[CAS NO. 5002-47-1]??Fluphenazine decanoate
PRODUCTS SPECIFICATIONS [5002-47-1]
DESCRIPTION [5002-47-1]
Overview
| MDL | MFCD00798504 |
|---|---|
| Molecular Weight | 591.77 |
| Molecular Formula | C32H44F3N3O2S |
| SMILES | CCCCCCCCCC(OCCN1CCN(CCCN2C3=C(C=CC=C3)SC4=CC=C(C(F)(F)F)C=C24)CC1)=O |
Summary
Fluphenazine decanoate is a dopamine D 2 receptor inhibitor, is a long-acting phenothiazine neuroleptic . Fluphenazine can be used for schizophrenia research [1] [2] [3] .
IC50 & Target
|
D 2 Receptor |
In Vitro
Fluphenazine decanoate shows activity against
T. gondii
in human fibroblast cell cultures with an IC
50
value of 1.7 mM
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Fluphenazine decanoate (0.22 mg/kg and followed by 0.33 mg/kg; i.m.; 8 times every 3 weeks), as an antipsychotic, increases sensitivity to dopamine on monkey model following extended treatment
[2]
.
Fluphenazine decanoate (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 (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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Cebus apella monkey [2] |
| Dosage: | 0.22 mg/kg and followed by 0.33 mg/kg |
| Administration: | Intramuscular injection; 8 times per 3 weeks; 0.22 mg/kg for 63 weeks and 0.33 mg/kg for 6 weeks |
| Result: |
Decreased the aggressiveness composite behavioral variables (CBV).
Resulted stereotypic behavior induced by agonist and decreased prolactin response to AMPH. |
| Animal Model: | Male Sprague-Dawley rats (250 g) [3] |
| Dosage: | 25 mg/kg |
| Administration: | Intramuscular injection into the hind limb; 24 weeks |
| Result: | Resulted in spontaneous vacuous chewing mouth movements and jaw tremor. |
| Animal Model: | Adult male rats [4] |
| Dosage: | 1, 2, 3 mg/kg/d |
| Administration: | Subcutaneous injection between 10:00-12:00 h; 60 days |
| 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. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00014001 | National Institute of Mental Health (NIMH) |
Schizophrenia
|
December 2000 | Phase 4 |
| NCT00356200 | Tufts Medical Center|Immune Control |
Psoriasis
|
July 2006 | Phase 2 |
Appearance
Oil
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Pure form | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 125 mg/mL ( 211.23 mM ; Need ultrasonic)
Ethanol : 50 mg/mL ( 84.49 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |
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.
Synonyms