Brain research bulletin · 2026
Evaluation of cerebral cannabinoid type 2 receptors using [11C]RSR-056 PET in a rat model of epilepsy.
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Zeng Chunyuan, Tang Guixian, Jiang Yuanfang, Dong Chenchen, Wei Huiyi, Hou Lu, Liao Kai, Tan Zhiqiang, Wu Huanhua, Wu Biao, Ye Weijian, Zhu Honghao, Gong Jian, Xu Hao, Ling Xueying
Аннотация
PURPOSE: Cannabinoid receptor type 2 (CB2R) plays a critical yet mechanistically undefined role in epileptogenesis. This study employed a CB2R-targeting PET probe to visualize spatiotemporal alterations in cerebral CB2R expression in epileptic rats, elucidating its potential role in epileptogenesis.
METHODS: The CB2R-targeting PET probe [11C]RSR-056 underwent automated radiosynthesis. A lithium chloride-pilocarpine-induced epileptic rat model was utilized, and [11C]RSR-056 PET/CT imaging was performed in controls and status epilepticus (SE) groups (1 d, 1 w, 1 m and 2 m post SE). Image analysis using PMOD software yielded data expressed as standard uptake value (SUV) and the percentage of injected dose per gram of tissue (%ID/g). Immunofluorescence was performed on brain tissue from all groups.
RESULTS: [11C]RSR-056 PET/CT imaging revealed higher SUV in the hippocampus, thalamus, hypothalamus, and cerebellum of epileptic rats at 1 w post SE, and significantly higher %ID/g in the cortex, hippocampus, striatum, thalamus, hypothalamus, and cerebellum at both 1 d and 1 w post SE, compared with the control group (all P < 0.05). Immunofluorescence confirmed CB2R co-localization in both microglia and neurons. Relative to controls, the 1 w post SE group showed a significant increase in the mean CB2R immunofluorescence intensity within the hippocampal CA1 region (P < 0.05).
CONCLUSION: CB2R-targeted PET probe [11C]RSR-056 enables non-invasive visualization of spatiotemporal changes in brain CB2R expression of living epileptic rats. CB2R expression elevated at 1 d post SE, peaked at 1 w post SE, and declined to baseline at 1 m and 2 m post SE. Elevated CB2R expression was associated not only with microglia but also with neurons.
METHODS: The CB2R-targeting PET probe [11C]RSR-056 underwent automated radiosynthesis. A lithium chloride-pilocarpine-induced epileptic rat model was utilized, and [11C]RSR-056 PET/CT imaging was performed in controls and status epilepticus (SE) groups (1 d, 1 w, 1 m and 2 m post SE). Image analysis using PMOD software yielded data expressed as standard uptake value (SUV) and the percentage of injected dose per gram of tissue (%ID/g). Immunofluorescence was performed on brain tissue from all groups.
RESULTS: [11C]RSR-056 PET/CT imaging revealed higher SUV in the hippocampus, thalamus, hypothalamus, and cerebellum of epileptic rats at 1 w post SE, and significantly higher %ID/g in the cortex, hippocampus, striatum, thalamus, hypothalamus, and cerebellum at both 1 d and 1 w post SE, compared with the control group (all P < 0.05). Immunofluorescence confirmed CB2R co-localization in both microglia and neurons. Relative to controls, the 1 w post SE group showed a significant increase in the mean CB2R immunofluorescence intensity within the hippocampal CA1 region (P < 0.05).
CONCLUSION: CB2R-targeted PET probe [11C]RSR-056 enables non-invasive visualization of spatiotemporal changes in brain CB2R expression of living epileptic rats. CB2R expression elevated at 1 d post SE, peaked at 1 w post SE, and declined to baseline at 1 m and 2 m post SE. Elevated CB2R expression was associated not only with microglia but also with neurons.