Synthesis and PET Imaging Biodistribution Studies of Radiolabeled Iododiflunisal, a Transthyretin Tetramer Stabilizer, Candidate Drug for Alzheimer’s Disease

• Published in: Molecules (Basel, Switzerland) Vol. 29; no. 2; p. 488
• Main Authors: Joshi, Sameer M., Wilson, Thomas C., Li, Zibo, Preshlock, Sean, Gómez-Vallejo, Vanessa, Gouverneur, Véronique, Llop, Jordi, Arsequell, Gemma
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 01.01.2024; MDPI
• Subjects: 18F; Advertising executives; Alzheimer Disease - diagnostic imaging; Alzheimer Disease - drug therapy; Alzheimer's disease; amyloid beta; Amyloid beta-Peptides; Animals; Biodistribution; Cerebrospinal fluid; Diflunisal; Diflunisal - analogs & derivatives; Drug therapy; Excipients; Humans; in vivo imaging; Iodine; iododiflunisal; Liver; Mice; Neurophysiology; PET imaging; Pharmaceutical Preparations; Potash; Potassium; Prealbumin; Proteins; small-molecule chaperone; Tissue Distribution; Tolcapone; Tomography; transthyretin tetramer stabilizer; in vivo imaging; transthyretin tetramer stabilizer; positron emission tomography (PET); iododiflunisal; amyloid beta; small-molecule chaperone; 18F

The small-molecule iododiflunisal (IDIF) is a transthyretin (TTR) tetramer stabilizer and acts as a chaperone of the TTR-Amyloid beta interaction. Oral administration of IDIF improves Alzheimer’s Disease (AD)-like pathology in mice, although the mechanism of action and pharmacokinetics remain unknow...