| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Fentonium bromide targets muscarinic acetylcholine receptors (mAChR), which are G protein-coupled receptors that mediate the effects of acetylcholine in the parasympathetic nervous system. As an anticholinergic agent, the compound blocks the action of acetylcholine at these receptors, inhibiting parasympathetic nerve impulses. This leads to reduced smooth muscle contraction, decreased secretions, and other anticholinergic effects. Its mechanism involves competitive antagonism of mAChR.
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| ln Vitro |
In vitro, fentonium bromide demonstrates anticholinergic activity by blocking muscarinic acetylcholine receptors. The compound inhibits acetylcholine-mediated signaling in cell-based assays, reducing calcium mobilization and other downstream effects. Its antispasmodic activity is measured using smooth muscle contraction assays. In cell-based systems, fentonium bromide shows concentration-dependent inhibition of muscarinic receptor activation. Its activity is compared to other anticholinergic agents.
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| ln Vivo |
Phenteronium bromide (phenythonium, 1 mg/kg, intraperitoneally) prevents stress ulcers in rats [1], while fentium bromide (1 mg/kg, iv) is a strong antagonist of gastric secretion in rats [1].
In vivo, fentonium bromide has been studied for its anti-ulcerogenic, anticholinergic, and antispasmodic effects. The compound is used in pharmacological research for gastrointestinal and neurological conditions. Its antispasmodic activity helps reduce smooth muscle spasms in the gastrointestinal tract. The compound's effects on bladder function have also been investigated. Its in vivo activity supports its use as a research tool for studying mAChR function. |
| Enzyme Assay |
The in vitro receptor binding assays for fentonium bromide involve assessment of binding affinity to muscarinic acetylcholine receptor subtypes. Competition binding assays are performed using radiolabeled ligands such as [³H]-NMS or [³H]-QNB to determine binding affinities (Ki values). Functional assays measure calcium mobilization or other signaling events in response to acetylcholine stimulation in the presence of fentonium bromide. The compound is tested at concentrations ranging from 0.1 nM to 100 µM. Reference anticholinergics such as atropine are used as positive controls.
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| Cell Assay |
In vitro cell-based experiments with fentonium bromide utilize cell lines expressing muscarinic acetylcholine receptors, such as CHO cells transfected with mAChR subtypes or neuronal cell lines. Cells are cultured in appropriate media and treated with fentonium bromide at various concentrations. Calcium mobilization is measured using fluorescent indicators in response to acetylcholine stimulation. Signaling pathway activation is assessed by Western blotting. Smooth muscle contraction is measured using organ bath preparations. All experiments include vehicle controls.
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| Animal Protocol |
Animal/Disease Models: carbamylcholine, pentagastrin and cerulein-induced gastric secretion in rats [1]
Doses: 1 mg/kg Route of Administration: intravenous (iv) (iv)injection Experimental Results: Inhibition of gastric acid secretion. Animal/Disease Models: Rat[2] Doses: 1 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: The number of pre-ulcerative lesions and the number of gastroduodenal ulcers were diminished compared with untreated controls. In vivo animal studies with fentonium bromide typically use rodent models to evaluate anticholinergic and antispasmodic effects. The compound is administered via oral or parenteral routes at doses determined from pharmacokinetic studies. Gastrointestinal motility is assessed by measuring intestinal transit or gastric emptying. Smooth muscle spasm is evaluated in models of induced contraction. Ulcer protection is assessed in gastric ulcer models. Bladder function is evaluated in cystometry studies. All procedures follow institutional animal care guidelines. |
| References |
| Molecular Formula |
C31H34BRNO4
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|---|---|
| Molecular Weight |
564.52
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| Exact Mass |
563.167
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| CAS # |
5868-06-4
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| PubChem CID |
71534
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| Appearance |
White to off-white solid powder
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| LogP |
1.958
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| tPSA |
63.6
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
37
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| Complexity |
734
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C[N+]1(C2CCC1CC(C2)OC(=O)C(CO)C3=CC=CC=C3)CC(=O)C4=CC=C(C=C4)C5=CC=CC=C5.[Br-]
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| InChi Key |
MPLNGQBULSHWQW-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C31H34NO4.BrH/c1-32(20-30(34)25-14-12-23(13-15-25)22-8-4-2-5-9-22)26-16-17-27(32)19-28(18-26)36-31(35)29(21-33)24-10-6-3-7-11-24;/h2-15,26-29,33H,16-21H2,1H3;1H/q+1;/p-1
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| Chemical Name |
[8-methyl-8-[2-oxo-2-(4-phenylphenyl)ethyl]-8-azoniabicyclo[3.2.1]octan-3-yl] 3-hydroxy-2-phenylpropanoate;bromide
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| Synonyms |
Fentonium bromide Z 326 FA 402
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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: ~130 mg/mL (~230.3 mM; with ultrasonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3.25 mg/mL (5.76 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 DMSO stock solution (32.5 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7714 mL | 8.8571 mL | 17.7142 mL | |
| 5 mM | 0.3543 mL | 1.7714 mL | 3.5428 mL | |
| 10 mM | 0.1771 mL | 0.8857 mL | 1.7714 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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