High-affinity dopamine D2/D3 PET radioligands 18F-fallypride and 11C-FLB457: a comparison of kinetics in extrastriatal regions using a multiple-injection protocol

J Cereb Blood Flow Metab. 2010 May;30(5):994-1007. doi: 10.1038/jcbfm.2009.270. Epub 2009 Dec 30.

Abstract

(18)F-Fallypride and (11)C-FLB457 are commonly used PET radioligands for imaging extrastriatal dopamine D(2)/D(3) receptors, but differences in their in vivo kinetics may affect the sensitivity for measuring subtle changes in receptor binding. Focusing on regions of low binding, a direct comparison of the kinetics of (18)F-fallypride and (11)C-FLB457 was made using a MI protocol. Injection protocols were designed to estimate K(1), k(2), f(ND)k(on), B(max), and k(off) in the midbrain and cortical regions of the rhesus monkey. (11)C-FLB457 cleared from the arterial plasma faster and yielded a ND space distribution volume (K(1)/k(2)) that is three times higher than (18)F-fallypride, primarily due to a slower k(2) (FAL:FLB; k(2)=0.54 min(-1):0.18 min(-1)). The dissociation rate constant, k(off), was slower for (11)C-FLB457, resulting in a lower K(Dapp) than (18)F-fallypride (FAL:FLB; 0.39 nM:0.13 nM). Specific D(2)/D(3) binding could be detected in the cerebellum for (11)C-FLB457 but not (18)F-fallypride. Both radioligands can be used to image extrastriatal D(2)/D(3) receptors, with (11)C-FLB457 providing greater sensitivity to subtle changes in low-receptor-density cortical regions and (18)F-fallypride being more sensitive to endogenous dopamine displacement in medium-to-high-receptor-density regions. In the presence of specific D(2)/D(3) binding in the cerebellum, reference region analysis methods will give a greater bias in BP(ND) with (11)C-FLB457 than with (18)F-fallypride.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Benzamides / chemical synthesis
  • Benzamides / chemistry
  • Benzamides / metabolism*
  • Brain* / anatomy & histology
  • Brain* / metabolism
  • Carbon Radioisotopes / chemistry
  • Carbon Radioisotopes / metabolism
  • Dopamine Antagonists / chemical synthesis
  • Dopamine Antagonists / chemistry
  • Dopamine Antagonists / metabolism*
  • Fluorine Radioisotopes / metabolism
  • Ligands
  • Macaca mulatta
  • Positron-Emission Tomography / methods*
  • Pyrrolidines / chemical synthesis
  • Pyrrolidines / chemistry
  • Pyrrolidines / metabolism*
  • Receptors, Dopamine D2 / metabolism*
  • Receptors, Dopamine D3 / metabolism*
  • Salicylamides / chemical synthesis
  • Salicylamides / chemistry
  • Salicylamides / metabolism*

Substances

  • Benzamides
  • Carbon Radioisotopes
  • Dopamine Antagonists
  • Fluorine Radioisotopes
  • Ligands
  • N-((1-allyl-2-pyrrolidinyl)methyl)-5-(3-fluoropropyl)-2,3-dimethoxybenzamide
  • Pyrrolidines
  • Receptors, Dopamine D2
  • Receptors, Dopamine D3
  • Salicylamides
  • FLB 457