Flunarizine

Modify Date: 2024-01-02 15:51:55

Flunarizine Structure
Flunarizine structure
Common Name Flunarizine
CAS Number 52468-60-7 Molecular Weight 404.49500
Density 1.17 g/cm3 Boiling Point 511.3ºC at 760 mmHg
Molecular Formula C26H26F2N2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Flunarizine


Flunarizine is a potent dual Na+/Ca2+ channel (T-type) blocker. Flunarizine is a D2 dopamine receptor antagonist. Flunarizine shows anticonvulsive and antimigraine activity, and peripheral vasodilator effects[1][2][3][4][5].

 Names

Name Flunarizine
Synonym More Synonyms

 Flunarizine Biological Activity

Description Flunarizine is a potent dual Na+/Ca2+ channel (T-type) blocker. Flunarizine is a D2 dopamine receptor antagonist. Flunarizine shows anticonvulsive and antimigraine activity, and peripheral vasodilator effects[1][2][3][4][5].
Related Catalog
Target

D2 Receptor

In Vitro Flunarizine blocks sodium currents (INa) and calcium currents (ICa) with IC50 values of 0.94 μM and 1.77 μM in cultured rat cortical neurons, respectively[2]. Flunarizine (10 and 30 μM; 24 h) shows cytotoxic effects to chromaffin cells[4]. Flunarizine (1-30 μM) causes clear cytoprotection of chromaffin cell at concentrations of 3-10 μM[4]. Cell Cytotoxicity Assay[4] Cell Line: Chromaffin cells[4] Concentration: 10 and 30 μM Incubation Time: 24 hours Result: Showed a tendency to increase cell death at the concentration of 10 μM, and showed near 100% cell loss at the concentration of 30 μM.
In Vivo Flunarizine (intraperitoneal injection; 30 mg/kg; once) protects mice from lipopolysaccharide- (LPS-) induced acute lung injury (ALI)[5]. Animal Model: Male BALB/c mice (6-8 weeks old) with acute lung injury induced by lipopolysaccharide[5] Dosage: 30 mg/kg Administration: Intraperitoneal injection; 30 mg/kg; once Result: Suppressed the LPS-induced cell influx, protein leakage, and inflammatory cytokines release. Inhibited the pulmonary inflammation.

 Chemical & Physical Properties

Density 1.17 g/cm3
Boiling Point 511.3ºC at 760 mmHg
Molecular Formula C26H26F2N2
Molecular Weight 404.49500
Exact Mass 404.20600
PSA 6.48000
LogP 5.26100
Index of Refraction 1.606
Storage condition 2-8°C

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
TK9188600
CHEMICAL NAME :
Piperazine, 1-(bis(4-fluorophenyl)methyl)-4-(3-phenyl-2-propenyl) -, (E)-
CAS REGISTRY NUMBER :
52468-60-7
LAST UPDATED :
199206
DATA ITEMS CITED :
3
MOLECULAR FORMULA :
C26-H26-F2-N2
MOLECULAR WEIGHT :
404.54

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
4286 ug/kg/30D-I
TOXIC EFFECTS :
Behavioral - tremor
REFERENCE :
NEURAI Neurology. (Modern Medicine Pub., Inc., 1 E. First St., Duluth, MN 55802) V.1- 1951- Volume(issue)/page/year: 37,881,1987
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
18 mg/kg/90D-I
TOXIC EFFECTS :
Behavioral - tremor
REFERENCE :
NEURAI Neurology. (Modern Medicine Pub., Inc., 1 E. First St., Duluth, MN 55802) V.1- 1951- Volume(issue)/page/year: 37,881,1987
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
960 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 37,1103,1987

 Precursor & DownStream

Precursor  2

DownStream  0

 Synonyms

flunarazine
(E)-1-[bis(4-fluorophenyl)methyl]-4-(cinnamyl)piperazine
Sibelium
1-[bis(4-fluorophenyl)methyl]-4-cinnamylpiperazine
1-[Bis(4-fluorophenyl)methyl]-4-[(2E)-3-phenyl-2-propenyl]piperazine
EINECS 257-937-5
(E)-1-[Bis-(p-fluorophenyl)methyl]-4-cinnamylpiperazine
Fluarizine
(e)-piperazin
1-[Bis(4-fluorophenyl)methyl]-4-[(E)-3-phenyl-2-propenyl]piperazine
1-[bis(4-fluorophenyl)methyl]-4-(3-phenyl-2-propenyl)piperazine
(e)-1-[bis(4-fluorophenyl)methyl]-4-(3-phenyl-2-propenyl)piperazine
MFCD00242731
Piperazine,1-[bis(4-fluorophenyl)methyl]-4-(3-phenyl-2-propenyl)-,(E)
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