Details

Autor(en) / Beteiligte

• Crunelle, Cleo L
• de Wit, Tim C
• de Bruin, Kora
• Ramakers, Ruud M
• van der Have, Frans
• Beekman, Freek J
• van den Brink, Wim
• Booij, Jan

Titel

Varenicline increases in vivo striatal dopamine D2/3 receptor binding: an ultra-high-resolution pinhole [123 I]IBZM SPECT study in rats

Ist Teil von

• Nuclear medicine and biology, 2012-07, Vol.39 (5), p.640-644

Ort / Verlag

New York, NY: Elsevier Inc

Erscheinungsjahr

2012

Link zum Volltext

Quelle

Elsevier ScienceDirect Journals Complete

Beschreibungen/Notizen

• Abstract Introduction Ex vivo storage phosphor imaging rat studies reported increased brain dopamine D2/3 receptor (DRD2/3 ) availability following treatment with varenicline, a nicotinergic drug. However, ex vivo studies can only be performed using cross-sectional designs. Small-animal imaging offers the opportunity to perform serial assessments. We evaluated whether high-resolution pinhole single photon emission computed tomography (SPECT) imaging in rats was able to reproduce previous ex vivo findings. Methods Rats were imaged for baseline striatal DRD2/3 availability using ultra-high-resolution pinhole SPECT (U-SPECT-II) and [123 I]IBZM as a radiotracer, and randomized to varenicline ( n =7; 2 mg/kg) or saline ( n =7). Following 2 weeks of treatment, a second scan was acquired. Results Significantly increased striatal DRD2/3 availability was found following varenicline treatment compared to saline (time⁎treatment effect): posttreatment difference in binding potential between groups corrected for initial baseline differences was 2.039 ( P =.022), indicating a large effect size ( d =1.48). Conclusions Ultra-high-resolution pinhole SPECT can be used to assess varenicline-induced changes in DRD2/3 availability in small laboratory animals over time. Future small-animal studies should include imaging techniques to enable repeated within-subjects measurements and reduce the amount of animals.