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F100

Fluspirilene

Name: Fluspirilene
Brand: SIGMA

Sinonimo/i:

8-[4,4-bis(p-Fluorophenyl)butyl]-1-phenyl-1,3,8-triazino[4.5]decan-4-one, R 6218

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Informazioni su questo articolo

Formula empirica (notazione di Hill):

C₂₉H₃₁F₂N₃O

Numero CAS:

1841-19-6

Peso molecolare:

475.57

NACRES:

NA.77

PubChem Substance ID:

24277915

UNSPSC Code:

12352200

EC Number:

217-418-6

MDL number:

MFCD00055137

Assay:

≥98% (HPLC)

Form:

solid

Quality level:

200

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assay

≥98% (HPLC)

Quality Level

200

form

solid

color

white

solubility

DMSO: ≥20 mg/mL, H₂O: insoluble, ethanol: soluble

originator

Johnson & Johnson

storage temp.

room temp

SMILES string

Fc1ccc(cc1)C(CCCN2CCC3(CC2)N(CNC3=O)c4ccccc4)c5ccc(F)cc5

InChI

1S/C29H31F2N3O/c30-24-12-8-22(9-13-24)27(23-10-14-25(31)15-11-23)7-4-18-33-19-16-29(17-20-33)28(35)32-21-34(29)26-5-2-1-3-6-26/h1-3,5-6,8-15,27H,4,7,16-21H2,(H,32,35)

InChI key

QOYHHIBFXOOADH-UHFFFAOYSA-N

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1 of 1

Questo articolo	P3371	JN0006	L9668
Sigma-Aldrich F100 Fluspirilene	Sigma-Aldrich P3371 Penfluridol	Sigma-Aldrich JN0006 Draflazine	Sigma-Aldrich L9668 Lidoflazine
assay ≥98% (HPLC)	assay ≥97% (HPLC)	assay ≥98% (HPLC)	assay ≥98% (HPLC)
form solid	form powder	form powder	form powder
Quality Level 200	Quality Level 100	Quality Level -	Quality Level 100
storage temp. room temp	storage temp. 2-8°C	storage temp. room temp	storage temp. 2-8°C
solubility DMSO: ≥20 mg/mL, ethanol: soluble, H₂O: insoluble	solubility DMSO: >20 mg/mL, H₂O: insoluble	solubility DMSO: 2 mg/mL, clear	solubility DMSO: ≥10 mg/mL
color white	color white	color white to beige	color white

Application

Fluspirilene has been used as a neuroleptic drug to study its effects on human ether-a-go-go related gene (HERG).

Fluspirilene has been used to study its cytotoxicity effect on malignant glioma.

Biochem/physiol Actions

Fluspirilene has a potential to inhibit the activity of cyclin-dependent kinase 2 (CDK2). It is an effective anti-cancer agent used for treating human hepatocellular carcinoma.

Fluspirilene is a dopamine receptor antagonist. It also acts as a calcium channel blocker. Fluspirilene is an antipsychotic agent and exhibits neuoleptic properties. It exhibits therapeutic effects against glioblastoma and Schizophrenia.

Features and Benefits

This compound was developed by Johnson & Johnson. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Classe di stoccaggio

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)

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Certificati d'analisi (COA)

Lot/Batch Number

0000245411

0000144674

0000101994

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Inhibition of P-type and N-type calcium channels by dopamine receptor antagonists.

D W Sah et al.

Molecular pharmacology, 45(1), 84-92 (1994-01-01)

P-type Ca2+ channels in cerebellar Purkinje neurons and N-type Ca2+ channels in sympathetic neurons were found to be inhibited by D2 dopamine receptor antagonists with diverse structures, including phenothiazines (chlorpromazine and thioridazine), diphenylbutylpiperidines (fluspirilene and pimozide), butyrophenones (haloperidol and spiperone)

Identification of antipsychotic drug fluspirilene as a potential anti-glioma stem cell drug

Dong Y, et al.

Oncotarget, 8(67), 111728-111728 (2017)

Fluspirilene block of N-type calcium current in NGF-differentiated PC 12 cells

Grantham, CJ and Main, MJ and Cannell, MB

British Journal of Pharmacology, 111(2), 483-488 (1994)

The pharmacology of fluspirilene (R 6218), a potent, long-acting and injectable neuroleptic drug.

P A Janssen et al.

Arzneimittel-Forschung, 20(11), 1689-1698 (1970-11-01)

Neuroleptics of the diphenylbutylpiperidine series are potent calcium channel inhibitors.

J P Galizzi et al.

Proceedings of the National Academy of Sciences of the United States of America, 83(19), 7513-7517 (1986-10-01)

[3H]Fluspirilene, a neuroleptic molecule of the diphenylbutylpiperidine series, binds to skeletal muscle transverse tubule membranes with a high affinity corresponding to a Kd of 0.11 +/- 0.04 nM, A 1:1 stoichiometry was found between [3H]fluspirilene binding and the binding of

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Numero articolo commerciale globale

SKU	GTIN
F100-50MG	04061832090740
F100-10MG	04061832090733

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