| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg | |||
| Other Sizes |
| Targets |
Muscarinic acetylcholine receptors (mAChRs). Propantheline bromide acts as a non-selective antagonist at these receptors.
|
|---|---|
| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as quantitative tracers while the drugs were being developed. Because deuteration may have an effect on a drug's pharmacokinetics and metabolic properties, it is a cause for concern [1].
Propantheline bromide, the non-deuterated form, is an antimuscarinic agent that inhibits involuntary muscle contractions by blocking muscarinic acetylcholine receptors. The deuterated form, Propantheline-d3 bromide, is expected to exhibit similar pharmacological properties due to the minimal isotopic effect of deuterium substitution. |
| ln Vivo |
In vivo, propantheline bromide is used for the treatment of hyperhidrosis, gastrointestinal and bladder spasms, and enuresis. It inhibits involuntary muscle contractions by blocking muscarinic receptors in smooth muscle. The deuterated form is used as an analytical standard rather than for therapeutic purposes.
|
| Enzyme Assay |
In vitro receptor binding assays are performed to determine the affinity of propantheline for muscarinic receptors. Radioligand binding studies using membrane preparations from cells or tissues expressing the receptors are conducted. The compound's ability to displace a specific radiolabeled ligand from the receptors is measured to calculate its binding affinity.
|
| Cell Assay |
In vitro cell-based assays are conducted using cells expressing muscarinic receptors. The cells are treated with propantheline, and the inhibition of agonist-induced intracellular signaling is measured to quantify the antagonistic activity.
|
| Animal Protocol |
In vivo studies are conducted in animal models to evaluate the pharmacological effects of propantheline. The compound is administered via various routes, and its effects on gastrointestinal motility, bladder function, and sweating are assessed.
|
| ADME/Pharmacokinetics |
Propantheline bromide is a quaternary ammonium compound with limited oral bioavailability due to its charged nature. It is primarily excreted unchanged in the urine. The deuterated form, Propantheline-d3 bromide, is used as an internal standard in pharmacokinetic studies to quantify propantheline levels in biological samples using mass spectrometry.
|
| Toxicity/Toxicokinetics |
Propantheline bromide is generally well-tolerated, but common side effects include dry mouth, blurred vision, constipation, and urinary retention, which are typical of antimuscarinic agents. At higher doses, it may cause more pronounced anticholinergic effects.
|
| References | |
| Additional Infomation |
Propantheline-d3 bromide is the deuterium-labeled form of propantheline bromide, an antimuscarinic agent used for the treatment of hyperhidrosis, gastrointestinal and bladder spasms, and enuresis. The deuterated form is used as an internal standard in analytical methods for the quantification of propantheline in biological samples. It is not intended for human therapeutic use and is strictly for research purposes.
|
| Molecular Formula |
C23H30BRNO3
|
|---|---|
| Molecular Weight |
448.393206119537
|
| Exact Mass |
450.159
|
| CAS # |
64717-35-7
|
| Related CAS # |
Propantheline bromide;50-34-0
|
| PubChem CID |
12491590
|
| Appearance |
Off-white to light yellow solid powder
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
28
|
| Complexity |
474
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C(C1C2=CC=CC=C2OC2C=CC=CC1=2)(=O)OCC[N+](C([H])([H])[H])(C(C)C)C(C)C.[Br-]
|
| InChi Key |
XLBIBBZXLMYSFF-OWKBQAHQSA-M
|
| InChi Code |
InChI=1S/C23H30NO3.BrH/c1-16(2)24(5,17(3)4)14-15-26-23(25)22-18-10-6-8-12-20(18)27-21-13-9-7-11-19(21)22;/h6-13,16-17,22H,14-15H2,1-5H3;1H/q+1;/p-1/i5D3;
|
| Chemical Name |
di(propan-2-yl)-(trideuteriomethyl)-[2-(9H-xanthene-9-carbonyloxy)ethyl]azanium;bromide
|
| 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 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)
|
| 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 | 2.2302 mL | 11.1510 mL | 22.3020 mL | |
| 5 mM | 0.4460 mL | 2.2302 mL | 4.4604 mL | |
| 10 mM | 0.2230 mL | 1.1151 mL | 2.2302 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
