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Description

An isoquinoline carboxamide that acts as a potent ligand for peripheral bezodiazepine receptor (Kd = 20 nM). Exhibits anti-inflammatory properties. Binds to monocytes and following lesioning its binding up-regulated in brain macrophages and activated microglia. Shown to enhance the susceptibility of cells to apoptosis induction by DNA damaging agents and can reverse the suppression of apoptosis by Bcl-2. Serves as a ligand of the outer membrane translocator protein and reduces mitochondrial transmembrane potential within 30 minutes of exposure (˜,100 µ,M).

Structure formula

PK 11195

Contents

Miscellaneous

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