Fluphenazine decanoate dihydrochloride
Fluphenazine decanoate dihydrochloride is a CNS-penetrant dopamine D2 receptor inhibitor, is a long-acting phenothiazine neuroleptic. Fluphenazine can be used for schizophrenia research.
For research use only. We do not sell to patients.
- CAS No.: 2376-65-0
- Formula: C32H46Cl2F3N3O2S
- Molecular Weight:664.69
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Dopamine Receptor Isoforms
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Biological Activity
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D2 Receptor |
Fluphenazine decanoate dihydrochloride shows activity against T. gondii in human fibroblast cell cultures with an IC50 value of 1.7 mM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Fluphenazine decanoate dihydrochloride (25 mg/kg; i.m.; 6 times every 3 weeks; 24 weeks) induces mouth movements in the rat, serves as a pharmacological model of human tardive dyskinesia[3].
Fluphenazine decanoate dihydrochloride (1, 2, 3 mg/kg/d; s.c.; 60 d) shows antifertility effects and induces hyperprolactinemia concomitant with gonadotropin suppression in adult male rat[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Cebus apella monkey[2]
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Dosage:0.22 mg/kg and followed by 0.33 mg/kg
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Administration:Intramuscular injection; 8 times per 3 weeks; 0.22 mg/kg for 63 weeks and 0.33 mg/kg for 6 weeks
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Result:Decreased the aggressiveness composite behavioral variables (CBV).
Resulted stereotypic behavior induced by agonist and decreased prolactin response to AMPH.
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Animal Model:Male Sprague-Dawley rats (250 g)[3]
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Dosage:25 mg/kg
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Administration:Intramuscular injection into the hind limb; 24 weeks
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Result:Resulted in spontaneous vacuous chewing mouth movements and jaw tremor.
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Animal Model:Adult male rats[4]
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Dosage:1, 2, 3 mg/kg/d
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Administration:Subcutaneous injection between 10:00-12:00 h; 60 days
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Result:Increased serum prolactin level and suppressed serum LH and FSH levels at day 60.
Increased hypothalamic tyrosine hydroxylase levels, enhanced chromatin decondensation, and resulted DNA denaturation.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2376-65-0
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Molecular Weight 664.69
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Formula C32H46Cl2F3N3O2S
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SMILES
CCCCCCCCCC(OCCN1CCN(CCCN2C3=C(C=CC=C3)SC4=CC=C(C(F)(F)F)C=C24)CC1)=O.[H]Cl.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[4]. Gill-Sharma MK, et al. Antifertility effects of fluphenazine in adult male rats. J Endocrinol Invest. 2003 Apr;26(4):316-26. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
- Fluphenazine decanoate
- 2376-65-0
- Dopamine Receptor
- long-acting
- phenothiazine
- neuroleptic
- schizophrenia
- dopamine-D2
- reproductive
- T. gondii
- hypothalamic tyrosine hydroxylase levels
- human tardive dyskinesia
- gonadotropin suppression
- antifertility
- hyperprolactinemia
- mouth movements
- vacuous chewing mouth movement
- jaw tremor
- serum prolactin
- Inhibitor
- inhibitor
- inhibit