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Esophageal cancer is the most markedly increasing tumor entity in Western countries. Due to very poor 5‐year‐survival, new therapeutic approaches are mandatory. Peripheral benzodiazepine receptors (PBR) have been implicated in growth control of various tumor models, but they have not been studied yet in esophageal cancer. We used esophageal cancer cell lines and primary cell cultures of human esophageal cancers and evaluated (i) expression and localization of PBR; (ii) PBR‐ligand‐induced inhibition of cell growth; (iii) induction of apoptosis; and (iv) alterations in cell cycle. Expression of PBR was detected both in cell lines and in primary cell cultures of human esophageal cancers. PBR was localized in the mitochondria. The PBR‐specific ligands FGIN‐1‐27 and PK 11195, but not the centrally acting benzodiazepine clonazepam or the indolacetamide FGIN‐1‐52, neither of which displaying any …