| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Pinaverium bromide selectively inhibits calcium influx through voltage-dependent calcium channels on the surface membranes of gastrointestinal smooth muscle cells. By blocking these channels, it reduces calcium ion entry into the smooth muscle cells. This leads to a spasmolytic effect, relaxing the gastrointestinal structures and relieving GI spasm, pain, and abnormal motility.
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|---|---|
| ln Vitro |
In vitro, pinaverium bromide (10⁻⁶-10⁻⁵ M) induces a spasmolytic effect on the longitudinal muscle layer of the colon. This effect is mediated by the reduction of calcium influx in the muscle cells, in a manner comparable to that of the typical calcium channel blocker D-600 (methoxyverapamil).
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| ln Vivo |
Pinaverium bromide is used in vivo as an orally administered antispasmodic for the treatment of gastrointestinal motility disorders. It relieves GI spasm, pain, and transit disturbances and is considered an effective first-line treatment for these conditions. In humans, pinaverium facilitates gastric emptying and decreases intestinal transit time in patients with constipation.
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| Enzyme Assay |
Non-cellular assays for pinaverium bromide are not standard, as it is a calcium channel blocker whose activity is assessed in functional tissue or cell-based assays. Its binding to voltage-dependent calcium channels can be studied using radioligand binding displacement studies with membrane preparations from intestinal smooth muscle.
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| Cell Assay |
In vitro cellular assays for pinaverium bromide involve treating isolated gastrointestinal smooth muscle cells or tissue strips with the compound and measuring contractile responses. Muscle strips are mounted in organ baths and stimulated with contractile agents (e.g., KCl, acetylcholine) in the presence of varying concentrations of pinaverium bromide. The reduction in contractile force is measured, and the IC₅₀ for spasmolytic activity is determined.
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| Animal Protocol |
In vivo animal experiments with pinaverium bromide are conducted in animal models of gastrointestinal motility. The compound is administered orally to rodents or other animals, and its effects on gastrointestinal transit time, intestinal motility, and intraluminal pressure are measured. The compound's ability to relieve induced spasms is also assessed in these models.
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| ADME/Pharmacokinetics |
Pinaverium bromide has a molecular weight of 511.45 and a molecular formula of C₂₆H₄₁Br₂NO₄. It is a white to off-white crystalline powder with a purity of ≥98%. The compound is typically stored at room temperature in a dry, dark place. It is soluble in water and is stable under recommended storage conditions.
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| Toxicity/Toxicokinetics |
Pinaverium bromide is generally well-tolerated at therapeutic doses. Side effects are rare but may include gastrointestinal disturbances, dry mouth, and dizziness. It is contraindicated in patients with known hypersensitivity to the drug. Standard safety precautions should be followed when handling the compound.
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| References |
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| Additional Infomation |
Pinaverium bromide is the oral bromide salt form of pivammonium, a calcium channel blocker (CCB) with antispasmodic effects. After oral administration, pivammonium blocks voltage-dependent calcium channels, inhibiting the influx of calcium ions into gastrointestinal smooth muscle cells. This prevents smooth muscle contraction and relaxes the gastrointestinal tract. Furthermore, pivammonium may reduce the absorption of locally active concomitant drugs in the intestine and enhance their effects.
Pinaverium bromide (CAS 53251-94-8) is a selective calcium channel blocker with antispasmodic activity on the gastrointestinal tract. It inhibits calcium influx through voltage-dependent calcium channels in GI smooth muscle cells, relieving spasm and pain. It is available as an oral medication (Dicetel) for the treatment of functional GI disorders. |
| Molecular Formula |
C26H41BR2NO4
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|---|---|
| Molecular Weight |
591.42
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| Exact Mass |
589.14
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| CAS # |
53251-94-8
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| Related CAS # |
Pinaverium bromide-d4
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| PubChem CID |
40703
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| Appearance |
White to off-white solid powder
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| Melting Point |
159-164ºC
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| LogP |
2.255
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
33
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| Complexity |
596
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
IKGXLCMLVINENI-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C26H41BrNO4.BrH/c1-26(2)21-6-5-19(22(26)16-21)7-11-31-12-8-28(9-13-32-14-10-28)18-20-15-24(29-3)25(30-4)17-23(20)27;/h15,17,19,21-22H,5-14,16,18H2,1-4H3;1H/q+1;/p-1
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| Chemical Name |
4-[(2-bromo-4,5-dimethoxyphenyl)methyl]-4-[2-[2-(6,6-dimethyl-2-bicyclo[3.1.1]heptanyl)ethoxy]ethyl]morpholin-4-ium;bromide
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| Synonyms |
LAT-1717; LAT 1717; Pinaverium bromide
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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 : ~50 mg/mL (~84.54 mM)
H2O : ~10 mg/mL (~16.91 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.52 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 20.8 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: ≥ 2.08 mg/mL (3.52 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 20.8 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: ≥ 2.08 mg/mL (3.52 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 | 1.6908 mL | 8.4542 mL | 16.9085 mL | |
| 5 mM | 0.3382 mL | 1.6908 mL | 3.3817 mL | |
| 10 mM | 0.1691 mL | 0.8454 mL | 1.6908 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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