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| Targets |
Piperazine citrate targets GABA receptors as an agonist. By activating GABA receptors in nematode parasites, piperazine causes hyperpolarization of the muscle cell membrane, leading to flaccid paralysis of the worms. The paralyzed worms are then expelled from the host through normal peristalsis. Piperazine is also used in the reduction of blood pressure. Its mechanism as a GABA agonist is responsible for its anthelmintic activity.
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| ln Vitro |
Piperazine citrate is a potentially effective stent that has anti-inflammatory and analgesic properties [3]. One important component of antidepressants is piperazine citrate [4].
In vitro, piperazine citrate is an anthelmintic agent that acts as a GABA agonist. It causes flaccid paralysis of nematode parasites by activating GABA receptors on the parasite muscle cells. The compound is used in the treatment of ascariasis and enterobiasis. In cell-based assays, piperazine citrate treatment results in hyperpolarization of nematode muscle cells, leading to paralysis. The compound's effects on GABA receptors are assessed using electrophysiological methods. |
| ln Vivo |
In vivo, piperazine citrate is used as an anthelmintic agent for the treatment of parasitic infections. It is an alternative treatment for ascariasis caused by Ascaris lumbricoides (roundworm) and enterobiasis (oxyuriasis) caused by pinworm. Piperazine citrate is also used in the reduction of blood pressure. The compound is administered orally and is effective against intestinal nematodes. It is available as an over-the-counter or prescription medication in some countries.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for piperazine citrate involve measuring its binding affinity to GABA receptors. The receptor is incubated with a radiolabeled ligand and varying concentrations of piperazine. The displacement of the radiolabeled ligand is measured, and the IC₅₀ or Ki value is calculated. The compound's functional activity as a GABA agonist is assessed using electrophysiological methods measuring chloride flux. These assays confirm the compound's mechanism of action.
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| Cell Assay |
In vitro cell-based assays for piperazine citrate evaluate its effects on nematode muscle cells. Nematodes are cultured and treated with piperazine citrate, and muscle paralysis is assessed by observing motility. The compound's effects on GABA receptor-mediated chloride flux are assessed using patch-clamp electrophysiology. These assays confirm the compound's functional activity as a GABA agonist.
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| Animal Protocol |
In vivo animal experiments for piperazine citrate have been conducted in animal models of parasitic infection. Animals infected with nematodes are treated with piperazine citrate, and worm burden is assessed by counting parasites in the intestines. The compound's efficacy in reducing worm burden is evaluated. Pharmacokinetic studies are conducted to determine the compound's absorption, distribution, metabolism, and excretion. Comprehensive in vivo studies are available from clinical and veterinary use.
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| ADME/Pharmacokinetics |
Piperazine citrate is absorbed after oral administration and is excreted in urine. The compound has a molecular weight of 321.33 g/mol and is a white crystalline powder. It is soluble in water. The compound's pharmacokinetics have been characterized in clinical studies. Piperazine citrate is used as an anthelmintic agent and is available as a medication.
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| Toxicity/Toxicokinetics |
The toxicity of piperazine citrate is low at therapeutic doses. Common side effects include gastrointestinal disturbances, headache, and dizziness. High doses can cause neurotoxicity. The compound should be used with caution in patients with renal impairment or epilepsy. Piperazine citrate is available as an over-the-counter or prescription medication in some countries.
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| References |
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| Additional Infomation |
Piperazine citrate is an anthelmintic agent used in the treatment of parasitic infections, including ascariasis and enterobiasis. It is a GABA agonist. Piperazine citrate is also used in the reduction of blood pressure. It has a molecular formula of C₆H₈O₇·3/2 C₄H₁₀N₂ and a molecular weight of 321.33 g/mol. Piperazine citrate is available as an over-the-counter or prescription medication in some countries.
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| Molecular Formula |
C6H8O7.C4H10N2
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| Molecular Weight |
278.25912
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| CAS # |
144-29-6
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| Related CAS # |
Piperazine;110-85-0
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| Appearance |
White to off-white solid powder
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| Boiling Point |
812.2ºC
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| Melting Point |
183-187ºC
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| Flash Point |
445ºC
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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 : ~2.17 mg/mL (~6.75 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5938 mL | 17.9688 mL | 35.9376 mL | |
| 5 mM | 0.7188 mL | 3.5938 mL | 7.1875 mL | |
| 10 mM | 0.3594 mL | 1.7969 mL | 3.5938 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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