Comparison of three high affinity SPECT radiotracers for the dopamine D2 receptor

Mohammed S. Al-Tikriti, Ronald M. Baldwin, Yolanda Zea-Ponce, Elzbieta Sybirska, Sami S. Zoghbi, Marc Laruelle, Robert T. Malison, Hank F. Kung, Robert M. Kessler, Dennis S. Charney, Paul B. Hoffer, Robert B. Innis

Research output: Contribution to journalArticlepeer-review

27 Scopus citations

Abstract

The regional brain distribution and pharmacological specificity of three high affinity tracers for the dopamine (DA) D2 receptor: [123I]IBF, [123I]epidepride, and [123I]2′-ISP were assessed by SPECT imaging of non-human primates. The ratios of striatal-to-occipital activities at the time of peak striatal uptake were 2.2, 6.3 and 1.7, respectively. From the peak striatal activities, washout rates were 33, 4 and 16%/h for [123I]IBF, [123I]epidepride and [123I]2′-ISP, respectively. The reversibility of the striatal uptake of all three agents was demonstrated by the rapid displacement induced by the dopamine D2 selective antipsychotic agent raclopride, which increased washout rates to 96, 58 and 43%/h. The administration of d-amphetamine, which induces release of dopamine, had no noticeable effect on [123I]epidepride but increased the washout rate of [123I]IBF. These results suggest that, among these three agents, [123I]epidepride is the superior tracer for in vivo displacement studies because of its slow washout and high target-to-background ratios. However, for tracer kinetic modeling, [123I]IBF may be the superior agent because of its early time of peak uptake and its higher target-to-background ratios than [123I]2′-ISP.

Original languageEnglish
Pages (from-to)179-188
Number of pages10
JournalNuclear Medicine and Biology
Volume21
Issue number2
DOIs
StatePublished - Feb 1994
Externally publishedYes

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