| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
Fluanisone acts as a typical antipsychotic, likely through antagonism of dopamine D2 receptors in the brain. As a butyrophenone derivative, it is structurally related to haloperidol. Its mechanism of action involves blocking dopamine receptors, particularly in the mesolimbic and mesocortical pathways, which reduces the positive symptoms of schizophrenia. The compound also has sedative properties.
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| ln Vitro |
In vitro studies demonstrate that fluanisone binds to dopamine D2 receptors, consistent with its antipsychotic mechanism. Its receptor binding profile includes affinity for dopamine D2 and possibly other neurotransmitter receptors. The compound's activity can be quantified in radioligand binding assays using [³H]-spiperone or other D2-selective radioligands.
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| ln Vivo |
Fluanisone is used in vivo as an antipsychotic for the treatment of schizophrenia. It has sedative properties and is a typical antipsychotic of the butyrophenone class. The compound's effects on psychotic symptoms have been demonstrated in clinical studies. It is used in some countries for the management of schizophrenia and other psychotic disorders.
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| Enzyme Assay |
For non-cellular receptor binding assays, fluanisone's affinity for dopamine D2 receptors can be evaluated using radioligand binding displacement studies. Membrane preparations from rat striatum or cells expressing human D2 receptors are incubated with [³H]-spiperone and varying concentrations of fluanisone. Binding displacement curves are generated to determine the IC₅₀ and Ki values for D2 receptor binding.
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| Cell Assay |
In vitro cellular assays for fluanisone involve treating dopamine receptor-expressing cells with the compound and measuring receptor-mediated signaling. Functional assays typically measure the inhibition of dopamine-stimulated cAMP accumulation in D2 receptor-expressing cells. Cells are treated with dopamine in the presence of varying concentrations of fluanisone, and cAMP levels are quantified.
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| Animal Protocol |
In vivo animal experiments with fluanisone involve administering the compound to rodent models of psychosis or dopamine-mediated behaviors. Conditioned avoidance response tests and apomorphine-induced stereotypy models are used to assess antipsychotic activity. Catalepsy tests evaluate extrapyramidal side effects. Pharmacokinetic and toxicological studies are conducted in rodents and other species.
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| ADME/Pharmacokinetics |
Fluanisone has a molecular weight of 356.43 and a molecular formula of C₂₁H₂₅FN₂O₂. It is a solid at room temperature and is typically stored at room temperature. The compound is soluble in chloroform, sparingly soluble in methanol, and slightly soluble in ether. Purity is typically ≥98%. It is stable under recommended storage conditions.
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| Toxicity/Toxicokinetics |
Fluanisone, like other typical antipsychotics, can cause extrapyramidal side effects including parkinsonism, dystonia, akathisia, and tardive dyskinesia due to its dopamine D2 receptor antagonism. It may also cause sedation, anticholinergic effects, and endocrine disturbances. The compound should be used with caution in patients with cardiovascular disease.
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| References |
: Arterial blood gas parameters in pet rabbits anaesthetized using a combination of fentanyl-fluanisone-midazolam-isoflurane. J Small Anim Pract. 2013 Jul;54(7):343-6. doi: 10.1111/jsap.12081. Epub 2013 May 10. PubMed PMID: 23659374.
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| Additional Infomation |
Fluanisone is an aromatic ketone.
Fluanisone is a butyrophenone derivative with sedative properties. It is a typical antipsychotic used in the treatment of schizophrenia. The compound is structurally related to haloperidol and acts through dopamine D2 receptor antagonism. It is available from various commercial suppliers for research applications. |
| Molecular Formula |
C21H25FN2O2
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|---|---|
| Molecular Weight |
356.44
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| Exact Mass |
356.19
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| CAS # |
1480-19-9
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| Related CAS # |
17160-71-3 (mono-hydrochloride)
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| PubChem CID |
15139
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| Appearance |
White to off-white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
511.8±50.0 °C at 760 mmHg
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| Melting Point |
67.5-68.5°
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| Flash Point |
263.3±30.1 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.558
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| LogP |
3.43
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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 |
7
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| Heavy Atom Count |
26
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| Complexity |
432
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=CC=CC=C1N2CCN(CCCC(=O)C3=CC=C(C=C3)F)CC2
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| InChi Key |
IRYFCWPNDIUQOW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H25FN2O2/c1-26-21-7-3-2-5-19(21)24-15-13-23(14-16-24)12-4-6-20(25)17-8-10-18(22)11-9-17/h2-3,5,7-11H,4,6,12-16H2,1H3
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| Chemical Name |
1-(4-fluorophenyl)-4-(4-(2-methoxyphenyl)piperazin-1-yl)butan-1-one
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| Synonyms |
R-2167R 2167 R2167Fluanisone MD 20282028 MD NSC 170977 R 2028 R2028 R-2028
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.8055 mL | 14.0276 mL | 28.0552 mL | |
| 5 mM | 0.5611 mL | 2.8055 mL | 5.6110 mL | |
| 10 mM | 0.2806 mL | 1.4028 mL | 2.8055 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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