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Purpose <p>Fallypride is a widely used high affinity radioligand for quantification of D2-dopamine receptor binding in small animal PET imaging. To examine the effect of mass both [<sup>18</sup>F]fallypride and [<sup>11</sup>C]fallypride was injected in mice over a wide range of molar activity and the binding potential (BP) was compared.</p> <p>Procedures.</p> <p>Eight mice (C57BL/6&#xa0;J) went through three PET measurements within two weeks. [<sup>11</sup>C]fallypride with the highest possible molar activity (MA) and [<sup>18</sup>F]fallypride with normal and lower molar activity (lowerMA).</p> Results <p>The binding of [<sup>11</sup>C]fallypride was highest with a BP<sub>ND</sub> of 13.5 ± 1.1 BP<sub>ND</sub>. The binding of [<sup>18</sup>F]fallypride was lower, 8.6 ± 2.2 BP<sub>ND</sub> in the normal condition and 5.3 ± 1.3 BP<sub>ND</sub> at the lowerMA condition. By consequence, BP<sub>ND</sub> showed a strong negative correlation with injected mass (R2 = 0.95, <i>P</i> &lt; 0.05). Binding data were entered in a Scatchard analysis yielding a B<sub>max</sub> of 62&#xa0;pmol/g and a K<sub>D</sub> of 0.25&#xa0;nM.</p> Conclusion <p>In this PET study in mice the average radioligand occupancy was estimated to 19% even for <sup>11</sup>C-labeled fallypride despite the high MA of 153.3&#xa0;GBq/µmol and low injected mass of 0.03 µg. Therefore, high affinity radioligands should be applied with care in small animal PET studies and radiochemistry has to be at its best to assure that tracer conditions are met in small animal imaging PET imaging.</p>

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The Binding of the High Affinity Radioligand Fallypride to the D2-dopamine Receptor is Sensitive to Injected Mass – a PET Study in Rodents

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2026年3月16日

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  • Miklós Tóth,
  • Lenke Tari,
  • Sangram Nag,
  • Tian Qiu,
  • Zhisheng Jia,
  • Jenny Häggkvist,
  • Jogeshwar Mukherjee,
  • Andrea Varrone,
  • Christer Halldin,
  • Lars Farde

摘要

Purpose

Fallypride is a widely used high affinity radioligand for quantification of D2-dopamine receptor binding in small animal PET imaging. To examine the effect of mass both [18F]fallypride and [11C]fallypride was injected in mice over a wide range of molar activity and the binding potential (BP) was compared.

Procedures.

Eight mice (C57BL/6 J) went through three PET measurements within two weeks. [11C]fallypride with the highest possible molar activity (MA) and [18F]fallypride with normal and lower molar activity (lowerMA).

Results

The binding of [11C]fallypride was highest with a BPND of 13.5 ± 1.1 BPND. The binding of [18F]fallypride was lower, 8.6 ± 2.2 BPND in the normal condition and 5.3 ± 1.3 BPND at the lowerMA condition. By consequence, BPND showed a strong negative correlation with injected mass (R2 = 0.95, P < 0.05). Binding data were entered in a Scatchard analysis yielding a Bmax of 62 pmol/g and a KD of 0.25 nM.

Conclusion

In this PET study in mice the average radioligand occupancy was estimated to 19% even for 11C-labeled fallypride despite the high MA of 153.3 GBq/µmol and low injected mass of 0.03 µg. Therefore, high affinity radioligands should be applied with care in small animal PET studies and radiochemistry has to be at its best to assure that tracer conditions are met in small animal imaging PET imaging.