Propiverine
Identification
- Summary
Propiverine is an antimuscarinic agent used to treat urinary incontinence or increased urinary frequency or urgency.
- Brand Names
- Mictoryl
- Generic Name
- Propiverine
- DrugBank Accession Number
- DB12278
- Background
Propiverine is a widely used antimuscarinic drug with a mixed mode of action in the treatment of symptoms associated with overactive bladder (OAB) 1.
Overactive bladder (OAB) is a chronic condition of the lower urinary tract characterized by urinary urgency, increased frequency of urination, and nocturia (frequent waking during the night to urinate). OAB has a negative impact on quality of life and may lead to leakage and inconvenient urinary accidents 15, 16. Overactive bladder syndrome affects millions of elderly individuals in the United States and shows equal prevalence in men and women. The impact of OAB on quality of life is sometimes devastating, especially to elderly patients with other medical conditions 16.
Propiverine hydrochloride is a bladder detrusor muscle relaxant drug with dual antimuscarinic and calcium-modulating properties for the treatment of OAB 7.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
- Weight
- Average: 367.4813
Monoisotopic: 367.214743799 - Chemical Formula
- C23H29NO3
- Synonyms
- Propiverina
- Propiverine
Pharmacology
- Indication
Indicated for symptomatic treatment of urinary incontinence and/or increased urinary frequency and urgency in patients with overactive bladder (OAB) 6. Propiverine may also be used in patients with neurogenic bladder as a result of spinal cord injury 5.
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 Symptomatic treatment of Urinary frequency •••••••••••• Symptomatic treatment of Urinary incontinence •••••••••••• Symptomatic treatment of Urinary urgency •••••••••••• - Contraindications & Blackbox Warnings
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- Pharmacodynamics
Propiverine hydrochloride inhibits abnormal contractions of bladder smooth muscle in vivo through not only its anticholinergic activity but also its concurrent calcium antagonistic activity 8. Through the above-mentioned mechanism, propiverine is able to relieve the symptoms of overactive bladder.
In animal models, this administration of this drug leads to a dose-dependent decrease in intravesical pressure of the bladder and an increase in bladder capacity 6. In patients with symptoms of OAB resulting from idiopathic detrusor muscle overactivity (IDO) or neurogenic detrusor overactivity (NDO), propiverine showed dose-dependent efficacy and tolerability 1.
- Mechanism of action
Propiverine demonstrates both anticholinergic and calcium-modulating properties. The efferent connection of the pelvic nerve is inhibited due to the anticholinergic action exerted by this drug, leading to relaxation of bladder smooth muscle. Propiverine blocks calcium ion influx and modulates the intracellular calcium in urinary bladder smooth muscle cells, resulting in the inhibition of muscle spasm 6. The bladder contains several muscarinic receptors. Acetylcholine is the main contractile neurotransmitter in the human bladder detrusor muscle, and antimuscarinics such as propiverine exert their effects by competitively inhibiting the binding of acetylcholine at muscarinic receptors on detrusor smooth muscle cells and other structures within the bladder wall 17. In one study, After oral treatment with propiverine, the bladder showed the highest concentration of M-2, indicating a targeted distribution of this metabolite into the bladder. Therefore, muscarinic receptor-2 may highly contribute to the relatively selective and long-lasting occupation of bladder muscarinic receptors after oral ingestion of propiverine 19.
Target Actions Organism AMuscarinic acetylcholine receptor M1 antagonistHumans AMuscarinic acetylcholine receptor M2 antagonistHumans AMuscarinic acetylcholine receptor M3 antagonistHumans AMuscarinic acetylcholine receptor M5 Not Available Humans AVoltage-dependent L-type calcium channel subunit alpha-1C antagonistHumans AAlpha-1A adrenergic receptor antagonistHumans UMuscarinic acetylcholine receptor M4 antagonistHumans - Absorption
Propiverine is rapidly absorbed from the gastrointestinal tract with maximum plasma concentrations attained after 2.3 hours. the mean absolute bioavailability of mictonorm 15 mg tablets (propiverine) is 40.5 %. It undergoes heavy first-pass metabolism in the liver 6.
- Volume of distribution
In one study, the volume of distribution was calculated in 21 healthy volunteers after intravenous (IV) administration of propiverine hydrochloride was measured to range from 125 to 4731 (average 2791) indicating, that a large amount of available propiverine is distributed to peripheral compartments 13.
- Protein binding
90-95% for the parent compound and about 60% for the main metabolite 13.
- Metabolism
The major metabolites were found to be as follows; 4-piperidyl diphenylpropoxyacetate (DM-P-4), 1-methyl-4-piperidyl benzilate (Dpr-P-4) and 1-methyl-4-piperidyl diphenyl-(2 carboxy) ethoxyacetate (ω-COOH-P-4) in the liver, Dpt-p-4, DM-P-4 in the kidney, and DM-P-4, DPr-P-4 in the lung 12. In the same pharmacokinetic study, All pharmacologically active compounds such as the unchanged compound, 1-methyl-4-piperidyl benzilate N-oxide (DPr-P-4 (N→O)), Dpt-p-4 and 1-methyl-4-piperidyl diphenylpropoxyacetate N-oxide (P-4 (N→O)) were present in the urinary bladder, a target organ for P-4, at higher concentrations than in the plasma 12.
Propiverine is metabolized by both intestinal and hepatic enzymes. The main metabolic pathway involves the oxidation of the piperidyl-N _and is mediated by _CYP 3A4 and _flavin-containing monooxygenases (FMO) _1 and 3 and results in the formation of the second main metabolite M-5, the plasma concentration of which is greater in concentration that of the parent substance propiverine. Four metabolites have been identified in the urine following propiverine ingestion; 3 them are pharmacologically active metabolites that may contribute to its therapeutic effect (M-5, M-6, M-23) 14.
The mean absolute bioavailability of propiverine IR 15 mg is 40.5% 6.
- Route of elimination
Following the ingestion of 30 mg propiverine, 60% radioactivity was recovered in urine and 21% was recovered in feces within 12 days. Less than 1% of an oral dose is excreted unchanged in the urine 6.
- Half-life
In three studies including a total of 37 healthy volunteers mean elimination half-life was 14.1, 20.1 and 22.1 hours, respectively 6.
- Clearance
Mean total clearance after single dose administration of 30 mg is 371 mL/min (191 – 870 mL/min) 6.
- Adverse Effects
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- Toxicity
The most common adverse reactions reported in patients treated with propiverine include dry mouth, headache, accommodation disorder, constipation, abdominal pain, dyspepsia and fatigue 6.
Propiverine may cause drowsiness and blurred vision. This may impair the ability to exert activities that require mental alertness such as operating a motor vehicle or other machinery, or to perform hazardous work while taking this drug 6.
There have been reports of QT interval prolongation with antimuscarinic medications in the same class of drugs of propiverine hydrochloride. Some drugs that may cause QT/QTc interval prolongation may increase the risk of a rare, but serious ventricular arrhythmia called torsades de pointes. Patients at risk for QT/QTc interval prolongation, such as those with diagnosed heart failure, long QT syndrome, recent significant hypokalemia episodes or receiving other drugs known to prolong QT/QTc, should be closely monitored while treated with propiverine. Patients who experience prolonged QT/QTc or symptoms of possible arrhythmias including dizziness, palpitations or fainting should be electrocardiographically evaluated and monitored for electrolyte disturbances 6.
Propiverine, like other anticholinergics, induces mydriasis. Therefore, the risk to induce acute angle-closure glaucoma in individuals predisposed with narrow angles of the anterior chamber may be increased. Drugs of this class, including propiverine, have been reported to induce or precipitate acute angle-closure glaucoma 6.
No clinical data are available on the use of propiverine in pregnant women. Studies in animals have shown reproductive toxicity 6.
- 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 softwareAbacavir Abacavir may decrease the excretion rate of Propiverine which could result in a higher serum level. Abametapir The serum concentration of Propiverine can be increased when it is combined with Abametapir. Acebutolol Acebutolol may increase the orthostatic hypotensive activities of Propiverine. Aceclofenac The risk or severity of hypertension can be increased when Aceclofenac is combined with Propiverine. Acemetacin The risk or severity of hypertension can be increased when Propiverine is combined with Acemetacin. - Food Interactions
- Take at the same time every day.
- Take separate from meals. PrMictoryl Pediatric (propiverine hydrochloride) tablets should be taken at least 1 hour before meals as high-fat meals reduce the bioavailability of PrMictoryl.
- Take with or without food. Mictoryl (propiverine hydrochloride) modified-release capsules can be taken with or without food as food does not affect its bioavailability.
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 Propiverine hydrochloride DC4GZD10H3 54556-98-8 KFUJMHHNLGCTIJ-UHFFFAOYSA-N - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Mictoryl Capsule, extended release 45 mg Oral Duchesnay Inc. 2017-05-08 Not applicable Canada Mictoryl Capsule, extended release 30 mg Oral Duchesnay Inc. 2017-05-08 Not applicable Canada Mictoryl Pediatric Tablet 5 mg Oral Duchesnay Inc. 2017-04-13 Not applicable Canada
Categories
- ATC Codes
- G04BD06 — Propiverine
- Drug Categories
- Acids, Carbocyclic
- Adrenergic alpha-1 Receptor Antagonists
- Adrenergic alpha-Antagonists
- Adrenergic Antagonists
- Agents producing tachycardia
- Agents that produce hypertension
- Anticholinergic Agents
- Autonomic Agents
- Cholinergic Agents
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Substrates
- Diphenylacetic Acids
- Drugs for Urinary Frequency and Incontinence
- Drugs that are Mainly Renally Excreted
- Genito Urinary System and Sex Hormones
- Genitourinary Agents
- Hydroxy Acids
- Muscarinic Antagonists
- Neurotransmitter Agents
- Parasympatholytics
- Peripheral Nervous System Agents
- Phenylacetates
- Urological Agents
- Urologicals
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as diphenylmethanes. These are compounds containing a diphenylmethane moiety, which consists of a methane wherein two hydrogen atoms are replaced by two phenyl groups.
- Kingdom
- Organic compounds
- Super Class
- Benzenoids
- Class
- Benzene and substituted derivatives
- Sub Class
- Diphenylmethanes
- Direct Parent
- Diphenylmethanes
- Alternative Parents
- Benzylethers / Piperidines / Trialkylamines / Carboxylic acid esters / Amino acids and derivatives / Monocarboxylic acids and derivatives / Dialkyl ethers / Azacyclic compounds / Organopnictogen compounds / Organic oxides show 2 more
- Substituents
- Amine / Amino acid or derivatives / Aromatic heteromonocyclic compound / Azacycle / Benzylether / Carbonyl group / Carboxylic acid derivative / Carboxylic acid ester / Dialkyl ether / Diphenylmethane show 13 more
- Molecular Framework
- Aromatic heteromonocyclic compounds
- External Descriptors
- diarylmethane (CHEBI:8493)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 468GE2241L
- CAS number
- 60569-19-9
- InChI Key
- QPCVHQBVMYCJOM-UHFFFAOYSA-N
- InChI
- InChI=1S/C23H29NO3/c1-3-18-26-23(19-10-6-4-7-11-19,20-12-8-5-9-13-20)22(25)27-21-14-16-24(2)17-15-21/h4-13,21H,3,14-18H2,1-2H3
- IUPAC Name
- 1-methylpiperidin-4-yl 2,2-diphenyl-2-propoxyacetate
- SMILES
- CCCOC(C(=O)OC1CCN(C)CC1)(C1=CC=CC=C1)C1=CC=CC=C1
References
- General References
- McKeage K: Propiverine: a review of its use in the treatment of adults and children with overactive bladder associated with idiopathic or neurogenic detrusor overactivity, and in men with lower urinary tract symptoms. Clin Drug Investig. 2013 Jan;33(1):71-91. doi: 10.1007/s40261-012-0046-9. [Article]
- Haustein KO, Huller G: On the pharmacokinetics and metabolism of propiverine in man. Eur J Drug Metab Pharmacokinet. 1988 Apr-Jun;13(2):81-90. [Article]
- Chess-Williams R: Muscarinic receptors of the urinary bladder: detrusor, urothelial and prejunctional. Auton Autacoid Pharmacol. 2002 Jun;22(3):133-45. [Article]
- Maruyama S, Oki T, Otsuka A, Shinbo H, Ozono S, Kageyama S, Mikami Y, Araki I, Takeda M, Masuyama K, Yamada S: Human muscarinic receptor binding characteristics of antimuscarinic agents to treat overactive bladder. J Urol. 2006 Jan;175(1):365-9. [Article]
- Sakakibara F, Takahama K, Nanri M, Sasaki E: Pharmacological Properties of Propiverine Contribute to Improving Lower Urinary Tract Dysfunctions in Rats with Spinal Cord Injuries. Drug Res (Stuttg). 2016 Sep;66(9):464-469. doi: 10.1055/s-0042-110855. Epub 2016 Oct 17. [Article]
- Mictoryl monograph [Link]
- CDR CLINICAL REVIEW REPORT FOR MICTORYL [Link]
- The Efficacy and Safety of Propiverine Hydrochloride in Patients with Overactive Bladder Symptoms Who Poorly Responded to Previous Anticholinergic Agents [Link]
- Propiverine hydrochloride [Link]
- Propiverine Hydrochloride PubChem [Link]
- Public assessment report [Link]
- Pharmacokinetic Studies on Propiverine Hydrochloride [Link]
- Mictonorm [Link]
- The muscarinic receptor antagonist propiverine exhibits α1-adrenoceptor antagonism in human prostate and porcine trigonum [Link]
- Mayo Clinic, Overactive Bladder [Link]
- Maximizing the Treatment of Overactive Bladder in the Elderly [Link]
- Muscarinic receptor antagonists for overactive bladder [Link]
- Propiverine overview [Link]
- The N-Oxide Metabolite Contributes to Bladder Selectivity Resulting from Oral Propiverine: Muscarinic Receptor Binding and Pharmacokinetics [Link]
- External Links
- Human Metabolome Database
- HMDB0041999
- KEGG Drug
- D08441
- KEGG Compound
- C07852
- PubChem Compound
- 4942
- PubChem Substance
- 347828547
- ChemSpider
- 4773
- 55175
- ChEBI
- 8493
- ChEMBL
- CHEMBL1078261
- ZINC
- ZINC000001530934
- Wikipedia
- Propiverine
- MSDS
- Download (168 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Treatment Overactive Bladder Syndrome (OABS) 2 3 Completed Treatment Children / Overactive Bladder Syndrome (OABS) / Urinary Incontinence (UI) 1 3 Completed Treatment Detrusor Hyperreflexia / Neurogenic Bladder / Neurogenic Bladder Disorder / Urinary Bladder Disorder, Neurogenic / Urinary Bladder Neurogenic Dysfunction / Urinary Incontinence (UI) / Urological Diseases 1 3 Completed Treatment Overactive Bladder Syndrome (OABS) 2 2 Completed Not Available Overactive Bladder Syndrome (OABS) 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet, coated Oral 5 mg Tablet, coated Oral 10 MG Capsule, delayed release Oral Tablet, coated Oral Tablet, coated Oral 15 mg Tablet, film coated Oral Tablet, sugar coated Oral Tablet, coated Oral 15.000 mg Capsule, delayed release Oral 30 mg Capsule, delayed release Oral 45 mg Tablet, film coated Oral 15 MG Capsule, coated pellets Oral 30 mg Capsule, coated pellets Oral 45 mg Tablet Oral 15 mg Capsule, extended release Oral 30 mg Capsule, extended release Oral 45 mg Tablet Oral 5 mg Capsule Oral 30.000 mg Tablet, film coated Oral 5 MG - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 224-226 http://www.chemicalbook.com/ChemicalProductProperty_EN_CB3855472.htm boiling point (°C) 484.2 MSDS water solubility 5mg/mL http://www.chemicalbook.com/ChemicalProductProperty_EN_CB3855472.htm - Predicted Properties
Property Value Source Water Solubility 0.00635 mg/mL ALOGPS logP 4.16 ALOGPS logP 4.25 Chemaxon logS -4.8 ALOGPS pKa (Strongest Basic) 8.72 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 3 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 38.77 Å2 Chemaxon Rotatable Bond Count 8 Chemaxon Refractivity 107.73 m3·mol-1 Chemaxon Polarizability 41.88 Å3 Chemaxon Number of Rings 3 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS splash10-004i-1190000000-eef1e2fe37269ab08043 Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-08fr-0096000000-d36dff140826b40bf5e1 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-02t9-2495000000-4e30bce9de75bef20200 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-004i-0091000000-67d1c82932916769cd81 Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-02t9-1944000000-ea170fe1ae59df879c8b Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-016v-9620000000-055431a7b1c850d72e39 Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-001v-0971000000-2a6f75543ebf58d7c2f9 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]- 206.4490489 predictedDarkChem Lite v0.1.0 [M-H]- 193.0164 predictedDeepCCS 1.0 (2019) [M+H]+ 206.4250489 predictedDarkChem Lite v0.1.0 [M+H]+ 195.74474 predictedDeepCCS 1.0 (2019) [M+Na]+ 206.1563489 predictedDarkChem Lite v0.1.0 [M+Na]+ 204.26714 predictedDeepCCS 1.0 (2019)
Targets
![](https://go.drugbank.com/assets/locked/DrugTargets2-682eb846d210ae4bf33ca03febccfb57bb1c61318e699b729e5df4dfab2c5b67.png)
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Phosphatidylinositol phospholipase c activity
- Specific Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
- Gene Name
- CHRM1
- Uniprot ID
- P11229
- Uniprot Name
- Muscarinic acetylcholine receptor M1
- Molecular Weight
- 51420.375 Da
References
- Maruyama S, Oki T, Otsuka A, Shinbo H, Ozono S, Kageyama S, Mikami Y, Araki I, Takeda M, Masuyama K, Yamada S: Human muscarinic receptor binding characteristics of antimuscarinic agents to treat overactive bladder. J Urol. 2006 Jan;175(1):365-9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- 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
- Maruyama S, Oki T, Otsuka A, Shinbo H, Ozono S, Kageyama S, Mikami Y, Araki I, Takeda M, Masuyama K, Yamada S: Human muscarinic receptor binding characteristics of antimuscarinic agents to treat overactive bladder. J Urol. 2006 Jan;175(1):365-9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- 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
- Maruyama S, Oki T, Otsuka A, Shinbo H, Ozono S, Kageyama S, Mikami Y, Araki I, Takeda M, Masuyama K, Yamada S: Human muscarinic receptor binding characteristics of antimuscarinic agents to treat overactive bladder. J Urol. 2006 Jan;175(1):365-9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- General Function
- Phosphatidylinositol phospholipase c activity
- Specific Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
- Gene Name
- CHRM5
- Uniprot ID
- P08912
- Uniprot Name
- Muscarinic acetylcholine receptor M5
- Molecular Weight
- 60073.205 Da
References
- Maruyama S, Oki T, Otsuka A, Shinbo H, Ozono S, Kageyama S, Mikami Y, Araki I, Takeda M, Masuyama K, Yamada S: Human muscarinic receptor binding characteristics of antimuscarinic agents to treat overactive bladder. J Urol. 2006 Jan;175(1):365-9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Voltage-gated calcium channel activity
- Specific Function
- Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
- Gene Name
- CACNA1C
- Uniprot ID
- Q13936
- Uniprot Name
- Voltage-dependent L-type calcium channel subunit alpha-1C
- Molecular Weight
- 248974.1 Da
References
- Maruyama S, Oki T, Otsuka A, Shinbo H, Ozono S, Kageyama S, Mikami Y, Araki I, Takeda M, Masuyama K, Yamada S: Human muscarinic receptor binding characteristics of antimuscarinic agents to treat overactive bladder. J Urol. 2006 Jan;175(1):365-9. [Article]
- The muscarinic receptor antagonist propiverine exhibits α1-adrenoceptor antagonism in human prostate and porcine trigonum [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Protein heterodimerization activity
- Specific Function
- This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
- Gene Name
- ADRA1A
- Uniprot ID
- P35348
- Uniprot Name
- Alpha-1A adrenergic receptor
- Molecular Weight
- 51486.005 Da
References
- The muscarinic receptor antagonist propiverine exhibits α1-adrenoceptor antagonism in human prostate and porcine trigonum [Link]
- 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
- Maruyama S, Oki T, Otsuka A, Shinbo H, Ozono S, Kageyama S, Mikami Y, Araki I, Takeda M, Masuyama K, Yamada S: Human muscarinic receptor binding characteristics of antimuscarinic agents to treat overactive bladder. J Urol. 2006 Jan;175(1):365-9. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- 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
- Mictoryl monograph [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Nadp binding
- Specific Function
- This protein is involved in the oxidative metabolism of a variety of xenobiotics such as drugs and pesticides. Form I catalyzes the N-oxygenation of secondary and tertiary amines.
- Gene Name
- FMO1
- Uniprot ID
- Q01740
- Uniprot Name
- Dimethylaniline monooxygenase [N-oxide-forming] 1
- Molecular Weight
- 60310.285 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Trimethylamine monooxygenase activity
- Specific Function
- Involved in the oxidative metabolism of a variety of xenobiotics such as drugs and pesticides. It N-oxygenates primary aliphatic alkylamines as well as secondary and tertiary amines. Plays an impor...
- Gene Name
- FMO3
- Uniprot ID
- P31513
- Uniprot Name
- Dimethylaniline monooxygenase [N-oxide-forming] 3
- Molecular Weight
- 60032.975 Da
Drug created at October 20, 2016 21:48 / Updated at February 20, 2024 23:55