NOMIFENSINE MALEATE SALT

Chemical Properties

Pale Yellow Solid

Originator

Alival,Hoechst,W. Germany ,1976

Uses

A novel antidepressant distinguished from existing tricyclic and tetracyclic antidepressants by its bicyclic structure.

Uses

Antidepressant;Dopamine uptake inhibitor

Uses

Nomifensine maleate salt has been used to study the β-CFT (cocaine analogue) binding using human embryonic kidney 293T cells.

Manufacturing Process

A solution of N-(2-aminobenzyl)-1-phenyl-2-methylaminoethanol-1 was prepared by the reaction of α-bromo-acetophenone and (2nitrobenzyl)methylamine, followed by hydrogenation of the nitro group by means of nickel on diatomaceous earth at room temperature and reduction of the CO group by means of sodium borohydride. The intermediate thus produced was dissolved in 100 ml of methylene chloride and introduced dropwise into 125 ml of sulfuric acid at 10° to 15°C. After a short standing, the reaction mixture was poured onto ice and rendered alkaline by means of a sodium hydroxide solution. By extraction with ether, there was obtained 1,2,3,4-tetrahydro-2-methyl-4-phenyl-8-amino-isoquinoline. The base is reacted with maleic acid to give the maleate; melting point of the maleate 199° to 201°C (from ethanol).

brand name

Merital (Hoechst-Roussel).

Therapeutic Function

Psychostimulant

Biochem/physiol Actions

Nomifensine maleate is a selective dopamine uptake inhibitor interacting with the dopamine transporter, at a site different from that of cocaine; antidepressant. Nomifensine serves as an antidepressant and is known to cause frequent hemolytic anemia. The aniline group in this compound results in blood and liver toxicities.

Safety Profile

Poison by ingestion,subcutaneous, intravenous, and intraperitoneal routes.Human systemic effects by intravenous route: heart ratechanges, blood pressure elevation. Experimentalreproductive effects. An antidepressant. When heated to decomposition it em

storage

Store at +4°C