• indole
• MPTP
• PET
• translocator protein

“Peripheral-type benzodiazepine receptor” (PBR) was discovered as peripheral binding site for the diazepam, a centrally acting benzodiazepine, and it was renamed “Translocator Protein 18kDa”(TSPO). This protein is located at the contact site between the outer and inner mitochondrial membrane and formed the “mitochondrial permeability transition pore” (MPTP) in associated with other proteins. TSPO has got an important role in numerous biological processes, for example: immunomodulation, regulation of steroidogenesis and apoptosis. It is expressed in peripheral tissues, for example: immune system, steroid producing tissues and in the central nervous system (glial cells, neurons).
The basal expression of TSPO is up-regulated in a variety of neuropathologies (gliomas) and neurodegenerative disorders (Huntington's and Alzheimer's disease), in some tumours and brain injury and inflammation; on the contrary, a decrease in TSPO levels is present in anxiety and mood disorders. For this reasons TSPO has been proposed as a diagnostic marker to image and measure the TSPO expression and distribution levels, and thus for evaluation of disease progression by means of specific radiolabeled ligands with the PET (Positron Emission Computed Tomography).
The aim of this work is to design and synthesized of new indole derivatives as molecular probes for TSPO.