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| Targets |
Beperidium iodide targets acetylcholine receptors, specifically the M1 and M3 muscarinic receptor subtypes. It acts as a competitive antagonist at these receptors. The compound has a pA2 value of 7.93 in isolated guinea-pig ileum, indicating potent antagonism. By blocking muscarinic receptors in peripheral smooth muscle and glands, Beperidium iodide inhibits smooth muscle contraction and glandular secretion. It is used as an antispasmodic and bronchodilator agent.
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| ln Vitro |
In vitro studies have shown that Beperidium iodide has a competitive antagonistic effect against acetylcholine receptors, with a pA2 value of 7.93 in isolated guinea-pig ileum. This indicates potent antagonism of muscarinic receptors. The compound's activity has been characterized in smooth muscle contraction assays, demonstrating its ability to inhibit acetylcholine-induced contractions. As an M1/M3 receptor antagonist, it blocks cholinergic signaling in peripheral tissues. Its antispasmodic properties have been confirmed in various in vitro models.
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| ln Vivo |
In vivo, Beperidium iodide has been used as an anticholinergic agent for the treatment of respiratory disorders such as chronic obstructive pulmonary disease (COPD) and asthma. It acts as a bronchodilator by relaxing airway smooth muscle. The compound also relieves gastrointestinal spasms and hypersecretion by inhibiting smooth muscle contraction and glandular secretion. Its clinical use has been reported in some countries, though it is not widely used. Its in vivo effects are consistent with its mechanism as a muscarinic receptor antagonist.
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| Enzyme Assay |
The in vitro assay for Beperidium iodide typically involves measuring its antagonistic effect on acetylcholine-induced contractions in isolated tissue preparations, such as guinea-pig ileum. The tissue is mounted in an organ bath and contractions are elicited by adding acetylcholine. Varying concentrations of Beperidium iodide are added to the bath, and the reduction in contraction amplitude is measured. The pA2 value of 7.93 is determined from Schild plot analysis. Data are analyzed using standard pharmacological methods to determine antagonist potency.
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| Cell Assay |
In vitro cellular assays for Beperidium iodide are conducted using cells expressing muscarinic receptors (M1, M3). Cells are treated with varying concentrations of Beperidium iodide, and receptor activation is assessed by measuring intracellular calcium mobilization or by using reporter gene assays. The compound's ability to inhibit agonist-induced responses is quantified. The IC50 values are determined from dose-response curves. Selectivity for M1/M3 receptors over other receptor subtypes can be assessed. All experiments are performed in triplicate with appropriate controls.
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| Animal Protocol |
In vivo animal studies for Beperidium iodide are typically performed in animal models of bronchoconstriction or gastrointestinal motility. For respiratory studies, animals are challenged with a bronchoconstrictor (e.g., histamine, methacholine), and the compound's ability to prevent bronchoconstriction is assessed by measuring airway resistance. For gastrointestinal studies, the compound's effects on intestinal motility or gastric secretion are evaluated. Standard study designs with vehicle control and positive control groups are employed. Specific published protocols are not available in the provided sources.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Beperidium iodide are not extensively reported. The compound has a molecular weight of 527.44 g/mol and a molecular formula of C23H34IN3O3. As a quaternary ammonium compound, it is poorly absorbed from the gastrointestinal tract and is typically administered via inhalation or injection. Its limited systemic absorption reduces systemic side effects. Specific pharmacokinetic parameters such as half-life, bioavailability, and tissue distribution are not provided in the available sources.
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| Toxicity/Toxicokinetics |
Toxicology data for Beperidium iodide are not extensively reported. As an anticholinergic agent, its side effects are related to its mechanism of action and include dry mouth, blurred vision, constipation, and urinary retention. At high doses, it can cause tachycardia and central nervous system effects. The compound has been used clinically, suggesting an acceptable safety profile for its indications. Specific toxicity data, including LD50 values and organ toxicity profiles, are not provided in the available sources.
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| References | |
| Additional Infomation |
Beperidium iodide is a quaternary ammonium anticholinergic agent that acts as a competitive antagonist at muscarinic acetylcholine receptors (M1/M3). It has a pA2 value of 7.93 in guinea-pig ileum. The compound inhibits smooth muscle contraction and glandular secretion and has been used to treat respiratory disorders (COPD, asthma) and gastrointestinal spasms. It has a molecular weight of 527.44 g/mol and a molecular formula of C23H34IN3O3.
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| Molecular Formula |
C23H34IN3O3
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| Molecular Weight |
527.438838481903
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| Exact Mass |
527.164
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| CAS # |
86434-57-3
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| PubChem CID |
72012
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| Appearance |
White to off-white solid powder
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| LogP |
0.817
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
30
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| Complexity |
542
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
XEHKKWZHSSPBNZ-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C23H34N3O3.HI/c1-3-26(2)16-12-18(13-17-26)28-23(27)22(25-14-8-4-5-9-15-25)21-19-10-6-7-11-20(19)29-24-21;/h6-7,10-11,18,22H,3-5,8-9,12-17H2,1-2H3;1H/q+1;/p-1
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| Chemical Name |
(1-ethyl-1-methylpiperidin-1-ium-4-yl) 2-(azepan-1-yl)-2-(1,2-benzoxazol-3-yl)acetate;iodide
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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 : ≥ 100 mg/mL (~189.60 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.74 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 (4.74 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 (4.74 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 | 1.8960 mL | 9.4798 mL | 18.9595 mL | |
| 5 mM | 0.3792 mL | 1.8960 mL | 3.7919 mL | |
| 10 mM | 0.1896 mL | 0.9480 mL | 1.8960 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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