| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Fluspirilene is a non-competitive L-type calcium channel antagonist with an IC50 of 0.03 μM. It is also a dopamine receptor antagonist, with high affinity for dopamine D2 receptors. Its clinical effects are mediated primarily by blockade of striatal and mesolimbic D2 receptors. It has lower intrinsic activity at muscarinic receptors and shows adrenergic alpha1 antagonism that contributes to orthostatic effects. Fluspirilene is a relatively long-acting injectable depot antipsychotic drug used for schizophrenia.
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| ln Vitro |
Anti-calcium channel activators' effects are selectively limited by fluspirilene at doses that change dihydropyridine binding non-competitively [1]. The viability of astrocytoma stem cell lines is lowered and spheroid formation is inhibited by fluspirilene in a dose-dependent manner. At 1.25, 2.5, and 5 μM, it inhibits the growth of T98, U87, and all GSC cell lines. At 2.5 and 5 μM, it inhibits the growth of U251 and SNB19 [2].
In vitro, Fluspirilene is a non-competitive L-type calcium channel antagonist with an IC50 of 0.03 μM. It is also a dopamine receptor antagonist. The compound's in vitro activity is characterized by potent inhibition of L-type calcium channels and dopamine receptors. Fluspirilene has lower intrinsic activity at muscarinic receptors. Its effects on calcium channels and dopamine receptors contribute to its antipsychotic activity. |
| ln Vivo |
Fluspirilene-treated mouse models demonstrated a notable decrease in volume. Fluspirilene considerably increased the TGS04 mouse model's survival time [2].
In vivo, Fluspirilene is a relatively long-acting injectable depot antipsychotic drug used for schizophrenia. It is formulated as a sustained-release drug and administered parenterally. Fluspirilene does not differ greatly from other depot antipsychotics with respect to treatment efficacy, response, or tolerability. Its in vivo effects are mediated primarily by blockade of striatal and mesolimbic D2 receptors. The compound's long-acting formulation provides sustained antipsychotic effects. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for Fluspirilene typically involve measuring its binding affinity to dopamine D2 receptors and L-type calcium channels. Radioligand binding assays using membrane preparations expressing these targets are performed to determine the binding affinity. These assays confirm the compound's mechanism of action as a dopamine receptor antagonist and calcium channel blocker. The compound's selectivity for D2 receptors over other receptor subtypes can also be assessed.
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| Cell Assay |
In vitro cellular assays for Fluspirilene typically involve measuring its effects on calcium channel activity or dopamine receptor signaling. The compound inhibits L-type calcium channels with an IC50 of 0.03 μM. Its effects on dopamine receptor signaling can be assessed using cAMP assays or other downstream signaling assays. These cell-based studies demonstrate the compound's functional antagonism at dopamine receptors and calcium channels.
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| Animal Protocol |
In vivo animal models for Fluspirilene are not typically used in research settings, as it is a well-established clinical antipsychotic. However, animal models have been used to study its antipsychotic efficacy and safety. Fluspirilene is a relatively long-acting injectable depot antipsychotic drug. Its efficacy and safety have been established through clinical use. Fluspirilene is for research use only and is not approved for human therapeutic use in many applications.
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| ADME/Pharmacokinetics |
Fluspirilene has a molecular formula of C29H31F2N3O and a molecular weight of 475.57 g/mol. It is a diphenylbutylpiperidine typical antipsychotic. The compound is typically stored under appropriate conditions to maintain stability. Its physicochemical properties support its use in both in vitro and in vivo studies. Fluspirilene's solubility and formulation for administration should be optimized based on specific experimental requirements. The compound is also used as a precursor for the development of 20S proteasome agonists.
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| Toxicity/Toxicokinetics |
Fluspirilene is an antipsychotic drug with a well-characterized safety profile. Common adverse effects include extrapyramidal symptoms, sedation, and orthostatic hypotension. The compound should be used with caution in patients with cardiovascular disease. Its safety profile is similar to other typical antipsychotics. Fluspirilene is for research use only and is not approved for human therapeutic use in many applications.
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| References | |
| Additional Infomation |
8-[4,4-bis(4-fluorophenyl)butyl]-1-phenyl-1,3,8-triazaspiro[4.5]decane-4-one is a diarylmethane compound.
A long-acting injectable antipsychotic for the treatment of chronic schizophrenia. A long-acting injectable antipsychotic for the treatment of chronic schizophrenia. Indications For the treatment of schizophrenia. Pharmacodynamics Fluperidine is a relatively long-acting, sustained-release injectable antipsychotic for the treatment of schizophrenia. Fluperidine showed no significant differences in therapeutic efficacy, response, or tolerability compared to other sustained-release antipsychotics (fluphenazine decanoate, fluphenazine enoxalate, onanacillin piperothiazide, piperothiazide undecenoate). The results indicated that fluperidine did not differ significantly from oral antipsychotics or different weekly dosing regimens, but due to the limited number of trials, few conclusions could be drawn. Fluspirilene (CAS# 1841-19-6), also known as R 6218 or Imap, is a long-acting injectable depot antipsychotic drug used for the treatment of schizophrenia. It is a non-competitive L-type calcium channel antagonist with an IC50 of 0.03 μM. Fluspirilene is also a dopamine receptor antagonist. Its clinical effects are mediated primarily by blockade of striatal and mesolimbic D2 receptors. The compound is for research use only and is not approved for human therapeutic use in many applications. |
| Molecular Formula |
C29H31N3OF2
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|---|---|
| Molecular Weight |
475.57274
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| Exact Mass |
475.243
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| CAS # |
1841-19-6
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| Related CAS # |
1841-19-6;
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| PubChem CID |
3396
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
668.9±55.0 °C at 760 mmHg
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| Melting Point |
187.5-190°
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| Flash Point |
358.3±31.5 °C
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| Vapour Pressure |
0.0±2.0 mmHg at 25°C
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| Index of Refraction |
1.632
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| LogP |
3.89
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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 |
35
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| Complexity |
653
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
QOYHHIBFXOOADH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C29H31F2N3O/c30-24-12-8-22(9-13-24)27(23-10-14-25(31)15-11-23)7-4-18-33-19-16-29(17-20-33)28(35)32-21-34(29)26-5-2-1-3-6-26/h1-3,5-6,8-15,27H,4,7,16-21H2,(H,32,35)
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| Chemical Name |
8-[4,4-bis(4-fluorophenyl)butyl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-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 : ~25 mg/mL (~52.57 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.26 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 25.0 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: ≥ 2.5 mg/mL (5.26 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1027 mL | 10.5137 mL | 21.0274 mL | |
| 5 mM | 0.4205 mL | 2.1027 mL | 4.2055 mL | |
| 10 mM | 0.2103 mL | 1.0514 mL | 2.1027 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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