| Size | Price | Stock | Qty |
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| 100mg |
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| Targets |
Piperacetazine targets dopamine receptors in the brain. As a phenothiazine antipsychotic, it acts as a dopamine receptor antagonist, blocking dopamine signaling in the mesolimbic and mesocortical pathways. This inhibition of dopamine receptors leads to a reduction in psychotic symptoms such as hallucinations and delusions. It may also have activity at other receptors including serotonin, histamine, and adrenergic receptors.
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| ln Vitro |
Piperacetazine demonstrates antipsychotic activity in vitro through dopamine receptor antagonism. Its binding affinity for dopamine D2 receptors and other receptors has been characterized in radioligand binding assays. Functional assays measure its ability to inhibit dopamine-induced signaling in cells expressing dopamine receptors. Its antipsychotic potency is correlated with its dopamine receptor affinity.
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| ln Vivo |
Piperacetazine is used clinically as an antipsychotic for the treatment of schizophrenia, bipolar disorder, and anxiety. Its in vivo efficacy has been established through clinical use. It reduces psychotic symptoms by inhibiting dopamine receptors in the brain. It is administered orally. Its therapeutic effects and side effect profile are characteristic of phenothiazine antipsychotics.
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| Enzyme Assay |
Dopamine receptor binding assays are performed using membranes prepared from cells expressing recombinant dopamine receptors (D1, D2, D3, D4, D5) or from brain tissue (striatum). Radioligand binding studies use [3H]-spiperone or [3H]-raclopride as labeled ligands. Membrane preparations are incubated with varying concentrations of Piperacetazine and a fixed concentration of radioligand in binding buffer for 60-120 minutes. Non-specific binding is determined using excess haloperidol. Bound radioactivity is measured by scintillation counting after filtration. IC50 and Ki values are calculated by non-linear regression.
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| Cell Assay |
Cellular dopamine receptor antagonism is evaluated in cell lines expressing recombinant dopamine receptors (e.g., HEK-293 cells transfected with D2 receptors). Cells are cultured in appropriate media and treated with Piperacetazine at various concentrations (0.1-100 µM). Functional assays measure receptor-mediated inhibition of cAMP accumulation (D2 receptors are Gi-coupled). The compound's antagonist activity is assessed by its ability to reverse dopamine-induced inhibition of cAMP. Cell viability is assessed using MTT or LDH assays. Each experiment includes known antipsychotics (e.g., haloperidol, chlorpromazine) as positive controls.
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| Animal Protocol |
In vivo studies are conducted in animal models of psychosis (e.g., amphetamine-induced hyperactivity, conditioned avoidance response). Piperacetazine is administered orally or intraperitoneally at doses determined by preclinical studies. Antipsychotic effects are assessed by inhibition of amphetamine-induced hyperactivity or conditioned avoidance response. Catalepsy is assessed as a measure of extrapyramidal side effects. Sample sizes typically range from 8-12 animals per group. Clinical studies have been conducted for schizophrenia, bipolar disorder, and anxiety.
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| ADME/Pharmacokinetics |
Piperacetazine has a molecular weight of 410.57 g/mol and a molecular formula of C24H30N2O2S. IUPAC name: 1-[10-[3-[4-(2-hydroxyethyl)piperidin-1-yl]propyl]phenothiazin-2-yl]ethanone. Appearance: solid. Storage: typically at room temperature. As an antipsychotic, it is orally administered. Pharmacokinetic parameters: it is absorbed from the gastrointestinal tract, metabolized in the liver, and excreted renally.
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| Toxicity/Toxicokinetics |
Piperacetazine is generally well-tolerated at therapeutic doses. Common adverse effects may include extrapyramidal symptoms (tardive dyskinesia, parkinsonism), sedation, dry mouth, and weight gain. It is contraindicated in patients with hypersensitivity to phenothiazines. Standard toxicology studies have demonstrated an acceptable safety profile. It is approved for clinical use in some countries.
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| Additional Infomation |
1-[10-[3-[4-(2-hydroxyethyl)-1-piperidinyl]propyl]-2-phenthiazinyl]acetone is a phenothiazine compound.
See also: phenothiazine (subclass). Piperacetazine is also known as 1-[10-[3-[4-(2-hydroxyethyl)-1-piperidinyl]propyl]-2-phenothiazinyl]ethanone. It is a potent antipsychotic drug used for schizophrenia, bipolar disorder, and anxiety. It is a member of the phenothiazines class. Regulatory approvals exist in some countries. |
| Molecular Formula |
C24H30N2O2S
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| Molecular Weight |
410.5722
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| Exact Mass |
410.203
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| CAS # |
3819-00-9
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| PubChem CID |
19675
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.17g/cm3
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| Boiling Point |
606.4ºC at 760mmHg
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| Melting Point |
99°C
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| Flash Point |
320.5ºC
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| Index of Refraction |
1.602
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| LogP |
4.979
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
29
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| Complexity |
537
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C(C=C1N2CCCN3CCC(CCO)CC3)=CC=C1SC4=C2C=CC=C4)=O
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| InChi Key |
BTFMCMVEUCGQDX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H30N2O2S/c1-18(28)20-7-8-24-22(17-20)26(21-5-2-3-6-23(21)29-24)13-4-12-25-14-9-19(10-15-25)11-16-27/h2-3,5-8,17,19,27H,4,9-16H2,1H3
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| Chemical Name |
1-[10-[3-[4-(2-hydroxyethyl)piperidin-1-yl]propyl]phenothiazin-2-yl]ethanone
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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 |
| 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) |
Ethanol : ~50 mg/mL (~121.78 mM)
DMSO : ≥ 6 mg/mL (~14.61 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.09 mM) (saturation unknown) in 10% EtOH + 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 EtOH 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 (6.09 mM) (saturation unknown) in 10% EtOH + 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 EtOH 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4356 mL | 12.1782 mL | 24.3564 mL | |
| 5 mM | 0.4871 mL | 2.4356 mL | 4.8713 mL | |
| 10 mM | 0.2436 mL | 1.2178 mL | 2.4356 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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