Chemical Properties
White Solid
Originator
Sibelium,Janssen,W. Germany,1977
Uses
antipsychotic, H1 antihistamine
Uses
Calcium channel blocker; fluorinated derivative of Cinnarizine. Vasodilator (cerebral and peripheral). This is the labeled analog.
Definition
ChEBI: Flunarizine hydrochloride is a diarylmethane.
Manufacturing Process
A mixture of 14.3 parts of di-(p-fluorophenyl)-chloromethane, 10.1 parts of 1-
cinnamylpiperazine, 12.7 parts of sodium carbonate, a few crystals of
potassium iodide in 200 parts of 4-methyl-2-pentanone is stirred and refluxed
for 21 hours. The reaction mixture is cooled and 50 parts of water are added.
The organic layer is separated, dried, filtered and evaporated.
The oily residue is dissolved in 480 parts of anhydrous diisopropyl ether. This
solution is boiled with activated charcoal, filtered and to the clear filtrate is
added an excess of 2-propanol, previously saturated with gaseous hydrogen
chloride. The precipitated salt is filtered off and recrystallized from a mixture
of 2-propanol and ethanol, yielding 1-cinnamyl-4-(di-p-fluorobenzhydryl)
piperazine dihydrochloride, MP 251.5°C.
Therapeutic Function
Vasodilator
General Description
Flunarizine has antihistamine, anticonvulsant and vestibular depressive properties. It protects endothelial cells from calcium overload-induced damage. Flunarizine is used to treat epilepsy, migraine prophylaxis, cerebral blood flow disturbances, peripheral vascular disease and vertigo.
Biological Activity
Dual Na + /Ca 2+ channel blocker; a cerebral and peripheral vasodilator. Neuroprotective.
Biochem/physiol Actions
Blocks T-type Ca2+/Na+ channels; inhibits K+-induced catecholamine release from chromaffin cells
