Bioorganic & Medicinal Chemistry Letters 2002-02-11

A lipophilic thioflavin-T derivative for positron emission tomography (PET) imaging of amyloid in brain.

Chester A Mathis, Brian J Bacskai, Stephen T Kajdasz, Megan E McLellan, Matthew P Frosch, Bradley T Hyman, Daniel P Holt, Yanming Wang, Guo-Feng Huang, Manik L Debnath, William E Klunk

Index: Bioorg. Med. Chem. Lett. 12 , 295-298, (2002)

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Abstract

The synthesis of a new lipophilic thioflavin-T analogue (2-[4' -(methylamino)phenyl]benzothiazole, 6) with high affinity for amyloid is reported. Intravenous injection of [(11)C]-labeled 6 in control mice resulted in high brain uptake. Amyloid deposits were imaged with multiphoton microscopy in the brains of living transgenic mice following the systemic injection of unlabeled 6. [(11)C]6 is a promising amyloid imaging agent for Alzheimer's disease.