| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| 1g |
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| 5g |
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| 10g |
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| Other Sizes |
| Targets |
5-HT1A Receptor 101 nM (IC50)
Alverine citrate targets smooth muscle cells in the gastrointestinal tract. It acts as a calcium channel blocker, effectively inhibiting calcium ions from entering the smooth muscle cells of the intestinal wall. By reducing calcium influx, it prevents muscle contraction and relieves spasms. This mechanism helps to improve symptoms of diarrhea or frequent bowel movements and alleviates abdominal pain caused by intestinal cramps. |
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| ln Vitro |
One medication for functional gastrointestinal problems is alverine. Alverine relaxes the gut muscle immediately by acting on it. The action of 5-HTP is suppressed by alverine citrate (20 mg/kg), but not that of 8-OH-DPAT. Nevertheless, alverine citrate injection intracerebroventricularly (75 μg/rat) lessens the increase of abdominal contractions generated by rectal distension due to 8-OH-DPAT. Alverine citrate has a poor affinity for 5-HT3 and 5-HT4 subtypes and a high affinity for 5-HT1A receptors, according to in-vitro binding studies[1]. Due to its ability to prevent the inactivation of L-type Ca channels, alverine has the potential to increase Ca inflow during action potentials. However, it also has the potential to reduce evoked activity by reducing the sensitivity of contractile proteins to Ca2+ [2].
In vitro, Alverine citrate is used in pharmacological studies to investigate its smooth muscle relaxant properties. Its activity is typically assessed by measuring its ability to inhibit contractile responses in isolated smooth muscle preparations, such as guinea pig ileum or rat colon. The compound's effects on calcium influx and muscle contraction are studied using organ bath assays and electrophysiological techniques. |
| ln Vivo |
In vivo, Alverine citrate is used clinically to treat functional gastrointestinal disorders, including irritable bowel syndrome. It is effective in relieving abdominal pain, bloating, and intestinal spasms. It is available in oral formulations, often in combination with simethicone. The compound is well-tolerated and has been used for many years in clinical practice.
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| Enzyme Assay |
For non-cell-based receptor binding assays, Alverine citrate is not typically used. Its mechanism of action is on smooth muscle contractility rather than through a specific receptor. It can be studied in organ bath assays using isolated tissue preparations, where its effects on muscle contraction are measured. It is not used in standard radioligand binding displacement assays.
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| Cell Assay |
For in vitro cellular assays, cells expressing calcium channels or smooth muscle cells can be used. For functional assays, intracellular calcium mobilization is measured using fluorescent calcium indicators. Cells are treated with various concentrations of Alverine citrate, and calcium influx is stimulated by depolarizing agents. The reduction in calcium signal compared to control indicates calcium channel blocking activity. IC50 values are calculated from dose-response curves.
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| Animal Protocol |
For in vivo animal studies, Alverine citrate can be administered to rodents via oral gavage. In models of gastrointestinal motility, its effects on intestinal transit and colonic motility are assessed. In models of visceral pain, its effects on abdominal pain responses are evaluated. Dosing regimens vary depending on the specific model and desired exposure levels. Blood and tissue samples may be collected for pharmacokinetic analysis.
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| ADME/Pharmacokinetics |
Alverine citrate has a molecular weight of 473.56 and a molecular formula of C26H35NO7. It is a white to almost white powder. The compound is soluble in DMSO. It should be stored at room temperature. It is available as a pharmaceutical ingredient and for research purposes.
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| Toxicity/Toxicokinetics |
The toxicity profile of Alverine citrate is well established from clinical use. It is generally well-tolerated. Common side effects may include nausea, headache, and dizziness. Serious adverse effects are rare. The compound is for research use only and is not intended for human consumption outside of approved clinical indications.
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| References | |
| Additional Infomation |
Alverine citrate is the citrate salt of Alverine, produced by the reaction of equimolar amounts of Alverine and citric acid. It is an antispasmodic that acts directly on the smooth muscle of the intestine and uterus, and is used to treat irritable bowel syndrome. It has a dual role as both a cholinergic antagonist and an antispasmodic agent. It is a citrate and an organic ammonium salt. It contains an Alverine(1+) ion.
Alverine citrate (NSC 35459, CAS 5560-59-8) is a smooth muscle relaxant used to treat functional gastrointestinal disorders, including irritable bowel syndrome. It works by inhibiting calcium influx into smooth muscle cells. It is often combined with simethicone. It is available for research purposes only. |
| Molecular Formula |
C26H35NO7
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|---|---|
| Molecular Weight |
473.56
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| Exact Mass |
473.241
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| CAS # |
5560-59-8
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| Related CAS # |
150-59-4 (Parent)
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| PubChem CID |
21718
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| Appearance |
White to off-white solid powder
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| Boiling Point |
358.8ºC at 760mmHg
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| Flash Point |
174.4ºC
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| LogP |
3.325
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
34
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| Complexity |
442
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCN(CCCC1=CC=CC=C1)CCCC2=CC=CC=C2.C(C(=O)O)C(CC(=O)O)(C(=O)O)O
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| InChi Key |
RYHCACJBKCOBTJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H27N.C6H8O7/c1-2-21(17-9-15-19-11-5-3-6-12-19)18-10-16-20-13-7-4-8-14-20;7-3(8)1-6(13,5(11)12)2-4(9)10/h3-8,11-14H,2,9-10,15-18H2,1H3;13H,1-2H2,(H,7,8)(H,9,10)(H,11,12)
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| Chemical Name |
N-ethyl-3-phenyl-N-(3-phenylpropyl)propan-1-amine;2-hydroxypropane-1,2,3-tricarboxylic acid
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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 (211.17 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.28 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 (5.28 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 (5.28 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 | 2.1117 mL | 10.5583 mL | 21.1166 mL | |
| 5 mM | 0.4223 mL | 2.1117 mL | 4.2233 mL | |
| 10 mM | 0.2112 mL | 1.0558 mL | 2.1117 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.
Link: https://clinicaltrials.gov/ct2/show/NCT05508633
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