Identification | Back Directory | [Name]
FLUPHENAZINE DIMALEATE | [CAS]
3093-66-1 | [Synonyms]
Fluphenazine maleate FLUPHENAZINE DIMALEATE Fluphenazine Dimaleate, 98.0+ % (Titration) | [Molecular Formula]
C30H34F3N3O9S | [MDL Number]
MFCD00792778 | [MOL File]
3093-66-1.mol | [Molecular Weight]
669.666 |
Hazard Information | Back Directory | [Uses]
Fluphenazine dimaleate is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine dimaleate blocks neuronal voltage-gated sodium channels. Fluphenazine dimaleate acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine dimaleate can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine dimaleate can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2[1][2][3][4][6]. | [in vivo]
Fluphenazine (1 mg/kg; IG, treated from day 6 to day 15 of gestation) causes malformations in pregnant mice[5].
Fluphenazine (0.125-1 mg/kg; IP, single dosage) antagonizes Methylphenidate-induced stereotyped gnawing; inhibits significantly climbing behaviour[6]. Animal Model: | Mature female Swiss-Webster mice[5] | Dosage: | 1 mg/kg | Administration: | IG, treated from day 6 to day 15 of gestation | Result: | Significantly reduced fetal weight and length, increased the incidence of incomplete ossification of sternebrae and skull bones.
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Animal Model: | Mice (injected with 60 mg/kg Methylphenidate)[6] | Dosage: | 0.125, 0.25, 0.5, and 1 mg/kg | Administration: | IP, single dosage | Result: | Antagonized Methylphenidate-induced stereotyped gnawing; inhibited significantly climbing behaviour in mice at 0.0625-0.5 mg/kg, and at the dose of 1 mg/kg abolished this effect completely. |
| [References]
[1] Zhou X, et al. The neuroleptic drug, fluphenazine, blocks neuronal voltage-gated sodium channels. Brain Res. 2006 Aug 23;1106(1):72-81. DOI:10.1016/j.brainres.2006.05.076 [2] Nazeam J, et al. Based on Principles and Insights of COVID-19 Epidemiology, Genome Sequencing, and Pathogenesis: Retrospective Analysis of Sinigrin and ProlixinRX (Fluphenazine) Provides Off-Label Drug Candidates. SLAS Discov. 2020 Dec;25(10):1123-1140. DOI:10.1177/2472555220950236 [3] Siragusa S, Bistas KG, Saadabadi A. Fluphenazine. 2022 May 8. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2022 Jan. PMID:29083807 [4] Davis JL, et al. Peripheral diabetic neuropathy treated with amitriptyline and fluphenazine. JAMA. 1977 Nov 21;238(21):2291-2. PMID:29083807 [5] Abdel-Hamid HA, et al. Teratogenic effect of diphenylhydantoin and/or fluphenazine in mice. J Appl Toxicol. 1996 May-Jun;16(3):221-5. DOI:10.1002/(SICI)1099-1263(199605)16:33.0.CO;2-Q [6] Langwiński R, Niedzielski J. Narcotic analgesics and stereotyped behaviour in mice. Naunyn Schmiedebergs Arch Pharmacol. 1980 Jul;312(3):225-7. DOI:10.1007/BF00499150 |
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