Research ArticleCLINICAL INVESTIGATIONS

Cerebral Histamine H1 Receptor Binding Potential Measured with PET Under a Test Dose of Olopatadine, an Antihistamine, Is Reduced After Repeated Administration of Olopatadine

Michio Senda, Nobuo Kubo, Kazuhiko Adachi, Yasuhiko Ikari, Keiichi Matsumoto, Keiji Shimizu and Hideyuki Tominaga
Journal of Nuclear Medicine June 2009, 50 (6) 887-892; DOI: https://doi.org/10.2967/jnumed.108.058537

Article Figures & Data

Figures

  • FIGURE 1. 
    FIGURE 1. 

    (A) Entire study schedule. (B) PET measurement protocol. Trans = transmission scan.

  • FIGURE 2. 
    FIGURE 2. 

    PET images of standardized uptake value (tissue activity divided by injected activity per body weight) acquired at 70–90 min after injection of 11C-doxepin on representative subject at baseline (placebo), following an initial single dose (acute scan), and following a dose after repeated administration (chronic scan).

  • FIGURE 3. 
    FIGURE 3. 

    BPND of 11C-doxepin in DLPFC of each subject at baseline (placebo), following an initial single 5-mg dose of olopatadine (acute scan), and following another single 5-mg dose after repeated administration of olopatadine for 4 wk (chronic scan).

Tables

  • TABLE 1

    Saccadic Latency Before and After Administration of Placebo or 5 mg of Olopatadine

    After administration
    VisitBefore administration30 min60 min180 minIncrease*
    Baseline (placebo)0.24 ± 0.160.27 ± 0.140.29 ± 0.120.33 ± 0.1238% ± 12%
    Acute scan (0 wk)0.21 ± 0.080.23 ± 0.100.22 ± 0.180.30 ± 0.1742% ± 17%
    Interim (2 wk)0.23 ± 0.100.25 ± 0.200.24 ± 0.12
    Chronic scan (4 wk)0.23 ± 0.110.25 ± 0.180.26 ± 0.140.30 ± 0.1630% ± 14%

    • ↵* Average percentage increase in maximum latency for each subject after drug administration.

    • Data are mean ± SD, in seconds (n = 14). No statistically significant difference was found between pre- and postadministration data at any visit.

  • TABLE 2

    Histamine H1 Receptor BPND of 11C-Doxepine for the Various Regions Measured with PET at Baseline and After Administration of 5 mg of Olopatadine in Acute and Chronic Scans

    BPND
    RegionBaselineAcute (0 wk)Chronic (4 wk)Acute scan receptor occupancy
    DLPFC0.28 ± 0.060.24 ± 0.070.13 ± 0.08*15% ± 15%
    Frontobasal0.33 ± 0.080.27 ± 0.07†0.15 ± 0.08*18% ± 15%
    Parietal0.25 ± 0.050.20 ± 0.080.09 ± 0.08*24% ± 24%
    Temporal0.37 ± 0.070.33 ± 0.080.21 ± 0.09*11% ± 12%
    Occipital0.19 ± 0.040.16 ± 0.060.09 ± 0.05*19% ± 22%
    Anterior cingulate0.29 ± 0.070.26 ± 0.070.13 ± 0.09*14% ± 14%
    Thalamus0.26 ± 0.070.18 ± 0.06†0.20 ± 0.0626% ± 20%

    • ↵† P < 0.05/7 in comparison between baseline and acute scan by 2-way ANOVA.

    • ↵* P < 0.01/7 in comparison between acute scan and chronic scan by 2-way ANOVA.

    • Data are mean ± SD (n = 14). Receptor occupancy was computed as percentage decrease in BPND at time of acute scan, compared with baseline.

Back to top

In this issue

Print
Download PDF
Article Alerts
Email Article
Citation Tools
Bookmark this article

Jump to section