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Dopamine D1 receptor imaging in the rodent and primate brain using the isoquinoline (+)-[11C]A-69024 and positron emission tomography

✍ Scribed by Laurent Besret; Frédéric Dollé; Anne-Sophie Hérard; Martine Guillermier; Stéphane Demphel; Françoise Hinnen; Christine Coulon; Michèle Ottaviani; Michel Bottlaender; Philippe Hantraye; Michael Kassiou

Publisher
John Wiley and Sons
Year
2008
Tongue
English
Weight
267 KB
Volume
97
Category
Article
ISSN
0022-3549

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✦ Synopsis

In vivo pharmacokinetic and brain binding characteristics of (+)-[(11)C]A-69024, a high-affinity-D1-selective dopamine receptor antagonist, were assessed with micro-PET and beta-microprobes in the rat and PET in the baboon. The biodistribution of (+)-[(11)C]A-69024 in rats and baboons showed a rapid brain uptake (reaching a maximal value at 5 and 15 min postinjection in rats and baboons, respectively), followed by a slow wash out. The region/cerebellum concentration ratio was characterized by a fourfold higher uptake in striatum and a twofold higher uptake in cortical regions, consistent with in vivo specific binding of the radiotracer in these cerebral regions. Furthermore, this specific (+)-[(11)C]A-69024 binding significantly correlated with the reported in vitro distribution of dopamine D1-receptors. Finally, the specific uptake of the tracer in the striatum and cortical regions was completely prevented by either a pretreatment with large doses of nonradioactive (+/-)A-69024 or of the D1-selective antagonist SCH23390, resulting in a similar uptake in the reference region (cerebellum) and in other brain regions. Thus, (+)-[(11)C]A-69024 appears to be a specific and enantioselective radioligand to visualize and quantify brain dopamine D1 receptors in vivo using positron emission tomography.

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