Identification
- Summary
Trimebutine is a spasmolytic agent used for the symptomatic treatment of irritable bowel syndrome (IBS) and treatment of postoperative paralytic ileus following abdominal surgery.
- Generic Name
- Trimebutine
- DrugBank Accession Number
- DB09089
- Background
Trimebutine is a spasmolytic agent that regulates intestinal and colonic motility and relieves abdominal pain with antimuscarinic and weak mu opioid agonist effects. It is marketed for the treatment of irritable bowel syndrome (IBS) and lower gastrointestinal tract motility disorders, with IBS being one of the most common multifactorial GI disorders 2. It is used to restore normal bowel function and is commonly present in pharmaceutical mixtures as trimebutine maleate salt form. Trimebutine is not a FDA-approved drug, but it is available in Canada and several other international countries.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Trimebutine (DB09089)
- Weight
- Average: 387.476
Monoisotopic: 387.204573038 - Chemical Formula
- C22H29NO5
- Synonyms
- 2-Dimethylamino-2-phenylbutyl 3,4,5-trimethoxybenzoat
- Trimébutine
- Trimebutine
- Trimebutino
Pharmacology
- Indication
Indicated for symptomatic treatment of irritable bowel syndrome (IBS) and treatment of postoperative paralytic ileus following abdominal surgery.
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 Irritable bowel syndrome •••••••••••• Symptomatic treatment of Irritable bowel syndrome •••••••••••• Used in combination to treat Gastrointestinal spasms Combination Product in combination with: Medazepam (DB13437) •••••••••••• ••••••• Management of Postoperative paralytic ileus •••••••••••• - 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
Trimebutine is a spasmolytic agent that acts directly on smooth muscle to modulate gastric motility. It shows a "dual function" that stimulates or inhibits spontaneous contractions depending on the concentration and prior contractile activity in the preparation. Targeting ion conductance that regulates GI motility, trimebutine inhibits the inward calcium currents and calcium-dependent potassium currents in a concentration-dependent manner 2. At lower concentrations (1-10uM), trimebutine depolarizes the resting membrane potential without affecting the amplitude of contractions, which is thought to be mediated by inhibition of outward potassium currents. It is also shown to activate T-type Ca2+ channel and increase gastric emptying, intestinal and colonic contractility 1. At higher concentrations (100-300uM), reduced amplitude of spontaneous contractions and action potentials is thought to be mediated by inhibition of L-type Ca2+ channels and inward calcium current 2. Trimebutine mediates a local anesthetic action by acting as a weak agonist at mu opioid receptors.
- Mechanism of action
At high concentrations, trimebutine is shown to inhibit the extracellular Ca2+ influx in the smooth muscle cells through voltage dependent L-type Ca2+ channels and further Ca2+ release from intracellular Ca2+ stores 2,4. Trimebutine is suggested to bind to the inactivated state of the calcium channel with high affinity. Reduced calcium influx attenuates membrane depolarization and decrease colon peristalsis. It also inhibits outward K+ currents in response to membrane depolarization of the GI smooth muscle cells at resting conditions through inhibition of delayed rectifier K+ channels and Ca2+ dependent K+ channels, which results in induced muscle contractions 2,6. Trimebutine binds to mu opioid receptors with more selectivity compared to delta or kappa opioid receptors but with lower affinity than their natural ligands. Its metabolites (N-monodesmethyl-trimebutine or nor-trimebutine), are also shown to bind to opoid receptors on brain membranes and myenteric synaptosomes 3.
Target Actions Organism AMu-type opioid receptor agonistHumans AVoltage-dependent L-type calcium channel inhibitorHumans ACalcium-activated potassium channel inhibitorHumans AMuscarinic acetylcholine receptor M1 antagonistHumans AMuscarinic acetylcholine receptor M2 antagonistHumans AMuscarinic acetylcholine receptor M3 antagonistHumans AMuscarinic acetylcholine receptor M4 antagonistHumans UVoltage-dependent T-type calcium channel activatorHumans - Absorption
The free base form or salt form of trimebutine are rapidly absorbed after oral administration, with the peak plasma concentration reached after 1 hour of ingestion 3. The time to reach peak plasma concentration following a single oral dose of 200mg trimebutine is 0.80 hours 8.
- Volume of distribution
Trimebutine is most likely to be accumulated in the stomach and the intestinal walls in highest concentrations. The fetal transfer is reported to be low 3.
- Protein binding
Protein binding is minimal with 5% in vivo and in vitro to serum albumin 8.
- Metabolism
Trimebutine undergoes extensive hepatic first-pass metabolism. Nortrimebutine, or N-monodesmethyltrimebutine, is the main metabolite that retains pharmacological activity on the colon. This metabolite can undergo second N-demethylation to form N-didesmethyltrimebutine. Other main urinary metabolites (2-amino, 2-methylamino or 2-dimethylamino-2-phenylbutan-1-ol) can be formed via hydrolysis of the ester bond of desmethylated metabolites or initial hydrolysis of the ester bond of trimebutine followed by sequential N-demethylation 5. Trimebutine is also prone to sulphate and/or glucuronic acid conjugation 8.
Hover over products below to view reaction partners
- Route of elimination
Renal elimination is predominant while excretion into feces is also observed (5-12%). About 94% of an oral dose of trimebutine is eliminated by the kidneys in the form of various metabolites 3 and less than 2.4% of total ingested drug is recovered as unchanged parent drug in the urine 8.
- Half-life
The elimination half life is approximately 1 hour following a single oral dose of 2mg/kg 3, and 2.77 hours following a single oral dose 200 mg 8.
- Clearance
Not Available
- 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
Common gastrointestinal adverse effects include dry mouth, foul taste, diarrhea, dyspepsia, epigastric pain, nausea and constipation. Some CNS effects include drowsiness, fatigue, dizziness, hot/cold sensations and headaches. In case of overdosage, gastric lavage is recommended. Oral LD50 in mouse and rats is >5000 mg/kg and 2500 mg/kg in rabbits, respectively. Trimebutine is not reported to display teratogenic, mutagenic or carcinogenic potential 8.
- 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 Trimebutine which could result in a higher serum level. Abametapir The serum concentration of Trimebutine can be increased when it is combined with Abametapir. Acarbose The risk or severity of hypoglycemia can be increased when Trimebutine is combined with Acarbose. Acebutolol Acebutolol may increase the arrhythmogenic activities of Trimebutine. Aceclofenac The risk or severity of hyperkalemia can be increased when Aceclofenac is combined with Trimebutine. - Food Interactions
- Take before a meal.
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 Trimebutine maleate 2A051GM4YM 34140-59-5 FSRLGULMGJGKGI-BTJKTKAUSA-N - International/Other Brands
- Altrip (Spedrog-Caillon, Argentina) / Anytin (Ahngook, South Korea) / Biorgan (Ivax, Argentina) / Bumetin (Galeno) / Butikinon (Towa Yakuhin) / Cerekinon (Mitsubishi Tanabe Pharma) / Cineprac (Liferpal, Mexico) / Colixane (Sanitas, Argentina) / Colonix (Grupo Farma, Ecuador) / Colperin (Gedeon Richter, Romania) / Coltrim (Novamed, Colombia) / Colypan (Grupo Farma) / Crobutin (Daewoo, South Korea) / Debretin (Polpharma, Poland) / Debricalm (Pfizer) / Debricol (Galpharma, Tunisia) / Debridat (Pfizer) / Digerent (Polifarma, Italy) / Diway (Poly Pharm, China) / Dolpic Forte (Laboratorios Pasteur, Chile) / Esun (Productos Farmaceuticos Medipharm, Chile) / Eumotil (Baliarda, Argentina) / Eumotrix (Lafrancol, Colombia) / Eutransil (Baliarda, Ecuador) / Fenatrop (Gador, Argentina) / Garapepsin (Farmellas Enterprises, Greece) / Gaspat (Indunidas, Ecuador) / Gast Reg (Amoun, Egypt) / Gismotal (Biofarma, Turkey) / Ircolon (Polfarmex, Poland) / Libertrim (Carnot Laboratorios, Mexico) / Mebucolon (Kyowa Yakuhin, Japan) / Mebutit (Sawai Seiyaku, Japan) / Miopropan (Bernabo, Argentina) / Neotina (Rossmore Pharma, Argentina) / Nepten (Nagase Medicals, Japan) / Newbutin SR (Korea United Pharm, Vietnam) / Ni Wei Fu (Anglikang Pharmaceutical, China) / Normopax (Eczane, Argentina) / Plidex (Roemmers, Argentina) / Polibutin (Desma, Spain) / Polybutine (Samil, South Korea) / Procinet NF (Eurofarma, Argentina) / Puridat Fort (Bilim, Turkey) / Rui Jian (Ante Bio-Pharmaceutical, China) / Sakion (Harasawa Seiyaku, Japan) / Shuang Di (Sanyu Pharmaceutical, China) / Spabutine (Hanmi, South Korea) / Supeslone (Koa Isei, Japan) / Tarabutine (Kukje, South Korea) / Tefmetin (Kobayashi Kako, Japan) / Tempolib (Medix, Mexico) / Tidomel (Laboratorios Euromed Chile, Chile) / Timotor (Square, Bangladesh) / Transacalm (Pharma Développement, France) / Trebutel (Laboratorios Andromaco, Chile) / Tribudat (Santa-Farma, Turkey; Sigma, Egypt) / Tributin (Incobra, Colombia) / Tributina (Lafedar, Argentina) / Tribux (Biofarm) / Trim (Laboratorio Saval, Chile) / Trimebutina (Anglopharma) / Trimedat (Life Pharma, Lebanon) / Trimedine (Opalia, Tunisia) / Trimotil (Incepta, Bangladesh) / Trimspa (Macleods, India) / VeM (Kyorin Rimedio, Japan) / Yuan Sheng Li Wei (Kaikai Yuansheng Medicine, China)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Modulon Tablet 200 mg Oral Aptalis Pharma Canada Ulc 1991-12-31 2019-01-28 Canada 
Modulon Inj 50mg/5ml Liquid 10 mg / 1 mL Intramuscular; Intravenous Axcan Pharma 1983-12-31 2000-01-07 Canada Modulon Tab 100mg Tablet 100 mg Oral Axcan Pharma 1983-12-31 2002-08-19 Canada Trimebutine Tablet 200 mg Oral Aa Pharma Inc 2002-10-21 Not applicable Canada Trimebutine Tablet 100 mg Oral Aa Pharma Inc 2002-10-21 Not applicable Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Mint-trimebutine Tablet 200 mg Oral Mint Pharmaceuticals Inc Not applicable Not applicable Canada Mint-trimebutine Tablet 100 mg Oral Mint Pharmaceuticals Inc Not applicable Not applicable Canada - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image ALTEGAM® TABLETAS RECUBIERTAS Trimebutine maleate (200 mg) + Simethicone (120 mg) Tablet, coated Oral CLARIPACK S.A. 2018-05-16 Not applicable Colombia 
COLTRIM PLUS Trimebutine maleate (200 mg) + Simethicone (120 mg) Tablet, coated Oral C.I. FARMACAPSULAS S.A.S. - PLANTA NO. 2 2015-08-05 Not applicable Colombia EUMOTRIX® PLUS Trimebutine (200 mg) + Simethicone (230.77 mg) Tablet, chewable Oral LABORATORIO FRANCO COLOMBIANO - LAFRANCOL S.A.S. 2009-06-17 Not applicable Colombia LIBERTRIM SII COMPRIMIDOS Trimebutine maleate (200 mg) + Simethicone (75 mg) Tablet, coated Oral AULEN PHARMA S.A. 2009-12-10 2020-07-01 Colombia MUVETT S Trimebutine maleate (200 mg) + Simethicone (120 mg) Tablet, coated Oral PROCAPS S.A. 2006-11-10 2020-09-04 Colombia
Categories
- ATC Codes
- A03AA05 — Trimebutine
- Drug Categories
- Acids, Carbocyclic
- Agents causing hyperkalemia
- Agents producing tachycardia
- Alimentary Tract and Metabolism
- Antiarrhythmic agents
- Anticholinergic Agents
- Antimuscarinics Antispasmodics
- Autonomic Agents
- Benzene Derivatives
- Benzoates
- Bradycardia-Causing Agents
- Calcium Channel Blockers
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Substrates
- Drugs for Functional Gastrointestinal Disorders
- Drugs that are Mainly Renally Excreted
- Gastrointestinal Agents
- Hydroxy Acids
- Hydroxybenzoate Ethers
- Hydroxybenzoates
- Muscarinic Antagonists
- Parasympatholytics
- Peripheral Nervous System Agents
- Phenols
- Phenyl Ethers
- Potential QTc-Prolonging Agents
- Prokinetic Agents
- QTc Prolonging Agents
- Synthetic Anticholinergics, Esters With Tertiary Amino Group
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as gallic acid and derivatives. These are compounds containing a 3,4,5-trihydroxybenzoic acid moiety.
- Kingdom
- Organic compounds
- Super Class
- Benzenoids
- Class
- Benzene and substituted derivatives
- Sub Class
- Benzoic acids and derivatives
- Direct Parent
- Gallic acid and derivatives
- Alternative Parents
- M-methoxybenzoic acids and derivatives / P-methoxybenzoic acids and derivatives / Benzoic acid esters / Phenylpropanes / Methoxybenzenes / Benzoyl derivatives / Anisoles / Phenoxy compounds / Alkyl aryl ethers / Aralkylamines show 7 more
- Substituents
- Alkyl aryl ether / Amine / Amino acid or derivatives / Anisole / Aralkylamine / Aromatic homomonocyclic compound / Benzoate ester / Benzoyl / Carboxylic acid derivative / Carboxylic acid ester show 18 more
- Molecular Framework
- Aromatic homomonocyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- QZ1OJ92E5R
- CAS number
- 39133-31-8
- InChI Key
- LORDFXWUHHSAQU-UHFFFAOYSA-N
- InChI
- InChI=1S/C22H29NO5/c1-7-22(23(2)3,17-11-9-8-10-12-17)15-28-21(24)16-13-18(25-4)20(27-6)19(14-16)26-5/h8-14H,7,15H2,1-6H3
- IUPAC Name
- 2-(dimethylamino)-2-phenylbutyl 3,4,5-trimethoxybenzoate
- SMILES
- CCC(COC(=O)C1=CC(OC)=C(OC)C(OC)=C1)(N(C)C)C1=CC=CC=C1
References
- General References
- Radulovic M, Anand P, Korsten MA, Gong B: Targeting Ion Channels: An Important Therapeutic Implication in Gastrointestinal Dysmotility in Patients With Spinal Cord Injury. J Neurogastroenterol Motil. 2015 Oct 1;21(4):494-502. doi: 10.5056/jnm15061. [Article]
- Lee HT, Kim BJ: Trimebutine as a modulator of gastrointestinal motility. Arch Pharm Res. 2011 Jun;34(6):861-4. doi: 10.1007/s12272-011-0600-7. [Article]
- Delvaux M, Wingate D: Trimebutine: mechanism of action, effects on gastrointestinal function and clinical results. J Int Med Res. 1997 Sep-Oct;25(5):225-46. [Article]
- Nagasaki M, Komori S, Ohashi H: Effect of trimebutine on voltage-activated calcium current in rabbit ileal smooth muscle cells. Br J Pharmacol. 1993 Sep;110(1):399-403. [Article]
- Miura Y, Chishima S, Takeyama S: Studies of metabolic pathways of trimebutine by simultaneous administration of trimebutine and its deuterium-labeled metabolite. Drug Metab Dispos. 1989 Jul-Aug;17(4):455-62. [Article]
- Tan W, Zhang H, Luo HS, Xia H: Effects of trimebutine maleate on colonic motility through Ca(2)+-activated K+ channels and L-type Ca(2)+ channels. Arch Pharm Res. 2011 Jun;34(6):979-85. doi: 10.1007/s12272-011-0615-0. Epub 2011 Jul 2. [Article]
- Nagasaki M, Komori S, Tamaki H, Ohashi H: Effect of trimebutine on K+ current in rabbit ileal smooth muscle cells. Eur J Pharmacol. 1993 Apr 28;235(2-3):197-203. [Article]
- AA Pharma Inc.: TRIMEBUTINE product monograph [Link]
- External Links
- PubChem Compound
- 5573
- PubChem Substance
- 310265016
- ChemSpider
- 5372
- BindingDB
- 83417
- 10819
- ChEBI
- 94458
- ChEMBL
- CHEMBL190044
- Wikipedia
- Trimebutine
- MSDS
- Download (33.4 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 Helicobacter Pylori Infection 1 4 Completed Treatment Irritable Bowel Syndrome (IBS) 1 4 Withdrawn Treatment Refractory Reflux Esophagitis 1 3 Unknown Status Prevention Nausea / Vomiting 1 2 Completed Prevention Cancer / Colonic Diseases / Pain 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet Oral 200.0 mg Tablet, extended release Oral 300 mg Tablet, film coated Oral 100 mg Tablet Oral 100.00 mg Tablet Oral 200.000 mg Solution Intramuscular; Intravenous 50 mg Capsule Granule, for suspension Oral 72 MG/15ML Injection, solution Intravenous Suppository Tablet Oral Suspension Oral 250 ml Suspension Oral 0.787 g/100g Solution Intramuscular 50 mg Tablet Oral 100 mg Capsule Oral Tablet, film coated Oral 300 mg Tablet Oral 300 mg Tablet, chewable Oral Tablet, coated Oral 200 mg Tablet Oral 300.000 mg Suspension Oral Tablet Oral Powder, for suspension Oral Powder, for suspension Oral 1.334 g Granule Liquid Intramuscular; Intravenous 10 mg / 1 mL Capsule, coated Oral 200 mg Powder, for suspension Oral 300 mg Solution Intramuscular; Intravenous 5000000 mg Tablet, coated Oral Powder, for suspension Oral 1.333 g Cream Rectal Suppository Rectal Suppository Rectal 10 mg Granule, for suspension Oral 24 mg/5ml Tablet Oral 200 mg Tablet Oral 300.00 mg Granule, for suspension Oral 4.8 mg/ml Tablet, film coated Oral 200 mg Tablet, coated Oral 300 mg Granule, for suspension Oral Tablet Oral 20000000 mg Suspension Oral 1.33 g Tablet, coated Oral 20000000 mg Tablet, extended release Oral 30000000 mg - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 78-82 Product monograph water solubility Insoluble Product monograph - Predicted Properties
Property Value Source Water Solubility 0.019 mg/mL ALOGPS logP 3.94 ALOGPS logP 4.11 Chemaxon logS -4.3 ALOGPS pKa (Strongest Basic) 8.48 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 57.23 Å2 Chemaxon Rotatable Bond Count 10 Chemaxon Refractivity 108.94 m3·mol-1 Chemaxon Polarizability 42.43 Å3 Chemaxon Number of Rings 2 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 206.2003 predictedDeepCCS 1.0 (2019) [M+H]+ 208.78345 predictedDeepCCS 1.0 (2019) [M+Na]+ 216.61562 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Voltage-gated calcium channel activity
- Specific Function
- Receptor for endogenous opioids such as beta-endorphin and endomorphin. Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone...
- Gene Name
- OPRM1
- Uniprot ID
- P35372
- Uniprot Name
- Mu-type opioid receptor
- Molecular Weight
- 44778.855 Da
References
- Kaneto H, Takahashi M, Watanabe J: The opioid receptor selectivity for trimebutine in isolated tissues experiments and receptor binding studies. J Pharmacobiodyn. 1990 Jul;13(7):448-53. [Article]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- 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...
Components:
References
- Nagasaki M, Komori S, Ohashi H: Effect of trimebutine on voltage-activated calcium current in rabbit ileal smooth muscle cells. Br J Pharmacol. 1993 Sep;110(1):399-403. [Article]
- Radulovic M, Anand P, Korsten MA, Gong B: Targeting Ion Channels: An Important Therapeutic Implication in Gastrointestinal Dysmotility in Patients With Spinal Cord Injury. J Neurogastroenterol Motil. 2015 Oct 1;21(4):494-502. doi: 10.5056/jnm15061. [Article]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Voltage-gated potassium channel activity
- Specific Function
- Potassium channel activated by both membrane depolarization or increase in cytosolic Ca(2+) that mediates export of K(+). It is also activated by the concentration of cytosolic Mg(2+). Its activati...
Components:
References
- Radulovic M, Anand P, Korsten MA, Gong B: Targeting Ion Channels: An Important Therapeutic Implication in Gastrointestinal Dysmotility in Patients With Spinal Cord Injury. J Neurogastroenterol Motil. 2015 Oct 1;21(4):494-502. doi: 10.5056/jnm15061. [Article]
- Lee HT, Kim BJ: Trimebutine as a modulator of gastrointestinal motility. Arch Pharm Res. 2011 Jun;34(6):861-4. doi: 10.1007/s12272-011-0600-7. [Article]
- 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
- Eglen RM, Watson N: Selective muscarinic receptor agonists and antagonists. Pharmacol Toxicol. 1996 Feb;78(2):59-68. [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
- Eglen RM, Watson N: Selective muscarinic receptor agonists and antagonists. Pharmacol Toxicol. 1996 Feb;78(2):59-68. [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
- Eglen RM, Watson N: Selective muscarinic receptor agonists and antagonists. Pharmacol Toxicol. 1996 Feb;78(2):59-68. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- 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
- Eglen RM, Watson N: Selective muscarinic receptor agonists and antagonists. Pharmacol Toxicol. 1996 Feb;78(2):59-68. [Article]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Activator
- General Function
- Scaffold protein binding
- 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...
Components:
References
- Radulovic M, Anand P, Korsten MA, Gong B: Targeting Ion Channels: An Important Therapeutic Implication in Gastrointestinal Dysmotility in Patients With Spinal Cord Injury. J Neurogastroenterol Motil. 2015 Oct 1;21(4):494-502. doi: 10.5056/jnm15061. [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
- Uesawa Y, Takeuchi T, Mohri K: Integrated analysis on the physicochemical properties of dihydropyridine calcium channel blockers in grapefruit juice interactions. Curr Pharm Biotechnol. 2012 Jul;13(9):1705-17. [Article]
Drug created at September 15, 2015 21:18 / Updated at February 20, 2024 23:54