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

3D

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MOLSDF3D-SDFPDBSMILESInChI

Similar Structures

Structure for Propiverine (DB12278)

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Weight

Average: 367.4813
Monoisotopic: 367.214743799

Chemical Formula

C₂₃H₂₉NO₃

Synonyms

• Propiverina
• Propiverine

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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.

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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		••••••••••••

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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	antagonist	Humans
AMuscarinic acetylcholine receptor M2	antagonist	Humans
AMuscarinic acetylcholine receptor M3	antagonist	Humans
AMuscarinic acetylcholine receptor M5	Not Available	Humans
AVoltage-dependent L-type calcium channel subunit alpha-1C	antagonist	Humans
AAlpha-1A adrenergic receptor	antagonist	Humans
UMuscarinic acetylcholine receptor M4	antagonist	Humans

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

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Interactions

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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.

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drug	Interaction
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Abacavir	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.

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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
Mictoryl	Capsule, extended release	30 mg	Oral	Duchesnay Inc.	2017-05-08	Not applicable
Mictoryl Pediatric	Tablet	5 mg	Oral	Duchesnay Inc.	2017-04-13	Not applicable

Categories

ATC Codes

G04BD06 — Propiverine

• G04BD — Drugs for urinary frequency and incontinence
• G04B — UROLOGICALS
• G04 — UROLOGICALS
• G — GENITO URINARY SYSTEM AND SEX HORMONES

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 / Hydrocarbon derivatives / Carbonyl compounds

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Substituents

Amine / Amino acid or derivatives / Aromatic heteromonocyclic compound / Azacycle / Benzylether / Carbonyl group / Carboxylic acid derivative / Carboxylic acid ester / Dialkyl ether / Diphenylmethane / Ether / Hydrocarbon derivative / Monocarboxylic acid or derivatives / Organic nitrogen compound / Organic oxide / Organic oxygen compound / Organoheterocyclic compound / Organonitrogen compound / Organooxygen compound / Organopnictogen compound / Piperidine / Tertiary aliphatic amine / Tertiary amine

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

1. 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]
2. 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]
3. Chess-Williams R: Muscarinic receptors of the urinary bladder: detrusor, urothelial and prejunctional. Auton Autacoid Pharmacol. 2002 Jun;22(3):133-45. [Article]
4. 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]
5. 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]
6. Mictoryl monograph [Link]
7. CDR CLINICAL REVIEW REPORT FOR MICTORYL [Link]
8. The Efficacy and Safety of Propiverine Hydrochloride in Patients with Overactive Bladder Symptoms Who Poorly Responded to Previous Anticholinergic Agents [Link]
9. Propiverine hydrochloride [Link]
10. Propiverine Hydrochloride PubChem [Link]
11. Public assessment report [Link]
12. Pharmacokinetic Studies on Propiverine Hydrochloride [Link]
13. Mictonorm [Link]
14. The muscarinic receptor antagonist propiverine exhibits α1-adrenoceptor antagonism in human prostate and porcine trigonum [Link]
15. Mayo Clinic, Overactive Bladder [Link]
16. Maximizing the Treatment of Overactive Bladder in the Elderly [Link]
17. Muscarinic receptor antagonists for overactive bladder [Link]
18. Propiverine overview [Link]
19. 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

RxNav

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	predicted	DarkChem Lite v0.1.0
[M-H]-	193.0164	predicted	DeepCCS 1.0 (2019)
[M+H]+	206.4250489	predicted	DarkChem Lite v0.1.0
[M+H]+	195.74474	predicted	DeepCCS 1.0 (2019)
[M+Na]+	206.1563489	predicted	DarkChem Lite v0.1.0
[M+Na]+	204.26714	predicted	DeepCCS 1.0 (2019)

Targets

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insights and accelerate drug research.

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Details1. Muscarinic acetylcholine receptor M1

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

1. Maruyama S, Oki T, Otsuka A, Shinbo H, Ozono S, Kageyama S, Mikami Y, Araki I, Takeda M, Masuyama K, Yamada S: Human muscarinic receptor binding characteristics of antimuscarinic agents to treat overactive bladder. J Urol. 2006 Jan;175(1):365-9. [Article]

Details2. Muscarinic acetylcholine receptor M2

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

1. Maruyama S, Oki T, Otsuka A, Shinbo H, Ozono S, Kageyama S, Mikami Y, Araki I, Takeda M, Masuyama K, Yamada S: Human muscarinic receptor binding characteristics of antimuscarinic agents to treat overactive bladder. J Urol. 2006 Jan;175(1):365-9. [Article]

Details3. Muscarinic acetylcholine receptor M3

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

1. Maruyama S, Oki T, Otsuka A, Shinbo H, Ozono S, Kageyama S, Mikami Y, Araki I, Takeda M, Masuyama K, Yamada S: Human muscarinic receptor binding characteristics of antimuscarinic agents to treat overactive bladder. J Urol. 2006 Jan;175(1):365-9. [Article]

Details4. Muscarinic acetylcholine receptor M5

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

1. Maruyama S, Oki T, Otsuka A, Shinbo H, Ozono S, Kageyama S, Mikami Y, Araki I, Takeda M, Masuyama K, Yamada S: Human muscarinic receptor binding characteristics of antimuscarinic agents to treat overactive bladder. J Urol. 2006 Jan;175(1):365-9. [Article]

Details5. Voltage-dependent L-type calcium channel subunit alpha-1C

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

1. Maruyama S, Oki T, Otsuka A, Shinbo H, Ozono S, Kageyama S, Mikami Y, Araki I, Takeda M, Masuyama K, Yamada S: Human muscarinic receptor binding characteristics of antimuscarinic agents to treat overactive bladder. J Urol. 2006 Jan;175(1):365-9. [Article]
2. The muscarinic receptor antagonist propiverine exhibits α1-adrenoceptor antagonism in human prostate and porcine trigonum [Link]

Details6. Alpha-1A adrenergic receptor

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

1. The muscarinic receptor antagonist propiverine exhibits α1-adrenoceptor antagonism in human prostate and porcine trigonum [Link]

Details7. Muscarinic acetylcholine receptor M4

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

1. Maruyama S, Oki T, Otsuka A, Shinbo H, Ozono S, Kageyama S, Mikami Y, Araki I, Takeda M, Masuyama K, Yamada S: Human muscarinic receptor binding characteristics of antimuscarinic agents to treat overactive bladder. J Urol. 2006 Jan;175(1):365-9. [Article]

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Drug created at October 20, 2016 21:48 / Updated at February 20, 2024 23:55