| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
|
||
| 1g |
|
||
| 2g |
|
||
| 5g |
|
||
| Other Sizes |
| Targets |
Isopropamide targets muscarinic acetylcholine receptors, specifically the M1, M2, and M3 subtypes. As a quaternary ammonium compound, it does not readily cross the blood-brain barrier, so its effects are primarily peripheral. By blocking muscarinic receptors in the gastrointestinal tract, it reduces gastric acid secretion, decreases gastrointestinal motility, and relieves smooth muscle spasms.
|
|---|---|
| ln Vitro |
Isopropamide exhibits anticholinergic activity in vitro. Its activity is characterized by its ability to inhibit muscarinic receptor-mediated responses in isolated tissue preparations, such as the contraction of smooth muscle. The compound's potency as a muscarinic receptor antagonist has been confirmed in various pharmacological assays.
|
| ln Vivo |
Isopropamide is effective in vivo for reducing gastric acid secretion and gastrointestinal motility. It is used clinically for the treatment of peptic ulcer disease and other gastrointestinal disorders. Its effects are mediated by peripheral muscarinic receptor blockade, which reduces parasympathetic stimulation of the gastrointestinal tract.
|
| Enzyme Assay |
The primary in vitro assay for isopropamide is a radioligand binding assay using membrane preparations from cells expressing muscarinic receptors. The compound's ability to displace a labeled muscarinic ligand is measured to determine its binding affinity. Functional assays measure its ability to inhibit muscarinic receptor-mediated responses, such as smooth muscle contraction.
|
| Cell Assay |
In vitro cellular assays for isopropamide involve treating cells expressing muscarinic receptors with the compound and measuring its effect on receptor-mediated signaling. This can include measuring changes in intracellular calcium levels or other downstream signaling events. The compound's ability to inhibit muscarinic receptor activation confirms its antagonist activity.
|
| Animal Protocol |
In vivo animal experiments for isopropamide would involve administering the compound to animal models to assess its effects on gastric acid secretion and gastrointestinal motility. The compound's ability to reduce acid secretion and inhibit motility would be measured. These studies would confirm its efficacy as an anticholinergic agent.
|
| ADME/Pharmacokinetics |
Isopropamide is a quaternary ammonium compound with a molecular weight of approximately 346.3 g/mol. It is poorly absorbed from the gastrointestinal tract due to its quaternary ammonium structure, which limits its systemic bioavailability. Its effects are primarily local in the gastrointestinal tract. The compound is typically administered orally in combination with other drugs.
|
| Toxicity/Toxicokinetics |
The toxicological profile of isopropamide is characteristic of anticholinergic agents. Common adverse effects include dry mouth, blurred vision, constipation, urinary retention, and tachycardia. As a quaternary ammonium compound, it does not readily cross the blood-brain barrier, so central nervous system effects are less common than with tertiary amine anticholinergics.
|
| 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 is a synthetic anticholinergic agent used to reduce gastric acid secretion and gastrointestinal motility. It is a quaternary ammonium compound that acts as a muscarinic receptor antagonist. It is used in combination with other drugs for the treatment of peptic ulcer disease and other gastrointestinal disorders. The compound is not widely used as a single agent and has largely been replaced by newer medications. It is available from various chemical suppliers for research purposes. |
| Molecular Formula |
C23H33N2O+
|
|---|---|
| Molecular Weight |
353.5204
|
| Exact Mass |
353.259
|
| CAS # |
7492-32-2
|
| Related CAS # |
7492-32-2;71-81-8 (Iodide);
|
| PubChem CID |
3775
|
| Appearance |
Typically exists as solid at room temperature
|
| Melting Point |
182-184
|
| LogP |
4.811
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
1
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
26
|
| Complexity |
419
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC([N+](CCC(C1=CC=CC=C1)(C(N)=O)C2=CC=CC=C2)(C(C)C)C)C
|
| InChi Key |
JTPUMZTWMWIVPA-UHFFFAOYSA-O
|
| 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
|
| Chemical Name |
(4-amino-4-oxo-3,3-diphenylbutyl)-methyl-di(propan-2-yl)azanium
|
| Synonyms |
Dipramid, Dipramide Isopropamide, Chloroisopropamide, Piaccamide, Priazimide
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 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 | 2.8287 mL | 14.1435 mL | 28.2869 mL | |
| 5 mM | 0.5657 mL | 2.8287 mL | 5.6574 mL | |
| 10 mM | 0.2829 mL | 1.4143 mL | 2.8287 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
