| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
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| Other Sizes |
| Targets |
Propantheline Bromide targets muscarinic acetylcholine receptors (mAChRs), functioning as a competitive antagonist. It inhibits the action of acetylcholine at post-ganglionic synapses, interfering with the cholinergic signaling pathway. An aspartic acid residue present in the N-terminal portion of the third trans-membrane helix of the muscarinic receptor is believed to form an ionic bond with the quaternary nitrogen of the antagonist. Antagonism leads to a reduction of exocrine gland secretions, relaxation of bronchial muscle, and reduced tone and motility of intestinal smooth muscle.
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| ln Vitro |
The reactivity of bladder smooth muscle to cervical choline is lowered by brachpropantheline (10 μM–1 mM) [1].
In vitro, Propantheline bromide (10 μM-1 mM) decreases urinary bladder smooth muscle reactivity to acetylcholine. It competitively antagonizes acetylcholine activity at muscarinic receptors on smooth muscle and exocrine gland cells. The compound's ability to inhibit cholinergic signaling has been characterized in various smooth muscle preparations. Its effects on reducing smooth muscle tone and secretions are well documented in experimental models. |
| ln Vivo |
In patients with restrictive intestinal dysfunction, propantheline bromide (powder formulation, 10-300 mg/kg) lowers the incidence of diarrhea and the count of matrix particles [3].
In vivo, Propantheline bromide is an orally active mAChR antagonist. It reduces exocrine gland secretions, relaxes bronchial muscle, and reduces the tone and motility of intestinal smooth muscle. It is used in research related to smooth muscle dysfunction, excessive sweating, cramps or spasms of the stomach, intestines or bladder, and involuntary urination. It also has anti-inflammatory properties and has been used for the treatment of bowel disease, especially in elderly patients. |
| Enzyme Assay |
The activity of Propantheline bromide can be assessed using radioligand binding assays with membranes prepared from tissues expressing muscarinic receptors. The membrane preparations are incubated with a radiolabeled muscarinic antagonist (e.g., [³H]N-methylscopolamine) and varying concentrations of unlabeled Propantheline bromide. Non-specific binding is determined in the presence of an excess of a competing ligand. The IC₅₀ or Ki values for Propantheline bromide displacement are calculated from competition binding curves.
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| Cell Assay |
To evaluate the cellular effects of Propantheline bromide, cells expressing muscarinic receptors (e.g., smooth muscle cells or exocrine gland cells) are treated with the compound. The inhibition of acetylcholine-induced calcium mobilization, contraction, or secretion is measured. The IC₅₀ for these functional responses is determined from dose-response curves. Standard cell viability assays can also be used to assess any cytotoxic effects.
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| Animal Protocol |
Animal/Disease Models: Rat restraint stress intestinal dysfunction model [3]
Doses: 10-300 mg/kg Route of Administration: Oral Experimental Results:diminished fecal particle count, ED50 value is 41 mg/kg. The incidence of diarrhea was dose-dependently diminished, with an ED50 value of 64 mg/kg. In vivo studies with Propantheline bromide typically involve administration to animal models via oral or parenteral routes. The compound's effects on smooth muscle contraction, glandular secretion, and gastrointestinal motility are assessed. In models of bladder dysfunction or gastrointestinal spasms, the efficacy of Propantheline bromide in reducing symptoms is evaluated. Pharmacokinetic parameters, such as oral bioavailability and half-life, are also characterized. |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Approximately 70% of the dose is excreted in the urine, primarily as metabolites. 95 hours after oral administration of propylthiocyanate bromide, 5% (0.03 g) is excreted in the urine. /propylthiocyanate bromide, from table/ Quaternary ammonium derivatives of belladonna alkaloids are poorly absorbed orally; however, when applied topically to the eyes, some compounds can cause mydriasis and ciliary muscle paralysis. /Quaternary ammonium derivatives of belladonna alkaloids/ Propantheline Bromide has a molecular formula of C₂₃H₃₀BrNO₃ and a molecular weight of 448.39 g/mol. It appears as white crystals or a white powder with a melting point of 159-161 °C. It is soluble in water (50 mg/mL). The CAS number is 50-34-0. The compound should be stored at room temperature and protected from light. |
| Toxicity/Toxicokinetics |
Hepatotoxicity
As with other anticholinergic drugs, propylthioline has not been found to be associated with elevated liver enzymes or clinically significant liver injury. It is at least partially metabolized in the liver. Its safety may be related to its low daily dose. References on the safety and potential hepatotoxicity of anticholinergic drugs are listed after the "Overview of Anticholinergic Drugs" section. Drug Category: Anticholinergic Drugs Effects During Pregnancy and Lactation ◉ Overview of Use During Lactation There is currently no information regarding the use of propylthioline during lactation. Because propylthioline is a quaternary ammonium compound, it is unlikely to be absorbed by the infant and enter the bloodstream. Long-term use of propylthioline may reduce milk production or inhibit the milk ejection reflex. With long-term use, signs of reduced milk production (e.g., infant dissatisfaction, poor weight gain) should be observed. ◉ Effects on Breastfed Infants As of the revision date, no relevant published information was found. ◉ Effects on Lactation and Breast Milk Anticholinergic drugs can inhibit lactation in animals, possibly by suppressing the secretion of growth hormone and oxytocin. Anticholinergic drugs can also lower serum prolactin levels in non-lactating women. Prolactin levels in established lactating mothers may not affect their ability to breastfeed. Specific toxicology data for Propantheline bromide are not extensively detailed in the available literature. As an anticholinergic agent, it can cause typical side effects associated with muscarinic receptor antagonism, such as dry mouth, blurred vision, constipation, and urinary retention. Overdose may lead to severe anticholinergic effects. It should be used with caution in patients with glaucoma, prostatic hypertrophy, or gastrointestinal obstruction. |
| References | |
| Additional Infomation |
Propantheline belongs to the xaxidine class of drugs. It is a muscarinic receptor antagonist used as an antispasmodic to treat rhinitis, urinary incontinence, and ulcers. At high doses, it has nicotine-like effects, leading to neuromuscular blockade. Propantheline is an anticholinergic drug. Its mechanism of action is as a cholinergic antagonist. Propantheline is an anticholinergic drug used to treat gastrointestinal disorders associated with intestinal spasms and to reduce secretions during anesthesia. Propantheline has not been shown to cause elevated liver enzymes or clinically significant acute liver injury. It is a muscarinic receptor antagonist used as an antispasmodic to treat rhinitis, urinary incontinence, and ulcers. At high doses, it has nicotine-like effects, leading to neuromuscular blockade. See also: Propantheline bromide (salt form).
Drug Indications For the treatment of enuresis. It has also been used to treat hyperhidrosis and spasms of the stomach, intestines, or bladder. Mechanism of Action Its mechanism of action is dual: (1) it exerts a specific anticholinergic effect at acetylcholine receptor sites (antimuscarinic effect); (2) it has a direct effect on smooth muscle (muscle affinity). Anticholinergic drugs block the action of acetylcholine at postganglionic cholinergic sites, thereby reducing the number of motor impulses reaching the detrusor muscle and increasing bladder capacity. /Anticholinergic Drugs/ Propantheline Bromide (Pro-Banthine) is a muscarinic acetylcholine receptor antagonist used clinically and in research. It is a quaternary ammonium compound that does not readily cross the blood-brain barrier, limiting central nervous system effects. It has been used therapeutically as an antispasmodic and to reduce gastric acid secretion. Propantheline bromide is also used as a research tool to study cholinergic signaling pathways and smooth muscle physiology. |
| Molecular Formula |
C23H30BRNO3
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|---|---|
| Molecular Weight |
448.39
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| Exact Mass |
447.14
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| CAS # |
50-34-0
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| Related CAS # |
Propantheline-d3 bromide;64717-35-7;Propantheline;298-50-0
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| PubChem CID |
4934
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| Appearance |
White to off-white solid powder
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| Melting Point |
159-161°C
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| LogP |
1.734
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
27
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| Complexity |
474
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| Defined Atom Stereocenter Count |
0
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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 : ≥ 100 mg/mL (~223.02 mM)
H2O : ~50 mg/mL (~111.51 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.58 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.58 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.58 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 130 mg/mL (289.93 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| 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.
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