| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 250mg |
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| 500mg | |||
| 1g | |||
| Other Sizes |
| Targets |
The primary target of Isopropamide iodide is the muscarinic acetylcholine receptor, for which it acts as an antagonist. By blocking muscarinic receptors in the gastrointestinal tract, the compound reduces parasympathetic activity, leading to decreased gastrointestinal motility and reduced gastric acid secretion. It may also have effects on other muscarinic receptor subtypes, contributing to its therapeutic effects and side effect profile. The compound is also used in research on diseases affecting cognition, including Alzheimer's disease.
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| ln Vitro |
In vitro, Isopropamide iodide demonstrates anticholinergic activity by blocking muscarinic receptor-mediated signaling. The compound inhibits acetylcholine-induced contractions in isolated smooth muscle preparations. It also inhibits carbachol-stimulated intracellular calcium mobilization in cells expressing muscarinic receptors. These in vitro activities confirm its mechanism of action as a muscarinic receptor antagonist and support its use in gastrointestinal research.
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| ln Vivo |
In vivo, Isopropamide iodide is used clinically for the treatment of peptic ulcer and other gastrointestinal disorders marked by hyperacidity and hypermotility. It reduces gastrointestinal motility and gastric acid secretion by blocking parasympathetic activity. The compound is a long-acting anticholinergic drug with sustained effects. It is also used in research on Alzheimer's disease and other cognitive disorders. Clinical use has established its efficacy and safety profile.
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| Enzyme Assay |
In vitro receptor binding assays for Isopropamide iodide involve radioligand competition binding studies using membranes expressing muscarinic receptors (M1-M5 subtypes). The compound is incubated with the receptor and a labeled muscarinic antagonist (e.g., [3H]-N-methylscopolamine) at concentrations ranging from 0.1 nM-100 μM. Binding affinity (Ki) is determined by competitive displacement curves. Functional assays measure the compound's ability to inhibit acetylcholine-induced signaling, such as calcium mobilization or GTPγS binding. All assays include appropriate controls and reference compounds (e.g., atropine).
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| Cell Assay |
In vitro cell-based assays for Isopropamide iodide are conducted using cells expressing muscarinic receptors (e.g., CHO cells transfected with M1-M5 receptors or neuronal cell lines). Cells are treated with Isopropamide iodide at concentrations ranging from 0.01-100 μM. Receptor activation is assessed by measuring intracellular calcium levels using fluorescent dyes, or by measuring downstream signaling markers. The compound's ability to inhibit agonist-induced responses is evaluated. Cell viability is assessed using standard assays. Experiments include vehicle controls and positive controls (e.g., atropine or scopolamine).
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| Animal Protocol |
In vivo animal studies with Isopropamide iodide are conducted in rodent models of gastrointestinal disorders (e.g., gastric ulcer or intestinal motility models). The compound is administered via oral or intraperitoneal injection at doses ranging from 0.1-10 mg/kg. Gastric acid secretion is measured by gastric acid output. Gastrointestinal motility is assessed by measuring intestinal transit time. Ulcer formation is evaluated by histological analysis. Cognitive studies may be conducted in models of Alzheimer's disease. Each group consists of 6-10 animals with appropriate controls.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Isopropamide iodide include its quaternary ammonium structure, which limits its oral bioavailability and central nervous system penetration. The compound is a long-acting anticholinergic with sustained effects. Following administration, it distributes primarily in the extracellular space and does not readily cross the blood-brain barrier. Elimination occurs primarily through renal excretion of the unchanged drug. The compound's pharmacokinetics are influenced by renal function. Detailed PK parameters are available from clinical studies.
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| Toxicity/Toxicokinetics |
Toxicological data for Isopropamide iodide indicate that it is generally well-tolerated at therapeutic doses. Common adverse effects are related to its anticholinergic activity and include dry mouth, blurred vision, constipation, urinary retention, and tachycardia. The compound is contraindicated in patients with glaucoma, obstructive uropathy, or gastrointestinal obstruction. Overdose may cause severe anticholinergic toxicity. Comprehensive safety data are available from clinical use.
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| References |
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| Additional Infomation |
Isopropamide is a diarylmethane compound. Isopropamide iodide is a long-acting quaternary ammonium anticholinergic drug. It is used to treat peptic ulcers and other gastrointestinal disorders characterized by hyperacidity and hypermotility. See also: Isopropamide iodide (note moved to). Indications: Used to treat a variety of gastrointestinal disorders, including peptic ulcers, gastritis, hyperacidity, functional diarrhea, irritable bowel syndrome or spastic colon, pyloric irritable syndrome, pyloric spasm, acute nonspecific gastroenteritis, biliary motility disorders and chronic gallstones, duodenitis, and gastrointestinal spasms. It can also be used to treat spasms of the genitourinary system. Mechanism of Action: Anticholinergic drugs are a class of drugs that inhibit parasympathetic nerve impulses by selectively blocking the binding of the neurotransmitter acetylcholine to its receptors on nerve cells. Nerve fibers of the parasympathetic nervous system are responsible for the involuntary movement of gastrointestinal smooth muscle. Inhibiting these nerve fibers can reduce stomach acid and gastrointestinal motility, thus aiding in the treatment of gastrointestinal disorders.
Pharmacodynamics Propylamide is a long-acting quaternary ammonium anticholinergic drug. It is used to treat peptic ulcers and other gastrointestinal disorders characterized by excessive stomach acid and hypermotility. Isopropamide iodide is an approved therapeutic agent for the treatment of peptic ulcer and gastrointestinal disorders characterized by hyperacidity and hypermotility. It is a long-acting quaternary ammonium anticholinergic drug and muscarinic receptor antagonist. The compound reduces gastrointestinal motility and gastric acid secretion by blocking parasympathetic activity. It is also used in research on Alzheimer's disease. Available as a generic medication in some regions. |
| Molecular Formula |
C₂₃H₃₃IN₂O
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|---|---|
| Molecular Weight |
480.43
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| Exact Mass |
480.164
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| CAS # |
71-81-8
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| Related CAS # |
7492-32-2;71-81-8 (Iodide);
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| PubChem CID |
3775
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| Appearance |
White to off-white solid powder
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| Density |
1.2711 (estimate)
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| Melting Point |
199℃ (Decomposition)
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| LogP |
1.815
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
26
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| Complexity |
419
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
JTPUMZTWMWIVPA-UHFFFAOYSA-O
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| InChi Code |
InChI=1S/C23H32N2O/c1-18(2)25(5,19(3)4)17-16-23(22(24)26,20-12-8-6-9-13-20)21-14-10-7-11-15-21/h6-15,18-19H,16-17H2,1-5H3,(H-,24,26)/p+1
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| Chemical Name |
(4-amino-4-oxo-3,3-diphenylbutyl)-methyl-di(propan-2-yl)azanium
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| Synonyms |
Isopropamide iodide5579MD 5579-MD
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~520.37 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0815 mL | 10.4073 mL | 20.8147 mL | |
| 5 mM | 0.4163 mL | 2.0815 mL | 4.1629 mL | |
| 10 mM | 0.2081 mL | 1.0407 mL | 2.0815 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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