Evaluation of the PBR/TSPO radioligand [(18)F]DPA-714 in a rat model of focal cerebral ischemia

J Cereb Blood Flow Metab. 2010 Jan;30(1):230-41. doi: 10.1038/jcbfm.2009.205. Epub 2009 Sep 30.

Abstract

Focal cerebral ischemia leads to an inflammatory reaction involving an overexpression of the peripheral benzodiazepine receptor (PBR)/18-kDa translocator protein (TSPO) in the cerebral monocytic lineage (microglia and monocyte) and in astrocytes. Imaging of PBR/TSPO by positron emission tomography (PET) using radiolabeled ligands can document inflammatory processes induced by cerebral ischemia. We performed in vivo PET imaging with [(18)F]DPA-714 to determine the time course of PBR/TSPO expression over several days after induction of cerebral ischemia in rats. In vivo PET imaging showed significant increase in DPA (N,N-diethyl-2-(2-(4-(2-fluoroethoxy)phenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)acetamide) uptake on the injured side compared with that in the contralateral area on days 7, 11, 15, and 21 after ischemia; the maximal binding value was reached 11 days after ischemia. In vitro autoradiography confirmed these in vivo results. In vivo and in vitro [(18)F]DPA-714 binding was displaced from the lesion by PK11195 and DPA-714. Immunohistochemistry showed increased PBR/TSPO expression, peaking at day 11 in cells expressing microglia/macrophage antigens in the ischemic area. At later times, a centripetal migration of astrocytes toward the lesion was observed, promoting the formation of an astrocytic scar. These results show that [(18)F]DPA-714 provides accurate quantitative information of the time course of PBR/TSPO expression in experimental stroke.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Astrocytes / metabolism
  • Autoradiography
  • Brain Ischemia / diagnostic imaging*
  • Brain Ischemia / metabolism
  • Carrier Proteins / metabolism*
  • Cell Count
  • Data Interpretation, Statistical
  • Fluorine Radioisotopes
  • Image Processing, Computer-Assisted
  • Immunohistochemistry
  • Inflammation / diagnostic imaging
  • Inflammation / metabolism
  • Male
  • Microglia / metabolism
  • Models, Statistical
  • Positron-Emission Tomography
  • Pyrazoles*
  • Pyrimidines*
  • Radiopharmaceuticals*
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, GABA-A / metabolism*
  • Stroke / diagnostic imaging
  • Stroke / metabolism

Substances

  • Carrier Proteins
  • Fluorine Radioisotopes
  • N,N-diethyl-2-(2-(4-(2-fluoroethoxy)phenyl)-5,7-dimethylpyrazolo(1,5-a)pyrimidin-3-yl)acetamide
  • Pyrazoles
  • Pyrimidines
  • Radiopharmaceuticals
  • Receptors, GABA-A
  • Tspo protein, rat