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MedChemExpressModel Fluphenazine -69-23-8

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Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine blocks neuronal voltage-gated sodium channels. Fluphenazine acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine 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].
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Fluphenazine

MCE China:Fluphenazine

Brand:MedChemExpress (MCE)

Cat. No.HY-119980

CAS:69-23-8

Storage:Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping:Room temperature in continental US; may vary elsewhere.

Description:Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine blocks neuronal voltage-gated sodium channels. Fluphenazine acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2.

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].

IC50 & Target:Dopamine receptor, Sodium channels, SARS-CoV-2[1][2] 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]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Mice (injected with 60 mg/kg Methylphenidate)[6]

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References:

[1]. Zhou X, et al. The neuroleptic drug, fluphenazine, blocks neuronal voltage-gated sodium channels. Brain Res. 2006;1106(1):72-81.  [Content Brief]

[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.  [Content Brief]

[3]. Siragusa S, Bistas KG, Saadabadi A. Fluphenazine. 2022 May 8. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2022 Jan.  [Content Brief]

[4]. Davis JL, et al. Peripheral diabetic neuropathy treated with amitriptyline and fluphenazine. JAMA. 1977 Nov 21;238(21):2291-2.  [Content Brief]

[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.  [Content Brief]

[6]. Langwiński R, Niedzielski J. Narcotic analgesics and stereotyped behaviour in mice. Naunyn Schmiedebergs Arch Pharmacol. 1980 Jul;312(3):225-7.  [Content Brief]

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