Journal of Medicinal Chemistry · 2005 · 67 citations · 13 references
MedicineMedicinal ChemistryPharmacologyDrug DiscoveryMolecular PharmacologyNeuropharmacologyDrug-receptor InteractionsLigand BindingPhotodynamic TherapyReceptor ImagingReceptor PharmacologyReceptor-ligand InteractionsBenzodiazepine Receptor AgonistsDisplacementDrug PhotosensitizationFluorescent Chemical ProbesFluorescent ProbesPhotoaffinity ProbesPhotosensitizersPhotosensitizing Compounds
Pyropheophorbides and their metal complexes were synthesized to investigate their applications as nonradioactive peripheral benzodiazepine receptor (PBR) binding probes and photosensitizers for use in photodynamic therapy. They were found to be localized in mitochondria and showed significant binding to PBR. In some cases, the PBR binding values were similar to that for 17 (PK11195, 1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)isoquinoline-3-carboxamide). However, no direct correlation between 17 displacement ability and photosensitizing efficacy of photosensitizers was observed.
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