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

Bioorg Med Chem Lett. 2002 Feb 11;12(3):295-8. doi: 10.1016/s0960-894x(01)00734-x.

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.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Alzheimer Disease / diagnostic imaging
  • Amyloid / metabolism*
  • Animals
  • Benzothiazoles
  • Binding, Competitive / drug effects
  • Brain / diagnostic imaging*
  • Chemical Phenomena
  • Chemistry, Physical
  • Mice
  • Mice, Transgenic
  • Microscopy
  • Plaque, Amyloid / diagnostic imaging*
  • Radiopharmaceuticals / chemical synthesis
  • Radiopharmaceuticals / chemistry*
  • Structure-Activity Relationship
  • Thiazoles / chemical synthesis
  • Thiazoles / chemistry*
  • Tomography, Emission-Computed

Substances

  • Amyloid
  • Benzothiazoles
  • Radiopharmaceuticals
  • Thiazoles
  • thioflavin T