Drug intelligence / Profile preview

diclofensine

Development stage
Discontinued
Lead developer
Roche
Modality
Small Molecules
Administration
Oral
01

Overview

Diclofensine (RO 8-4650) is a potent **triple monoamine reuptake inhibitor** developed by Hoffmann-La Roche in the 1970s as a potential antidepressant. It inhibits the reuptake of **dopamine**, **norepinephrine**, and **serotonin** at their respective transporters, with primary effects on dopamine and norepinephrine. It is chemically a tetrahydroisoquinoline derivative. While found effective in human trials for depression, with relatively few side effects, it was discontinued from clinical development, possibly due to concerns about abuse potential.

Other names
diclofensine4-(3,4-dichlorophenyl)-7-methoxy-2-methyl-1,2,3,4-tetrahydroisoquinoline4-(3,4-dichlorophenyl)-7-methoxy-2-methyl-1,2,3,4-tetrahydroisoquinoline hydrochlorideRo 8-4650 hydrochlorideRo8-4650 hydrochlorideRo-8-4650 hydrochloridediclofensine hydrochloride
02

Targets

SERT (Sodium-dependent serotonin transporter)DAT (Dopamine plasma membrane transport protein)NET (Norepinephrine Transporter)

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