Drug intelligence / Profile preview

SKF-83566

Development stage
Preclinical
Lead developer
GSK
Modality
Small Molecules
Administration
Intraperitoneal, Intracerebroventricular
01

Overview

SKF-83566 is a selective small molecule antagonist of the dopamine D1-like receptors (D1 and D5). As a benzazepine derivative, it is widely utilized as a pharmacological research tool to investigate dopaminergic signaling and its role in neurological conditions such as Parkinson's disease and substance use disorders. In addition to its high affinity for dopamine D1 receptors, SKF-83566 also acts as an antagonist at serotonin 5-HT2 receptors. Recent preclinical research has explored the benzazepine skeleton of SKF-83566 as a scaffold for the development of novel antitumor agents. Specifically, derivatives created by linking SKF-83566 to pomalidomide have shown antiproliferative activity against breast and cervical cancer cell lines, suggesting potential applications in oncology beyond its traditional use in neuroscience.

Other names
8-bromo-2,3,4,5-tetrahydro-3-methyl-5-phenyl-1H-3-benzazepin-7-olSKF 83566SKF83566SKF-83566
02

Targets

DRD1 (Dopamine D1 Receptor)DRD5 (Dopamine D5 Receptor)DAT (Dopamine plasma membrane transport protein)

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