 mgoralAstellas Pharma Canada Inc2006-06-23Not applicableCanada
Vesicaretablet, film coated10 mg/1oralAstellas Pharma Technologies, Inc.2005-01-05Not applicableUs
Vesicaretablet, film coated10 mg/1oralCardinal Health2005-01-05Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
VesikurNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Solifenacin hydrochloride
Thumb
  • InChI Key: YAUBKMSXTZQZEB-VROPFNGYSA-N
  • Monoisotopic Mass: 398.1761058
  • Average Mass: 398.93
DBSALT001640
Solifenacin succinate
242478-38-2
Thumb
  • InChI Key: RXZMMZZRUPYENV-VROPFNGYSA-N
  • Monoisotopic Mass: 480.226036766
  • Average Mass: 480.5528
DBSALT001639
Categories
UNIIA8910SQJ1U
CAS number242478-37-1
WeightAverage: 362.473
Monoisotopic: 362.199428085
Chemical FormulaC23H26N2O2
InChI KeyFBOUYBDGKBSUES-VXKWHMMOSA-N
InChI
InChI=1S/C23H26N2O2/c26-23(27-21-16-24-13-10-18(21)11-14-24)25-15-12-17-6-4-5-9-20(17)22(25)19-7-2-1-3-8-19/h1-9,18,21-22H,10-16H2/t21-,22-/m0/s1
IUPAC Name
(3R)-1-azabicyclo[2.2.2]octan-3-yl (1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate
SMILES
O=C(O[[email protected]]1CN2CCC1CC2)N1CCC2=CC=CC=C2[C@@H]1C1=CC=CC=C1
Taxonomy
ClassificationNot classified
Pharmacology
IndicationFor the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and urinary frequency.
PharmacodynamicsSolifenacin is a competitive muscarinic receptor antagonist. Muscarinic receptors play an important role in several major cholinergically mediated functions, including contractions of urinary bladder smooth muscle and stimulation of salivary secretion.
Mechanism of actionSolifenacin is a competitive muscarinic acetylcholine receptor antagonist. The binding of acetylcholine to these receptors, particularly the M3 receptor subtype, plays a critical role in the contraction of smooth muscle. By preventing the binding of acetylcholine to these receptors, solifenacin reduces smooth muscle tone in the bladder, allowing the bladder to retain larger volumes of urine and reducing the number of incontinence episodes.
Related Articles
AbsorptionThe absolute bioavailability of solifenacin is approximately 90%, and plasma concentrations of solifenacin are proportional to the dose administered.
Volume of distribution
  • 600 L
Protein bindingSolifenacin is approximately 98% (in vivo) bound to human plasma proteins, principally to alpha1-acid glycoprotein.
Metabolism

Solifenacin is extensively metabolized in the liver. The primary pathway for elimination is by way of CYP3A4; however, alternate metabolic pathways exist. The primary metabolic routes of solifenacin are through N-oxidation of the quinuclidin ring and 4R-hydroxylation of tetrahydroisoquinoline ring. One pharmacologically active metabolite (4R-hydroxy solifenacin), occurring at low concentrations and unlikely to contribute significantly to clinical activity, and three pharmacologically inactive metabolites (N-glucuronide and the N-oxide and 4R-hydroxy-N-oxide of solifenacin) have been found in human plasma after oral dosing.

SubstrateEnzymesProduct
Solifenacin
Not Available
4R-hydroxy solifenacinDetails
Solifenacin
Not Available
4R-hydroxy-N-oxide solifenacinDetails
Route of eliminationThe primary pathway for elimination is by way of CYP3A4; however, alternate metabolic pathways exist.
Half lifeThe elimination half-life of solifenacin following chronic dosing is approximately 45-68 hours.
ClearanceNot Available
ToxicityOverdosage with solifenacin can potentially result in severe anticholinergic effects and should be treated accordingly. The highest solifenacin dose given to human volunteers was a single 100 mg dose. Intolerable anticholinergic side effects (fixed and dilated pupils, blurred vision, failure of heel-to-toe exam, tremors and dry skin) occurred on day 3 in normal volunteers taking 50 mg daily (5 times the maximum recommended therapeutic dose).
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+0.9706
Blood Brain Barrier+0.6159
Caco-2 permeable-0.6679
P-glycoprotein substrateSubstrate0.7801
P-glycoprotein inhibitor IInhibitor0.8572
P-glycoprotein inhibitor IIInhibitor0.8611
Renal organic cation transporterNon-inhibitor0.7498
CYP450 2C9 substrateNon-substrate0.8311
CYP450 2D6 substrateNon-substrate0.7264
CYP450 3A4 substrateSubstrate0.545
CYP450 1A2 substrateNon-inhibitor0.8445
CYP450 2C9 inhibitorNon-inhibitor0.8755
CYP450 2D6 inhibitorNon-inhibitor0.8593
CYP450 2C19 inhibitorNon-inhibitor0.7037
CYP450 3A4 inhibitorNon-inhibitor0.7027
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8748
Ames testNon AMES toxic0.8871
CarcinogenicityNon-carcinogens0.9596
BiodegradationNot ready biodegradable0.9828
Rat acute toxicity2.3839 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8115
hERG inhibition (predictor II)Inhibitor0.727
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Tabletoral10 mg
Tabletoral5 mg
Tablet, film coatedoral10 mg/1
Tablet, film coatedoral5 mg/1
Prices
Unit descriptionCostUnit
Fer-In-Sol 75 (15 Fe)mg/ml Solution 50ml Bottle19.0USD bottle
Fergon 100 240 (27 Fe)mg tablet Bottle15.99USD bottle
Fortabs 50-325-40 mg tablet0.4USD tablet
Hemocyte tablet0.33USD tablet
Hemocyte-f tablet0.33USD tablet
Feosol 45 mg tablet0.31USD tablet
Slow fe 142 mg tablet0.27USD tablet
Ferrous fumarate 324 mg tablet0.21USD tablet
Fer-in-sol 15 mg/ml drops0.19USD ml
Feosol 65 mg tablet0.18USD tablet
Ferretts 325 mg tablet0.14USD tablet
Fergon 27 mg tablet0.05USD tablet
Ferretts ips liquid0.05USD ml
Ferrous gluc 246 mg (27 mg) tablet0.04USD tablet
Ferrous gluconate 27 mg tablet0.04USD tablet
Ferrous sulfate 28 mg tablet0.04USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2208839 No2006-01-312015-12-27Canada
US6017927 No1998-11-192018-11-19Us
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
Water Solubility0.0729 mg/mLALOGPS
logP3.9ALOGPS
logP3.96ChemAxon
logS-3.7ALOGPS
pKa (Strongest Basic)8.88ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area32.78 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity106.06 m3·mol-1ChemAxon
Polarizability40.13 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Katsumi Saito, Masataka Katsuma, “Solifenacin transdermal preparation and method for enhancing transdermal permeation thereof.” U.S. Patent US20050181031, issued August 18, 2005.

US20050181031
General ReferencesNot Available
External Links
ATC CodesG04BD08G04CA53
AHFS Codes
  • 86:12.00
PDB EntriesNot Available
FDA labelDownload (68.6 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AclidiniumAclidinium may increase the anticholinergic activities of Solifenacin.
AprepitantThe serum concentration of Solifenacin can be increased when it is combined with Aprepitant.
BexaroteneThe serum concentration of Solifenacin can be decreased when it is combined with Bexarotene.
BosentanThe serum concentration of Solifenacin can be decreased when it is combined with Bosentan.
Botulinum Toxin Type ASolifenacin may increase the anticholinergic activities of Botulinum Toxin Type A.
Botulinum Toxin Type BSolifenacin may increase the anticholinergic activities of Botulinum Toxin Type B.
CimetropiumSolifenacin may increase the anticholinergic activities of Cimetropium Bromide.
CitalopramSolifenacin may increase the QTc-prolonging activities of Citalopram.
ConivaptanThe serum concentration of Solifenacin can be increased when it is combined with Conivaptan.
DabrafenibThe serum concentration of Solifenacin can be decreased when it is combined with Dabrafenib.
DasatinibThe serum concentration of Solifenacin can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Solifenacin can be decreased when it is combined with Deferasirox.
DofetilideSolifenacin may increase the QTc-prolonging activities of Dofetilide.
DronabinolSolifenacin may increase the tachycardic activities of Dronabinol.
EluxadolineSolifenacin may increase the activities of Eluxadoline.
FluconazoleThe metabolism of Solifenacin can be decreased when combined with Fluconazole.
FosaprepitantThe serum concentration of Solifenacin can be increased when it is combined with Fosaprepitant.
Fusidic AcidThe serum concentration of Solifenacin can be increased when it is combined with Fusidic Acid.
Glucagon recombinantThe risk or severity of adverse effects can be increased when Solifenacin is combined with Glucagon recombinant.
GoserelinSolifenacin may increase the QTc-prolonging activities of Goserelin.
IdelalisibThe serum concentration of Solifenacin can be increased when it is combined with Idelalisib.
Ipratropium bromideIpratropium bromide may increase the anticholinergic activities of Solifenacin.
ItoprideThe therapeutic efficacy of Itopride can be decreased when used in combination with Solifenacin.
ItraconazoleThe metabolism of Solifenacin can be decreased when combined with Itraconazole.
IvacaftorThe serum concentration of Solifenacin can be increased when it is combined with Ivacaftor.
KetoconazoleThe metabolism of Solifenacin can be decreased when combined with Ketoconazole.
LeuprolideSolifenacin may increase the QTc-prolonging activities of Leuprolide.
LuliconazoleThe serum concentration of Solifenacin can be increased when it is combined with Luliconazole.
MianserinMianserin may increase the anticholinergic activities of Solifenacin.
MifepristoneThe serum concentration of Solifenacin can be increased when it is combined with Mifepristone.
MirabegronThe risk or severity of adverse effects can be increased when Mirabegron is combined with Solifenacin.
MitotaneThe serum concentration of Solifenacin can be decreased when it is combined with Mitotane.
MorphineThe risk or severity of adverse effects can be increased when Solifenacin is combined with Morphine.
NelfinavirThe metabolism of Solifenacin can be decreased when combined with Nelfinavir.
NetupitantThe serum concentration of Solifenacin can be increased when it is combined with Netupitant.
PalbociclibThe serum concentration of Solifenacin can be increased when it is combined with Palbociclib.
PhenytoinThe metabolism of Solifenacin can be increased when combined with Phenytoin.
PosaconazoleThe metabolism of Solifenacin can be decreased when combined with Posaconazole.
Potassium ChlorideSolifenacin may increase the ulcerogenic activities of Potassium Chloride.
PramlintidePramlintide may increase the anticholinergic activities of Solifenacin.
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Solifenacin.
RamosetronSolifenacin may increase the activities of Ramosetron.
SecretinThe therapeutic efficacy of Secretin can be decreased when used in combination with Solifenacin.
SiltuximabThe serum concentration of Solifenacin can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Solifenacin can be increased when it is combined with Simeprevir.
St. John's WortThe serum concentration of Solifenacin can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Solifenacin can be increased when it is combined with Stiripentol.
SulpirideThe therapeutic efficacy of Sulpiride can be decreased when used in combination with Solifenacin.
TacrineThe therapeutic efficacy of Solifenacin can be decreased when used in combination with Tacrine.
TiotropiumSolifenacin may increase the anticholinergic activities of Tiotropium.
TocilizumabThe serum concentration of Solifenacin can be decreased when it is combined with Tocilizumab.
TopiramateThe risk or severity of adverse effects can be increased when Solifenacin is combined with Topiramate.
TrichlormethiazideThe serum concentration of Trichlormethiazide can be increased when it is combined with Solifenacin.
UmeclidiniumUmeclidinium may increase the anticholinergic activities of Solifenacin.
VoriconazoleThe metabolism of Solifenacin can be decreased when combined with Voriconazole.
Food InteractionsNot Available

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. 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. Ito Y, Oyunzul L, Yoshida A, Fujino T, Noguchi Y, Yuyama H, Ohtake A, Suzuki M, Sasamata M, Matsui M, Yamada S: Comparison of muscarinic receptor selectivity of solifenacin and oxybutynin in the bladder and submandibular gland of muscarinic receptor knockout mice. Eur J Pharmacol. 2009 Aug 1;615(1-3):201-6. doi: 10.1016/j.ejphar.2009.04.068. Epub 2009 May 13. [PubMed:19446545 ]
  4. Sinha S, Gupta S, Malhotra S, Krishna NS, Meru AV, Babu V, Bansal V, Garg M, Kumar N, Chugh A, Ray A: AE9C90CB: a novel, bladder-selective muscarinic receptor antagonist for the treatment of overactive bladder. Br J Pharmacol. 2010 Jul;160(5):1119-27. doi: 10.1111/j.1476-5381.2010.00752.x. [PubMed:20590605 ]
  5. Mansfield KJ, Chandran JJ, Vaux KJ, Millard RJ, Christopoulos A, Mitchelson FJ, Burcher E: Comparison of receptor binding characteristics of commonly used muscarinic antagonists in human bladder detrusor and mucosa. J Pharmacol Exp Ther. 2009 Mar;328(3):893-9. doi: 10.1124/jpet.108.145508. Epub 2008 Nov 24. [PubMed:19029429 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Phosphatidylinositol phospholipase c activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the 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. Sinha S, Gupta S, Malhotra S, Krishna NS, Meru AV, Babu V, Bansal V, Garg M, Kumar N, Chugh A, Ray A: AE9C90CB: a novel, bladder-selective muscarinic receptor antagonist for the treatment of overactive bladder. Br J Pharmacol. 2010 Jul;160(5):1119-27. doi: 10.1111/j.1476-5381.2010.00752.x. [PubMed:20590605 ]
  4. Mansfield KJ, Chandran JJ, Vaux KJ, Millard RJ, Christopoulos A, Mitchelson FJ, Burcher E: Comparison of receptor binding characteristics of commonly used muscarinic antagonists in human bladder detrusor and mucosa. J Pharmacol Exp Ther. 2009 Mar;328(3):893-9. doi: 10.1124/jpet.108.145508. Epub 2008 Nov 24. [PubMed:19029429 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
G-protein coupled acetylcholine receptor activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the 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. Sinha S, Gupta S, Malhotra S, Krishna NS, Meru AV, Babu V, Bansal V, Garg M, Kumar N, Chugh A, Ray A: AE9C90CB: a novel, bladder-selective muscarinic receptor antagonist for the treatment of overactive bladder. Br J Pharmacol. 2010 Jul;160(5):1119-27. doi: 10.1111/j.1476-5381.2010.00752.x. [PubMed:20590605 ]
  2. Mansfield KJ, Chandran JJ, Vaux KJ, Millard RJ, Christopoulos A, Mitchelson FJ, Burcher E: Comparison of receptor binding characteristics of commonly used muscarinic antagonists in human bladder detrusor and mucosa. J Pharmacol Exp Ther. 2009 Mar;328(3):893-9. doi: 10.1124/jpet.108.145508. Epub 2008 Nov 24. [PubMed:19029429 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Guanyl-nucleotide exchange factor activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the 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. Mansfield KJ, Chandran JJ, Vaux KJ, Millard RJ, Christopoulos A, Mitchelson FJ, Burcher E: Comparison of receptor binding characteristics of commonly used muscarinic antagonists in human bladder detrusor and mucosa. J Pharmacol Exp Ther. 2009 Mar;328(3):893-9. doi: 10.1124/jpet.108.145508. Epub 2008 Nov 24. [PubMed:19029429 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Phosphatidylinositol phospholipase c activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM5
Uniprot ID:
P08912
Molecular Weight:
60073.205 Da
References
  1. Mansfield KJ, Chandran JJ, Vaux KJ, Millard RJ, Christopoulos A, Mitchelson FJ, Burcher E: Comparison of receptor binding characteristics of commonly used muscarinic antagonists in human bladder detrusor and mucosa. J Pharmacol Exp Ther. 2009 Mar;328(3):893-9. doi: 10.1124/jpet.108.145508. Epub 2008 Nov 24. [PubMed:19029429 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation 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. 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 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on August 24, 2016 01:52