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| ln Vitro |
In human fibroblast cells, fluphenazine decanoate exhibits action against Toxoplasma gondii, with an IC50 value of 1.7 mM[1].
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| ln Vivo |
In monkey models, long-term treatment with the antipsychotic fluphenazine decanoate (0.22 mg/kg, then 0.33 mg/kg; IM; 8 times every 3 weeks) increases dopamine sensitivity [2]. In order to create a pharmacological model of human tardive dyskinesia, fluphenazine decanoate (25 mg/kg; intramuscular injection; six times every three weeks; 24 weeks) causes oral movements in rats [3]. In adult male rats, fluphenazine decanoate (1, 2, 3 mg/kg/d; SC; 60 days) causes hyperprolactinemia with gonadotropins and has antifertility effects[4].
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| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat (250 g) [3]
Doses: 25 mg/kg Route of Administration: intramuscularinjection of hind limbs; 24-week Experimental Results: Result in spontaneous chewing movements and mandibular tremors. Animal/Disease Models: adult male rats [4] Doses: 1, 2, 3 mg/kg/d Route of Administration: 10:00-12:00 h subcutaneous injection; 60-day Experimental Results: On the 60th day, serum prolactin levels increased High, serum LH and FSH levels are suppressed. The level of hypothalamic tyrosine hydroxylase increases and chromatin decondensation is enhanced, leading to DNA denaturation. |
| References |
[1]. Goodwin DG, et al. Evaluation of five antischizophrenic agents against Toxoplasma gondii in human cell cultures. J Parasitol. 2011 Feb;97(1):148-51.
[2]. Lifshitz K, et al. Effects of dopamine agonists on Cebus apella monkeys with previous long-term exposure to fluphenazine. Biol Psychiatry. 1997 Mar 15;41(6):657-67. [3]. Stoessl AJ, et al. Chronic neuroleptic-induced mouth movements in the rat: suppression by CCK and selective dopamine D1 and D2 receptor antagonists. Psychopharmacology (Berl). 1989;98(3):372-9. [4]. Gill-Sharma MK, et al. Antifertility effects of fluphenazine in adult male rats. J Endocrinol Invest. 2003 Apr;26(4):316-26. |
| Additional Infomation |
Fluphenazine decanoate is the prodrug of fluphenazine, an antipsychotic drug used for the symptomatic management of psychosis in patients with schizophrenia. It has a role as a phenothiazine antipsychotic drug, a prodrug and a dopaminergic antagonist. It is a member of phenothiazines, a decanoate ester, an organofluorine compound and a N-alkylpiperazine. It is functionally related to a fluphenazine.
Fluphenazine Decanoate is the decanoate salt form of fluphenazine, a phenothiazine with antipsychotic activity. Fluphenazine decanoate exerts its actions by blocking postsynaptic dopamine D2 receptors in the limbic, cortical system and basal ganglia. This prevents the actions of dopamine, thereby reducing the hallucinations and delusions that are associated with schizophrenia. |
| Molecular Formula |
C32H44F3N3O2S
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|---|---|
| Molecular Weight |
591.77
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| Exact Mass |
591.311
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| CAS # |
5002-47-1
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| Related CAS # |
Fluphenazine dihydrochloride;146-56-5;Fluphenazine decanoate dihydrochloride;2376-65-0
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| PubChem CID |
3388
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| Appearance |
Light yellow to yellow <30°C solid powder,>32°C liquid
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| Density |
1.149 g/cm3
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| Boiling Point |
658.1ºCat 760 mmHg
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| Melting Point |
30-32°
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| Flash Point |
351.8ºC
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| Index of Refraction |
1.537
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| LogP |
7.94
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
16
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| Heavy Atom Count |
41
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| Complexity |
765
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
VIQCGTZFEYDQMR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C32H44F3N3O2S/c1-2-3-4-5-6-7-8-14-31(39)40-24-23-37-21-19-36(20-22-37)17-11-18-38-27-12-9-10-13-29(27)41-30-16-15-26(25-28(30)38)32(33,34)35/h9-10,12-13,15-16,25H,2-8,11,14,17-24H2,1H3
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| Chemical Name |
2-[4-[3-[2-(trifluoromethyl)phenothiazin-10-yl]propyl]piperazin-1-yl]ethyl decanoate
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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 : ~125 mg/mL (~211.23 mM)
Ethanol : ~50 mg/mL (~84.49 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.08 mg/mL (1.83 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 10.8 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: ≥ 1.08 mg/mL (1.83 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 10.8 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: ≥ 1.08 mg/mL (1.83 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 | 1.6898 mL | 8.4492 mL | 16.8985 mL | |
| 5 mM | 0.3380 mL | 1.6898 mL | 3.3797 mL | |
| 10 mM | 0.1690 mL | 0.8449 mL | 1.6898 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00356200 | TERMINATEDWITH RESULTS | Drug: Fluphenazine Decanoate
Drug: Placebo |
Psoriasis | Tufts Medical Center | 2006-07 | Phase 2 |
| NCT05766007 | RECRUITING | Antipsychotic Agents Breastfeeding Drug Exposure Via Breast Milk Drug Exposure in Utero |
University of Liverpool | 2023-08-01 | ||
| NCT00014001 | COMPLETED | Drug: perphenazine Drug: olanzapine Drug: quetiapine |
Schizophrenia | National Institute of Mental Health (NIMH) | 2000-12 | Phase 4 |
| NCT02203786 | COMPLETEDWITH RESULTS | Drug: Haloperidol Drug: Fluphenazine Drug: Dexedrine |
Pathological Gambling | Centre for Addiction and Mental Health | 2009-09 | Phase 2 |
| NCT01323205 | COMPLETED | Drug: JNJ-40411813 Drug: JNJ-40411813 Drug: Placebo Drug: Antipsychotic medication |
Schizophrenia | Janssen Research & Development, LLC | 2011-05 | Phase 2 |
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