Identification
- Summary
Solifenacin is a muscarinic antagonist with antispasmodic properties used to treat urge urinary incontinence, urgency, and urinary frequency associated with an overactive bladder.
- Brand Names
- Vesicare
- Generic Name
- Solifenacin
- DrugBank Accession Number
- DB01591
- Background
Solifenacin is a competitive muscarinic receptor antagonist indicated to treat an overactive bladder with urinary incontinence, urgency, and frequency.3 It has a long duration of action as it is usually taken once daily.3
Solifenacin was granted FDA approval on 19 November 2004.3
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Solifenacin (DB01591)
- Weight
- Average: 362.473
Monoisotopic: 362.199428085 - Chemical Formula
- C23H26N2O2
- Synonyms
- Solifenacin
- Solifenacina
- External IDs
- YM-67905
- YM-905
Pharmacology
- Indication
Solifenacin tablets are indicated to treat an overactive bladder with urinary incontinence, urgency, and frequency.3
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 Used in combination for symptomatic treatment of Benign prostatic hyperplasia (bph) Combination Product in combination with: Tamsulosin (DB00706) •••••••••••• •••••••••• •••••••• •• •••••••••• ••••••••••• •••••• Used in combination to treat Benign prostatic hyperplasia (bph) Combination Product in combination with: Tamsulosin (DB00706) •••••••••••• •••••• ••••••• •••••••• •• •••••• ••••••••• •••••••••• •••••••• •• ••••••••••• ••••••• ••••••• ••••••• Treatment of Overactive bladder •••••••••••• ••••• - 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
Solifenacin antagonizes the M2 and M3 muscarinic receptors in the bladder to treat an overactive bladder.3,2 It has a long duration of action as it is usually taken once daily.3 Patients taking solifenacin should be aware of the risks of angioedema and anaphylaxis.3
- Mechanism of action
Solifenacin is a competitive muscarinic receptor antagonist.3 It has the highest affinity for M3, M1, and M2 muscarinic receptors.1 80% of the muscarinic receptors in the bladder are M2, while 20% are M3.2 Solifenacin's antagonism of the M3 receptor prevents contraction of the detrusor muscle, while antagonism of the M2 receptor may prevent contraction of smooth muscle in the bladder.2
Target Actions Organism AMuscarinic acetylcholine receptor M3 antagonistHumans UMuscarinic acetylcholine receptor M2 antagonistHumans UMuscarinic acetylcholine receptor M4 antagonistHumans UMuscarinic acetylcholine receptor M5 antagonistHumans UMuscarinic acetylcholine receptor M1 antagonistHumans - Absorption
Solifenacin is well absorbed in the duodenum, jejunum, and ileum but not the stomach.1 Absorption occurs via passive diffusion and so no transporters are involved.1 The mean oral bioavailability of solifenacin is 88%.1 The Tmax of solifenacin is 3-8 hours with a Css of 32.3ng/mL for a 5mg oral dose and 62.9ng/mL for a 10mg oral dose.3
- Volume of distribution
The volume of distribution of solifenacin is 600L.1
- Protein binding
Solifenacin is 93-96% protein bound in plasma, mainly to alpha-1-acid glycoprotein.1
- Metabolism
Solifenacin undergoes N-oxidation at the quinuclidin ring by cytochrome P450, though the exact enzymes are not revealed in the literature.1 The tetrahydroisoquinolone ring is 4R-hydroxylated by CYP3A4, CYP1A1, and CYP2D6.1 A 4R-hydroxy N-oxide metabolite is also formed by CYP3A4.1 Finally, solifenacin can undergo direct glucuronidation.1 Only solifenacin and the 4R-hydroxy metabolite are pharmacologically active.1
Hover over products below to view reaction partners
- Route of elimination
69.2±7.8% of a radiolabelled dose is recovered in the urine, 22.5±3.3% was recovered in feces, and 0.4±7.8% was recovered in exhaled air.1 18% of solifenacin is eliminated as the N-oxide metabolite, 9% is eliminated as the 4R-hydroxy N-oxide metabolite, and 8% is eliminated as the 4R-hydroxy metabolite.1
- Half-life
The elimination half life of solifenacin ranges from 33-85 hours.1
- Clearance
The clearance of solifenacin is 7-14L/h and a renal clearance of 0.67-1.51L/h.1
- 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
The LD50 of Solifenacin has yet to be determined.4
Signs of overdose include severe anticholinergic effects, mental status changes, and decreased consciousness.3 In case of overdose, treat patients with gastric lavage and supportive measures.3 Monitor patients with an ECG.3
- 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);">
- Not Available
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 softwareAbametapir The serum concentration of Solifenacin can be increased when it is combined with Abametapir. Abatacept The metabolism of Solifenacin can be increased when combined with Abatacept. Abiraterone The metabolism of Solifenacin can be decreased when combined with Abiraterone. Acebutolol The metabolism of Solifenacin can be decreased when combined with Acebutolol. Aceclofenac The risk or severity of hypertension can be increased when Solifenacin is combined with Aceclofenac. - Food Interactions
- Take with or without 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 Solifenacin hydrochloride Not Available 180468-39-7 YAUBKMSXTZQZEB-VROPFNGYSA-N Solifenacin succinate KKA5DLD701 242478-38-2 RXZMMZZRUPYENV-VROPFNGYSA-N - Product Images
- International/Other Brands
- Vesikur
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Act Solifenacin Tablet 5 mg Oral Actavis Pharma Company 2015-09-30 2018-04-30 Canada 
Act Solifenacin Tablet 10 mg Oral Actavis Pharma Company 2015-09-30 2018-04-30 Canada M-solifenacin Succinate Tablet 5 mg Oral Mantra Pharma Inc 2023-08-18 Not applicable Canada M-solifenacin Succinate Tablet 10 mg Oral Mantra Pharma Inc 2023-08-18 Not applicable Canada Prz-solifenacin Tablet 10 mg Oral Pharmaris Canada Inc 2020-11-13 Not applicable Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Ach-solifenacin Succinate Tablet 10 mg Oral Accord Healthcare Inc 2023-03-20 Not applicable Canada Ach-solifenacin Succinate Tablet 5 mg Oral Accord Healthcare Inc 2023-03-20 Not applicable Canada Apo-solifenacin Tablet 5 mg Oral Apotex Corporation 2018-09-05 Not applicable Canada Apo-solifenacin Tablet 10 mg Oral Apotex Corporation 2018-09-05 Not applicable Canada Auro-solifenacin Tablet 5 mg Oral Auro Pharma Inc 2016-01-04 Not applicable Canada - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Vesomni 6 mg/0,4 mg Tabletten mit veränderter Wirkstofffreisetzung Solifenacin succinate (6 mg) + Tamsulosin hydrochloride (400 mcg) Tablet, delayed release Oral Astellas Pharma Inc 2013-12-02 Not applicable Austria 
VESOMNİ 6 MG/0.4 MG DEĞİŞTİRİLMİŞ SALIMLI TABLET, 30 ADET Solifenacin succinate (6 mg) + Tamsulosin hydrochloride (0.4 mg) Tablet, delayed release Oral ASTELLAS PHARMA İLAÇ TİC. VE SAN. A.Ş. 2017-10-06 2022-12-21 Turkey 
VESOMNI® Solifenacin succinate (6 mg) + Tamsulosin hydrochloride (0.4 mg) Tablet Oral ASTELLAS FARMA COLOMBIA SAS 2017-05-23 Not applicable Colombia 
Categories
- ATC Codes
- G04BD08 — Solifenacin
- G04BD — Drugs for urinary frequency and incontinence
- G04B — UROLOGICALS
- G04 — UROLOGICALS
- G — GENITO URINARY SYSTEM AND SEX HORMONES
- Drug Categories
- Agents producing tachycardia
- Agents that produce hypertension
- Anticholinergic Agents
- Cholinergic Agents
- 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 Used in Benign Prostatic Hypertrophy
- Genito Urinary System and Sex Hormones
- Genitourinary Agents
- Heterocyclic Compounds, Fused-Ring
- Isoquinolines
- Muscarinic Antagonists
- Neurotransmitter Agents
- Potential QTc-Prolonging Agents
- QTc Prolonging Agents
- Quinuclidines
- Tetrahydroisoquinolines
- Urological Agents
- Urologicals
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as 1-phenyltetrahydroisoquinolines. These are compounds containing a phenyl group attached to the C1-atom of a tetrahydroisoquinoline moiety.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Tetrahydroisoquinolines
- Sub Class
- 1-phenyltetrahydroisoquinolines
- Direct Parent
- 1-phenyltetrahydroisoquinolines
- Alternative Parents
- Quinuclidines / Piperidines / Benzene and substituted derivatives / Carbamate esters / Trialkylamines / Organic carbonic acids and derivatives / Azacyclic compounds / Organopnictogen compounds / Organic oxides / Hydrocarbon derivatives show 1 more
- Substituents
- 1-phenyltetrahydroisoquinoline / Amine / Aromatic heteropolycyclic compound / Azacycle / Benzenoid / Carbamic acid ester / Carbonic acid derivative / Carbonyl group / Hydrocarbon derivative / Monocyclic benzene moiety show 10 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- A8910SQJ1U
- CAS number
- 242478-37-1
- InChI Key
- FBOUYBDGKBSUES-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[C@H]1CN2CCC1CC2)N1CCC2=CC=CC=C2[C@@H]1C1=CC=CC=C1
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 References
- Doroshyenko O, Fuhr U: Clinical pharmacokinetics and pharmacodynamics of solifenacin. Clin Pharmacokinet. 2009;48(5):281-302. doi: 10.2165/00003088-200948050-00001. [Article]
- Kreder KJ: Solifenacin. Urol Clin North Am. 2006 Nov;33(4):483-90, ix. doi: 10.1016/j.ucl.2006.06.008. [Article]
- FDA Approved Drug Products: Solifenacin Succinate Tablets [Link]
- Cayman Chemicals: Solifenacin MSDS [Link]
- External Links
- KEGG Drug
- D08522
- PubChem Compound
- 154059
- PubChem Substance
- 46506006
- ChemSpider
- 135771
- BindingDB
- 50370682
- 322167
- ChEBI
- 135530
- ChEMBL
- CHEMBL1734
- ZINC
- ZINC000003936683
- Therapeutic Targets Database
- DAP001129
- PharmGKB
- PA164783810
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Solifenacin
- FDA label
- Download (68.6 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 Active Not Recruiting Treatment Benign Prostatic Hyperplasia (BPH) / Overactive Bladder Syndrome (OABS) 1 4 Completed Not Available Cognitive Functioning 1 4 Completed Not Available Overactive Bladder Syndrome (OABS) 1 4 Completed Basic Science Detrusor Hyperreflexia / Overactive Bladder Syndrome (OABS) 1 4 Completed Prevention Dementia / Lower Urinary Tract Symptoms (LUTS) / Overactive Bladder Syndrome (OABS) / Urinary Urge Incontinence 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Astellas Pharma Inc.
- Bayer Healthcare
- Cypress Pharmaceutical Inc.
- Ivax Pharmaceuticals
- Lake Erie Medical and Surgical Supply
- MJ Nutritional
- Murfreesboro Pharmaceutical Nursing Supply
- Nature's Bounty
- Novartis AG
- Pharmics Inc.
- Physicians Total Care Inc.
- Redpharm Drug
- United Research Laboratories Inc.
- US Pharmaceutical Corp.
- Dosage Forms
Form Route Strength Tablet, film coated Oral Tablet, film coated Oral 5.00 mg Tablet, film coated Oral 3.8 MG Tablet, film coated Oral 7.5 MG Tablet, film coated Oral 10 MG Tablet, film coated Oral 5 MG Tablet, orally disintegrating Oral 10 MG Tablet, orally disintegrating Oral 5 MG Tablet, coated Oral 10 mg/1 Tablet, coated Oral 5 mg/1 Tablet, film coated, extended release Oral 10 mg/1 Solution Oral 1 MG/ML Tablet Oral 10 mg/1 Tablet Oral 5 mg/1 Tablet, film coated Oral 10.00 mg Tablet, film coated Oral 5.0 mg Tablet Oral Tablet Oral 10 mg Tablet Oral 5 mg Tablet Oral 5.000 mg Tablet, film coated Oral 10 mg/1 Tablet, film coated Oral 5 mg/1 Suspension Oral 1 mg/ml Suspension Oral 1 mg/1mL Suspension Oral Tablet Oral 5.00 mg Tablet Oral Tablet, delayed release Oral Tablet Oral 6 MG/0.4MG Tablet, coated Oral 10 mg Tablet, coated Oral 5 mg - Prices
Unit description Cost Unit Fer-In-Sol 75 (15 Fe)mg/ml Solution 50ml Bottle 19.0USD bottle Fergon 100 240 (27 Fe)mg tablet Bottle 15.99USD bottle Fortabs 50-325-40 mg tablet 0.4USD tablet Hemocyte tablet 0.33USD tablet Hemocyte-f tablet 0.33USD tablet Feosol 45 mg tablet 0.31USD tablet Slow fe 142 mg tablet 0.27USD tablet Ferrous fumarate 324 mg tablet 0.21USD tablet Fer-in-sol 15 mg/ml drops 0.19USD ml Feosol 65 mg tablet 0.18USD tablet Ferretts 325 mg tablet 0.14USD tablet Fergon 27 mg tablet 0.05USD tablet Ferretts ips liquid 0.05USD ml Ferrous gluc 246 mg (27 mg) tablet 0.04USD tablet Ferrous gluconate 27 mg tablet 0.04USD tablet Ferrous sulfate 28 mg tablet 0.04USD 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 CA2208839 No 2006-01-31 2015-12-27 Canada US6017927 Yes 2000-01-25 2019-05-19 US 
US9918970 No 2018-03-20 2031-05-18 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 134-136 https://www.trc-canada.com/product-detail/?S676701 - Predicted Properties
Property Value Source Water Solubility 0.0729 mg/mL ALOGPS logP 3.9 ALOGPS logP 3.96 Chemaxon logS -3.7 ALOGPS pKa (Strongest Basic) 8.88 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 2 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 32.78 Å2 Chemaxon Rotatable Bond Count 3 Chemaxon Refractivity 106.06 m3·mol-1 Chemaxon Polarizability 40.13 Å3 Chemaxon Number of Rings 5 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9706 Blood Brain Barrier + 0.6159 Caco-2 permeable - 0.6679 P-glycoprotein substrate Substrate 0.7801 P-glycoprotein inhibitor I Inhibitor 0.8572 P-glycoprotein inhibitor II Inhibitor 0.8611 Renal organic cation transporter Non-inhibitor 0.7498 CYP450 2C9 substrate Non-substrate 0.8311 CYP450 2D6 substrate Non-substrate 0.7264 CYP450 3A4 substrate Substrate 0.545 CYP450 1A2 substrate Non-inhibitor 0.8445 CYP450 2C9 inhibitor Non-inhibitor 0.8755 CYP450 2D6 inhibitor Non-inhibitor 0.8593 CYP450 2C19 inhibitor Non-inhibitor 0.7037 CYP450 3A4 inhibitor Non-inhibitor 0.7027 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.8748 Ames test Non AMES toxic 0.8871 Carcinogenicity Non-carcinogens 0.9596 Biodegradation Not ready biodegradable 0.9828 Rat acute toxicity 2.3839 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.8115 hERG inhibition (predictor II) Inhibitor 0.727
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-03di-0219000000-d464bb3d7b879ebe4aef Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-08fr-0069000000-b307beeb747761d75789 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-03di-0932000000-30e2cdcc0ae2b2109658 Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-08i0-0694000000-2350336c879143b3ba06 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-03di-2920000000-d863caa4275876dff20f Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-0560-0941000000-d32b110235ceae30f397 Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 202.4144716 predictedDarkChem Lite v0.1.0 [M-H]- 181.89146 predictedDeepCCS 1.0 (2019) [M+H]+ 203.5384716 predictedDarkChem Lite v0.1.0 [M+H]+ 184.24947 predictedDeepCCS 1.0 (2019) [M+Na]+ 203.1136716 predictedDarkChem Lite v0.1.0 [M+Na]+ 192.23601 predictedDeepCCS 1.0 (2019)
Targets
Build, predict & validate machine-learning models
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
- 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]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- G-protein coupled acetylcholine receptor activity
- Specific Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
- Gene Name
- CHRM2
- Uniprot ID
- P08172
- Uniprot Name
- Muscarinic acetylcholine receptor M2
- Molecular Weight
- 51714.605 Da
References
- 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. [Article]
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Guanyl-nucleotide exchange factor activity
- Specific Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
- Gene Name
- CHRM4
- Uniprot ID
- P08173
- Uniprot Name
- Muscarinic acetylcholine receptor M4
- Molecular Weight
- 53048.65 Da
References
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Phosphatidylinositol phospholipase c activity
- Specific Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
- Gene Name
- CHRM5
- Uniprot ID
- P08912
- Uniprot Name
- Muscarinic acetylcholine receptor M5
- Molecular Weight
- 60073.205 Da
References
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Phosphatidylinositol phospholipase c activity
- Specific Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
- Gene Name
- CHRM1
- Uniprot ID
- P11229
- Uniprot Name
- Muscarinic acetylcholine receptor M1
- Molecular Weight
- 51420.375 Da
References
- 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]
- 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. [Article]
- 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. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Vitamin d 24-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
- CYP1A1
- Uniprot ID
- P04798
- Uniprot Name
- Cytochrome P450 1A1
- Molecular Weight
- 58164.815 Da
References
- Doroshyenko O, Fuhr U: Clinical pharmacokinetics and pharmacodynamics of solifenacin. Clin Pharmacokinet. 2009;48(5):281-302. doi: 10.2165/00003088-200948050-00001. [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
- Doroshyenko O, Fuhr U: Clinical pharmacokinetics and pharmacodynamics of solifenacin. Clin Pharmacokinet. 2009;48(5):281-302. doi: 10.2165/00003088-200948050-00001. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- 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
- Doroshyenko O, Fuhr U: Clinical pharmacokinetics and pharmacodynamics of solifenacin. Clin Pharmacokinet. 2009;48(5):281-302. doi: 10.2165/00003088-200948050-00001. [Article]
- Swart PJ, Krauwinkel WJ, Smulders RA, Smith NN: Pharmacokinetic effect of ketoconazole on solifenacin in healthy volunteers. Basic Clin Pharmacol Toxicol. 2006 Jul;99(1):33-6. doi: 10.1111/j.1742-7843.2006.pto_285.x. [Article]
- FDA Approved Drug Products: Solifenacin Succinate Tablets [Link]
Carriers
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Not Available
- Specific Function
- Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in...
Components:
References
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55