| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
Atropine methylbromide targets muscarinic acetylcholine receptors (mAChRs), acting as a competitive antagonist. It competes with acetylcholine for binding sites on these receptors. It exhibited significant inhibitory potency (92.0 nM) in assays targeting Chronic Active B-Cell Receptor Signaling. The compound's quaternary ammonium structure limits its ability to cross the blood-brain barrier, resulting in peripheral anticholinergic effects with minimal central nervous system activity.
|
|---|---|
| ln Vitro |
In vitro, Atropine methylbromide acts as a potent muscarinic receptor antagonist. It has an IC₅₀ of <0.1 nM in a radioligand binding assay using isolated porcine brain membranes. It exhibited significant inhibitory potency (92.0 nM) in assays targeting Chronic Active B-Cell Receptor Signaling. The compound's ability to inhibit muscarinic receptor-mediated signaling has been characterized in various cell-based assays.
|
| ln Vivo |
In vivo, Atropine methylbromide is used as a mydriatic for dilation of the pupil during ophthalmic examination. Its high polarity makes it particularly effective in relieving pyloric spasm in infants. Due to its reduced central nervous system penetration compared to atropine, it is preferred for peripheral applications where central anticholinergic effects are undesirable. It is also used to reverse neuromuscular block.
|
| Enzyme Assay |
The activity of Atropine methylbromide can be assessed using radioligand binding assays. Membranes prepared from tissues expressing muscarinic receptors (e.g., porcine brain membranes) are incubated with a radiolabeled muscarinic antagonist (e.g., [³H]N-methylscopolamine) and varying concentrations of Atropine methylbromide. Non-specific binding is determined in the presence of an excess of a competing ligand. The IC₅₀ or Ki values for displacement are calculated from competition binding curves.
|
| Cell Assay |
To evaluate the cellular effects of Atropine methylbromide, cells expressing muscarinic receptors are treated with the compound. The inhibition of acetylcholine-induced calcium mobilization, cAMP production, or other downstream signaling events 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.
|
| Animal Protocol |
In vivo studies with Atropine methylbromide typically involve administration to animal models via oral, intravenous, or topical (ophthalmic) routes. In models of pyloric spasm or other gastrointestinal motility disorders, the compound's efficacy in reducing spasms is assessed. Its mydriatic effects are evaluated by measuring pupil dilation in ophthalmic studies. Pharmacokinetic parameters, such as bioavailability and tissue distribution, are also characterized.
|
| ADME/Pharmacokinetics |
Atropine methylbromide has a molecular formula of C₁₈H₂₆BrNO₃ and a molecular weight of 384.308 g/mol. Its CAS number is 2870-71-5. It is soluble in DMSO (149 mg/mL, 387.71 mM). For in vivo use, it can be formulated in 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline (4 mg/mL). Powder should be stored at -20°C for 3 years; in solvent at -80°C for 1 year.
|
| Toxicity/Toxicokinetics |
Specific toxicology data for Atropine methylbromide 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. Its reduced central nervous system penetration may limit central side effects compared to atropine.
|
| References | |
| Additional Infomation |
Atropine methylbromide (Methylatropine bromide) is a quaternary ammonium salt of atropine and a muscarinic receptor antagonist. It is used as a mydriatic for pupil dilation during ophthalmic examination and for relieving pyloric spasm in infants. Its high polarity limits central nervous system penetration, making it suitable for peripheral applications. It is a research tool for studying peripheral muscarinic receptor function and is not intended for systemic therapeutic use in research settings.
|
| Molecular Formula |
C18H26NO3.BR
|
|---|---|
| Molecular Weight |
384.31
|
| Exact Mass |
383.11
|
| CAS # |
2870-71-5
|
| Related CAS # |
2870-71-5 (bromide);52-88-0 (nitrate);
|
| PubChem CID |
656597
|
| Appearance |
White to off-white solid powder
|
| Melting Point |
222-223°
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
23
|
| Complexity |
387
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
C[N+]1([C@@H]2CC[C@H]1CC(C2)OC(=O)C(CO)C3=CC=CC=C3)C.[Br-]
|
| InChi Key |
XMLNCADGRIEXPK-ZNHDNBJUSA-M
|
| InChi Code |
InChI=1S/C18H26NO3.BrH/c1-19(2)14-8-9-15(19)11-16(10-14)22-18(21)17(12-20)13-6-4-3-5-7-13;/h3-7,14-17,20H,8-12H2,1-2H3;1H/q+1;/p-1/t14-,15+,16?,17?;
|
| Chemical Name |
[(1R,5S)-8,8-dimethyl-8-azoniabicyclo[3.2.1]octan-3-yl] 3-hydroxy-2-phenylpropanoate;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) |
DMSO : ~150 mg/mL (~390.31 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.51 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 (6.51 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 (6.51 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6021 mL | 13.0103 mL | 26.0207 mL | |
| 5 mM | 0.5204 mL | 2.6021 mL | 5.2041 mL | |
| 10 mM | 0.2602 mL | 1.3010 mL | 2.6021 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
