Identification

Name
Solifenacin
Accession Number
DB01591  (APRD00168)
Type
Small Molecule
Groups
Approved
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.

Structure
Thumb
Synonyms
  • Solifenacin
  • Solifenacina
External IDs
YM-67905 / YM-905
Product Ingredients
IngredientUNIICASInChI Key
Solifenacin hydrochlorideNot AvailableNot AvailableYAUBKMSXTZQZEB-VROPFNGYSA-N
Solifenacin succinateKKA5DLD701242478-38-2RXZMMZZRUPYENV-VROPFNGYSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Act SolifenacinTablet5 mgOralActavis Pharma Company2015-09-30Not applicableCanada
Act SolifenacinTablet10 mgOralActavis Pharma Company2015-09-30Not applicableCanada
Sandoz SolifenacinTablet5 mgOralSandoz Canada Incorporated2015-09-30Not applicableCanada
Sandoz SolifenacinTablet10 mgOralSandoz Canada Incorporated2015-09-30Not applicableCanada
SolifenacinTablet10 mgOralPro Doc Limitee2016-10-27Not applicableCanada
SolifenacinTablet10 mgOralSanis Health Inc2016-11-03Not applicableCanada
SolifenacinTablet5 mgOralSanis Health Inc2016-11-03Not applicableCanada
SolifenacinTablet5 mgOralPro Doc Limitee2016-10-27Not applicableCanada
Solifenacin SuccinateTablet5 mgOralJubilant Generics LimitedNot applicableNot applicableCanada
Solifenacin SuccinateTablet10 mgOralJubilant Generics LimitedNot applicableNot applicableCanada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Ach-solifenacin SuccinateTablet10 mgOralAccord Healthcare LimitedNot applicableNot applicableCanada
Ach-solifenacin SuccinateTablet5 mgOralAccord Healthcare LimitedNot applicableNot applicableCanada
Apo-solifenacinTablet10 mgOralApotex CorporationNot applicableNot applicableCanada
Apo-solifenacinTablet5 mgOralApotex CorporationNot applicableNot applicableCanada
Auro-solifenacinTablet5 mgOralAuro Pharma Inc2016-01-04Not applicableCanada
Auro-solifenacinTablet10 mgOralAuro Pharma Inc2016-01-04Not applicableCanada
Dom-solifenacinTablet10 mgOralDominion PharmacalNot applicableNot applicableCanada
Dom-solifenacinTablet5 mgOralDominion PharmacalNot applicableNot applicableCanada
Gpc-solifenacinTablet10 mgOralGeneric Partners (Canada) Inc.Not applicableNot applicableCanada
Gpc-solifenacinTablet5 mgOralGeneric Partners (Canada) Inc.Not applicableNot applicableCanada
International/Other Brands
Vesikur
Categories
UNII
A8910SQJ1U
CAS number
242478-37-1
Weight
Average: 362.473
Monoisotopic: 362.199428085
Chemical Formula
C23H26N2O2
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

Pharmacology

Indication

For the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and urinary frequency.

Associated Conditions
Pharmacodynamics

Solifenacin 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 action

Solifenacin 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.

TargetActionsOrganism
AMuscarinic acetylcholine receptor M3
antagonist
Human
UMuscarinic acetylcholine receptor M1
antagonist
Human
UMuscarinic acetylcholine receptor M2
antagonist
Human
UMuscarinic acetylcholine receptor M4
antagonist
Human
UMuscarinic acetylcholine receptor M5
antagonist
Human
Absorption

The absolute bioavailability of solifenacin is approximately 90%, and plasma concentrations of solifenacin are proportional to the dose administered.

Volume of distribution
  • 600 L
Protein binding

Solifenacin 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.

Route of elimination

The primary pathway for elimination is by way of CYP3A4; however, alternate metabolic pathways exist.

Half life

The elimination half-life of solifenacin following chronic dosing is approximately 45-68 hours.

Clearance
Not Available
Toxicity

Overdosage 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
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe metabolism of (R)-warfarin can be decreased when combined with Solifenacin.
(S)-WarfarinThe metabolism of (S)-Warfarin can be decreased when combined with Solifenacin.
1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic AcidThe risk or severity of hypertension can be increased when Solifenacin is combined with 1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid.
1-benzylimidazoleThe risk or severity of hypertension can be increased when Solifenacin is combined with 1-benzylimidazole.
1,10-PhenanthrolineThe therapeutic efficacy of Solifenacin can be decreased when used in combination with 1,10-Phenanthroline.
2,5-Dimethoxy-4-ethylamphetamineThe risk or severity of hypertension can be increased when 2,5-Dimethoxy-4-ethylamphetamine is combined with Solifenacin.
2,5-Dimethoxy-4-ethylthioamphetamineThe risk or severity of hypertension can be increased when Solifenacin is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3,4-MethylenedioxyamphetamineThe risk or severity of hypertension can be increased when 3,4-Methylenedioxyamphetamine is combined with Solifenacin.
3,5-diiodothyropropionic acidThe metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Solifenacin.
4-Bromo-2,5-dimethoxyamphetamineThe risk or severity of hypertension can be increased when 4-Bromo-2,5-dimethoxyamphetamine is combined with Solifenacin.
Food Interactions
Not 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 References
Not Available
External Links
KEGG Drug
D08522
PubChem Compound
154059
PubChem Substance
46506006
ChemSpider
135771
BindingDB
50344284
ChEBI
135530
ChEMBL
CHEMBL1734
Therapeutic Targets Database
DAP001129
PharmGKB
PA164783810
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Solifenacin
ATC Codes
G04BD08 — SolifenacinG04CA53 — Tamsulosin and solifenacin
AHFS Codes
  • 86:12.04 — Antimuscarinics
FDA label
Download (68.6 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableBioavailability of Solifenacin Succinate / Healthy Volunteers / Pharmacokinetics of Solifenacin Succinate1
1CompletedNot AvailableHealthy Volunteers / Pharmacokinetics of Solifenacin Succinate1
1CompletedBasic ScienceBenign Prostatic Hyperplasia (BPH) / Healthy Volunteers / Lower Urinary Tract Symptoms (LUTS) / Phase 11
1CompletedBasic ScienceBioavailability / Healthy Volunteers / Phase 11
1CompletedBasic ScienceDrug Drug Interaction (DDI) / Healthy Volunteers1
1CompletedBasic ScienceDrug Drug Interaction (DDI) / Healthy Volunteers / Pharmacokinetics2
1CompletedBasic ScienceEC905 / Healthy Volunteers / Multiple Dose / Pharmacokinetics1
1CompletedBasic ScienceEC905 / Healthy Volunteers / Pharmacokinetics1
1CompletedBasic ScienceHealthy Volunteers / Pharmacokinetics of Mirabegron1
1CompletedOtherNeurogenic Detrusor Overactivity / Urinary Bladder, Overactive1
1CompletedTreatmentBenign Prostatic Hyperplasia (BPH) / LUTS / Urinary Bladder, Overactive1
1CompletedTreatmentUrinary Bladder, Overactive2
1TerminatedTreatmentHealthy Volunteers1
1, 2RecruitingTreatmentSurgical Treatment of Urge Incontinence1
1, 2RecruitingTreatmentUrge Urinary Incontinence1
2CompletedNot AvailableDetrusor Underactivity / Urinary Bladder, Overactive1
2CompletedDiagnosticUrinary Bladder, Overactive1
2CompletedTreatmentBladder Outlet Obstruction / Lower Urinary Tract Symptoms (LUTS)1
2CompletedTreatmentLower Urinary Tract Symptoms (LUTS) / Prostatic Hyperplasia1
2CompletedTreatmentSigns and Symptoms / Urinary Bladder Diseases / Urinary Bladder, Overactive / Urologic Diseases / Urological Manifestations1
2RecruitingSupportive CareCancer, Breast / Menopausal Hot Flushes1
2RecruitingTreatmentUrinary Bladder, Overactive2
2, 3CompletedTreatmentDetrusor Uninhibited Activity / Incontinence / Nocturia / Quality of Life / Urinary Frequency / Urination urgency of1
3CompletedTreatmentNeurogenic Detrusor Overactivity1
3CompletedTreatmentNeurogenic Detrusor Overactivity / Pediatric1
3CompletedTreatmentUrge Urinary Incontinence / Urinary Bladder, Overactive1
3CompletedTreatmentUrgency Incontinence / Urinary Bladder Diseases\Urologic Diseases / Urinary Bladder, Overactive2
3CompletedTreatmentUrinary Bladder Diseases / Urinary Bladder, Overactive / Urologic Diseases2
3CompletedTreatmentUrinary Bladder, Overactive9
3CompletedTreatmentUrinary Bladder, Overactive / Urinary Incontinence (UI)1
3RecruitingTreatmentBenign Prostatic Hyperplasia (BPH)1
3RecruitingTreatmentBenign Prostatic Hyperplasia (BPH) / Lower Urinary Tract Symptoms (LUTS)1
3RecruitingTreatmentParkinson's Disease (PD) / Urinary Bladder, Overactive1
3TerminatedTreatmentUrinary Bladder, Overactive2
4Active Not RecruitingOtherUrinary Incontinence (UI)1
4CompletedNot AvailableCognition1
4CompletedNot AvailableUrinary Bladder, Overactive1
4CompletedBasic ScienceDetrusor Overactivity / Urinary Bladder, Overactive1
4CompletedTreatmentBenign Prostatic Hyperplasia (BPH) / Benign Prostatic Hypertrophy (BPH) / Urinary Bladder, Overactive1
4CompletedTreatmentBenign Prostatic Hyperplasia (BPH) / Lower Urinary Tract Symptoms (LUTS) / Urinary Bladder, Overactive1
4CompletedTreatmentBenign Prostatic Hyperplasia (BPH) / Photoselective Vaporization Prostatectomy / Transurethral Resection of Prostate / Urinary Bladder, Overactive1
4CompletedTreatmentDisseminated Sclerosis / Neurogenic Bladder Dysfunction / Spinal Cord Diseases1
4CompletedTreatmentFlank Pain / Urinary Bladder, Overactive1
4CompletedTreatmentOveractive Bladder in Parkinson's Disease1
4CompletedTreatmentPostmenopausal Disorder / Urinary Bladder, Overactive / Urination Disorders1
4CompletedTreatmentRelieve of Ureteral Stent Symptoms1
4CompletedTreatmentStress Urinary Incontinence (SUI) / Urgency Urinary Incontinence1
4CompletedTreatmentUrge Incontinence / Urinary Bladder, Overactive / Urinary Incontinence (UI)1
4CompletedTreatmentUrinary Bladder, Overactive13
4CompletedTreatmentUrinary Incontinence (UI)2
4RecruitingTreatmentBacillus Calmette-Guerin (BCG) Cystitis / Intra-vesical Instillation / Non-Muscle-invasive Bladder Cancer (NMIBC)1
4RecruitingTreatmentUrinary Bladder, Overactive2
4TerminatedTreatmentOver-Active Bladder1
4TerminatedTreatmentPelvic Organ Prolapse (POP)1
4TerminatedTreatmentUrinary Bladder, Overactive1
4Unknown StatusTreatmentUrinary Bladder, Overactive1
4Unknown StatusTreatmentUrinary Tract Infections (UTIs)1
4WithdrawnTreatmentParkinson's Disease (PD) / Urinary Incontinence (UI)1
4WithdrawnTreatmentUrge Incontinence / Urinary Bladder, Overactive / Urinary Urge1
Not AvailableActive Not RecruitingNot AvailableUrinary Bladder, Overactive1
Not AvailableCompletedNot AvailableEnuresis, Nocturnal, 2 (Disorder)1
Not AvailableCompletedNot AvailableLower Urinary Tract Predominant Storage Symptoms1
Not AvailableCompletedNot AvailableLower Urinary Tract Symptoms (LUTS) / Urinary Bladder, Overactive1
Not AvailableCompletedNot AvailableUrinary Bladder Diseases / Urinary Bladder, Overactive / Urologic Diseases1
Not AvailableCompletedNot AvailableUrinary Bladder, Overactive5
Not AvailableCompletedBasic ScienceUrethral Sphincter Activity1
Not AvailableCompletedSupportive CareUrge Urinary Incontinence1
Not AvailableCompletedTreatmentAntimuscarinic Drug1
Not AvailableCompletedTreatmentIncontinence / Post Micturition Dribble / Postvoid Dribbling1
Not AvailableCompletedTreatmentUrinary Incontinence (UI)2
Not AvailableRecruitingTreatmentUrinary Bladder, Overactive1
Not AvailableTerminatedTreatmentIncontinence1
Not AvailableUnknown StatusNot AvailableUrinary Bladder, Overactive1
Not AvailableUnknown StatusTreatmentUrinary Bladder, Overactive2

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
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)
CA2208839No2006-01-312015-12-27Canada
US6017927Yes2000-01-252019-05-19Us

Properties

State
Solid
Experimental Properties
Not 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 RuleNoChemAxon
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)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

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 / Quinuclidine / Monocyclic benzene moiety / Piperidine / Benzenoid / Carbamic acid ester / Carbonic acid derivative / Tertiary amine / Tertiary aliphatic amine / Azacycle
show 10 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not 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...
Gene Name
CHRM3
Uniprot ID
P20309
Uniprot Name
Muscarinic acetylcholine receptor M3
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...
Gene Name
CHRM1
Uniprot ID
P11229
Uniprot Name
Muscarinic acetylcholine receptor M1
Molecular Weight
51420.375 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [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...
Gene Name
CHRM2
Uniprot ID
P08172
Uniprot Name
Muscarinic acetylcholine receptor M2
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...
Gene Name
CHRM4
Uniprot ID
P08173
Uniprot Name
Muscarinic acetylcholine receptor M4
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...
Gene Name
CHRM5
Uniprot ID
P08912
Uniprot Name
Muscarinic acetylcholine receptor M5
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
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]

Drug created on June 13, 2005 07:24 / Updated on December 18, 2018 05:46