| 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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| 1g | |||
| Other Sizes |
| Targets |
Melperone targets dopamine D2 receptors in the brain, where it acts as an antagonist. It also has affinity for serotonin 5-HT2A receptors and α1-adrenergic receptors. Its antipsychotic effects are primarily mediated through D2 receptor blockade, while its lower propensity for extrapyramidal side effects compared to typical antipsychotics may be related to its 5-HT2A receptor antagonism.
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| ln Vitro |
In vitro, melperone has been shown to bind to dopamine D2 receptors, serotonin 5-HT2A receptors, and α1-adrenergic receptors. It inhibits receptor-mediated signaling pathways. It has been studied in cell lines expressing these receptors to determine its binding affinity and functional activity.
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| ln Vivo |
In vivo, melperone has antipsychotic effects in animal models and in clinical use. It reduces psychotic symptoms by blocking dopamine D2 receptors in the mesolimbic pathway. Its lower propensity for extrapyramidal side effects is attributed to its 5-HT2A receptor antagonism and its relatively low affinity for D2 receptors.
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| Enzyme Assay |
For non-cellular receptor binding assays, melperone can be evaluated for affinity to dopamine D2, serotonin 5-HT2A, and α1-adrenergic receptors using radioligand binding assays. Competitive binding experiments using [³H]spiperone (D2), [³H]ketanserin (5-HT2A), and [³H]prazosin (α1) are performed.
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| Cell Assay |
For in vitro cell-based assays, cells expressing the target receptors are cultured and treated with melperone. Receptor antagonism is measured by inhibition of agonist-induced signaling, such as calcium mobilization or cAMP accumulation.
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| Animal Protocol |
For in vivo animal studies, melperone can be administered to animal models. Behavioral assays for antipsychotic activity (such as conditioned avoidance response) can be used. Receptor occupancy studies can be performed to assess brain penetration and target engagement.
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Oral doses are rapidly absorbed (peak absorption time 1.5–3.0 hours after oral administration). Primarily excreted in the urine, with a small amount excreted unchanged. Metabolism/Metabolites Primarily metabolized in the liver. Biological Half-Life Approximately 3–4 hours after oral administration. After intramuscular injection, the half-life is approximately 6 hours. The pharmacokinetic properties of melperone include oral bioavailability, protein binding, and metabolism. It is metabolized in the liver and excreted in the urine. |
| Toxicity/Toxicokinetics |
Protein Binding
The bioavailability of melopiperone is 50-70%. The side effect profile of melperone includes sedation, orthostatic hypotension, and weight gain. It has a lower risk of extrapyramidal side effects compared to typical antipsychotics. |
| References |
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| Additional Infomation |
1-(4-fluorophenyl)-4-(4-methyl-1-piperidinyl)-1-butanone is an aromatic ketone. Meperone is an atypical antipsychotic, belonging to the butyrophenone class of compounds, and its structure is related to that of the typical antipsychotic haloperidol. Meperone has been used in the EU for over 30 years. It has been widely used to treat confusion, anxiety, agitation (especially in the elderly), and schizophrenia, and has good tolerability and safety. Recently, it has been investigated for the treatment of psychotic symptoms associated with Parkinson's disease. Drug Indications For the treatment of schizophrenia, sleep disorders, agitation, and confused states. Mechanism of Action Meperone has antagonistic activity against D2 dopaminergic receptors and 5HT2A serotonergic receptors. It has a weak affinity for D2 receptors, resulting in a low risk of inducing dopamine receptor hypersensitivity after acute or chronic administration. Furthermore, studies have shown that the dopamine D4/D2 receptor occupancy of meperone is similar to the binding characteristics of clozapine.
Melperone is a butyrophenone antipsychotic used in the treatment of schizophrenia and other psychotic disorders. It targets dopamine D2 and serotonin 5-HT2A receptors. It has a relatively favorable side effect profile compared to typical antipsychotics. |
| Molecular Formula |
C16H22FNO
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|---|---|
| Molecular Weight |
263.3504
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| Exact Mass |
263.169
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| CAS # |
3575-80-2
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| Related CAS # |
Melperone-d4 hydrochloride;1219798-80-7
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| PubChem CID |
15387
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| Appearance |
White to off-white solid powder
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| Density |
1.046g/cm3
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| Boiling Point |
376.1ºC at 760mmHg
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| Melting Point |
78-82°C
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| Flash Point |
181.3ºC
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| LogP |
3.458
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
19
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| Complexity |
279
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1C([H])=C([H])C(=C([H])C=1[H])C(C([H])([H])C([H])([H])C([H])([H])N1C([H])([H])C([H])([H])C([H])(C([H])([H])[H])C([H])([H])C1([H])[H])=O
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| InChi Key |
DKMFBWQBDIGMHM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H22FNO/c1-13-8-11-18(12-9-13)10-2-3-16(19)14-4-6-15(17)7-5-14/h4-7,13H,2-3,8-12H2,1H3
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| Chemical Name |
1-(4-fluorophenyl)-4-(4-methylpiperidin-1-yl)butan-1-one
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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) |
DMSO : ~41.67 mg/mL (~158.23 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.90 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 (7.90 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 (7.90 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 | 3.7972 mL | 18.9861 mL | 37.9723 mL | |
| 5 mM | 0.7594 mL | 3.7972 mL | 7.5945 mL | |
| 10 mM | 0.3797 mL | 1.8986 mL | 3.7972 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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