Chemical Properties
A white powder or pearly platelets.
Uses
A hydrazine derivative that is a non-selective and irreversible monoamine oxidase inhibitor (MAOI) and also inhibits GABA-transaminase (GABA-T), markedly increasing brain GABA levels. It is an antidep
ressant and anxiolytic used in the treatment of major depressive disorder (MDD) as well as other neural disorders.
Brand name
Nardil (Parke-Davis).
Originator
Nardil ,Parke Davis, US ,1959
Definition
ChEBI: Phenelzine sulfate is an organic molecular entity.
Manufacturing Process
To a refluxing solution containing 147.5 grams of 85% hydrazine hydrate in 500 cc of ethanol was added, during a period of 5 hours, 92.5 grams of phenethylbromide (0.50 mol) in 150 cc of ethanol. Stirring and refluxing were continued for two hours. The ethanol was removed by distillation and the residue extracted repeatedly with ether. The ether was dried with potassium carbonate and the product base collected by distillation, BP 74°C/0.1 mm, yield 52.3 grams (77%). The base is reacted with sulfuric acid in propanol to give the sulfate.
Therapeutic Function
Psychostimulant
General Description
Phenelzine sulfate, 2-(phenylethyl)hydrazine sulfate(Nardil), is an effective antidepressant agent. A mechanismbasedinactivator, it irreversibly inactivates the enzyme orits cofactor, presumably after oxidation to the diazine,which can then break up into molecular nitrogen, a hydrogen atom, and a phenethyl free radical. The latter would bethe active species in irreversible inhibition.
Biological Activity
Non-selective MAO-A/B inhibitor.
