OtherBASIC SCIENCE INVESTIGATIONS

Brain Adenosine A2A Receptor Occupancy by a Novel A1/A2A Receptor Antagonist, ASP5854, in Rhesus Monkeys: Relationship to Anticataleptic Effect

Takuma Mihara, Akihiro Noda, Hiroshi Arai, Kayoko Mihara, Akinori Iwashita, Yoshihiro Murakami, Takahiro Matsuya, Sosuke Miyoshi, Shintaro Nishimura and Nobuya Matsuoka
Journal of Nuclear Medicine July 2008, 49 (7) 1183-1188; DOI: https://doi.org/10.2967/jnumed.108.051474

Article Figures & Data

Figures

  • FIGURE 1. 
    FIGURE 1. 

    Averaged PET images of 11C-SCH442416 from 3 animals, from 5 to 10 min after tracer administration. Saline or ASP5854 (0.001–0.1 mg/kg) was intravenously administered at 1 h before 11C-SCH442416 administration. Images were anatomically standardized using NEUROSTAT and presented in cross-sectional images at striatum level.

  • FIGURE 2. 
    FIGURE 2. 

    Fitting curve of plasma concentration and occupancy for adenosine A2AR in rhesus monkeys.

  • FIGURE 3. 
    FIGURE 3. 

    Correlation between occupancy for adenosine A2ARs and plasma concentration after administration of ASP5854 at dose of 0.1 mg/kg in rhesus monkeys. (A) Time-dependent changes of occupancy and plasma concentration of 0.1 mg of ASP5854 per kilogram. Values are mean ± SE of 3 animals. (B) Averaged PET images of 11C-SCH442416 from 3 animals, from 5 to 10 min after tracer administration. ASP5854 (0.1 mg/kg) was intravenously administered at 1, 4, or 8 h before 11C-SCH442416 administration. Images were anatomically standardized using NEUROSTAT and presented in cross-sectional images at striatum level.

  • FIGURE 4. 
    FIGURE 4. 

    Effect of ASP5854 on haloperidol-induced catalepsy in rhesus monkeys. Catalepsy was measured 40 min after intramuscular injection of haloperidol. ASP5854 was orally administered 20 min before haloperidol injection. Each column represents duration of cataleptic posture and mean ± SE of 4 animals. ASP5854 suppressed haloperidol-induced catalepsy, and ED50 value was 0.1 mg/kg. *P < 0.05 (statistically significant compared with vehicle-treated group [by Kruskal–Wallis followed by Dunnett multiple comparison test]).

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