2. Membrane Transporter/Ion Channel GPCR/G Protein Neuronal Signaling Anti-infection
  3. Sodium Channel Dopamine Receptor SARS-CoV
  4. Fluphenazine

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.

The free form of the compound is prone to instability, it is advisable to consider the stable salt form (Fluphenazine dihydrochloride) that retains the same biological activity.

For research use only. We do not sell to patients.

Fluphenazine Chemical Structure

Fluphenazine Chemical Structure

CAS No. : 69-23-8

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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[1][2][3][4][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]
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.
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.
Clinical Trial
Molecular Weight

437.52

Formula

C22H26F3N3OS
CAS No.
SMILES

OCCN1CCN(CC1)CCCN2C3=C(SC4=C2C=C(C=C4)C(F)(F)F)C=CC=C3
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Fluphenazine Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Fluphenazine69-23-8Sodium ChannelDopamine ReceptorSARS-CoVNa channelsNa+ channelsSARS coronavirusneuronal voltage-gated sodium channelsoralschizophreniaphenothiazinegnawingclimbing behaviourpsychosisdiabetesSARS-CoV-2malformationsSwiss-Webster miceInhibitorinhibitorinhibit

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