Drug intelligence / Profile preview

SKF-104557

Development stage
Discontinued
Lead developer
GSK
Modality
Small Molecules
Administration
Not Applicable (metabolite, Not Administered Directly)
01

Overview

SKF-104557 is a **major human metabolite of ropinirole**, a non-ergoline dopamine agonist used primarily in the treatment of Parkinson's disease and restless legs syndrome[1][2][3][7]. Chemically, SKF-104557 is known as **N-despropyl ropinirole** or 4-(2-(propylamino)ethyl)indolin-2-one. It retains dopamine receptor binding properties similar to its parent compound but is significantly less potency (approximately 150-fold reduction relative to ropinirole)[1][3]. SKF-104557 functions as a **full agonist at human dopamine D2 and D3 receptors**, and as a **partial agonist at the dopamine D4 receptor**, with selectivity in radioligand binding and functional assays for the D3 subtype[1][3].

Other names
4-(2-(Propylamino)ethyl)indolin-2-one1,3-Dihydro-4-[2-(propylamino)ethyl]-2H-indol-2-one
02

Targets

DRD2 (Dopamine D2 Receptor)DRD4 (Dopamine D4 Receptor)DRD3 (Dopamine receptor D3)

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