التفاصيل البيبلوغرافية
| العنوان: |
Whole-body biodistribution of the cannabinoid type 1 receptor ligand [18F]MK-9470 in the rat. |
| المؤلفون: |
Buchholz, H.G.1, Uebbing, K.2, Maus, S.1, Pektor, S.1, Afahaene, N.1, Weyer-Elberich, V.3, Lutz, B.4, Schreckenberger, M.1, Miederer, I.1 isabelle.miederer@unimedizin-mainz.de |
| المصدر: |
Nuclear Medicine & Biology. Sep2017, Vol. 52, p63-69. 7p. |
| مصطلحات موضوعية: |
*CANNABINOID receptors, *TOTAL body irradiation, *ENERGY metabolism, *FOOD consumption, *POSITRON emission tomography, *LABORATORY rats |
| مستخلص: |
The endocannabinoid system participates in many processes in the body, including memory, reward, pain, motor activity, food intake, energy metabolism, and gastrointestinal functions. [ 18 F]MK-9470 is a positron emission tomography (PET) ligand that binds with high affinity and selectivity to the cannabinoid type 1 receptor. In order to fully characterize ligand behavior, tracer uptake measured using in vivo microPET was compared with results from ex vivo tissue dissection. Twelve male Sprague–Dawley rats were divided into three subgroups and scanned over time periods of 10 min, 30 min and 90 min using PET. Afterwards, a number of the animals' organs were dissected. Uptake of radioactivity was expressed in terms of %ID/ml and %ID/(g tissue). For comparison of in vivo and ex vivo methods, Bland–Altman plots were computed. The highest uptake of [ 18 F]MK-9470 was found in the liver and small intestine; the brain showed less uptake, while low and unspecific binding was observed in tissue of the heart, lung, kidney and bone. In the brain, normalized uptake of [ 18 F]MK-9470 was on average 0.25%ID/ml (range: 0.16 to 0.28%ID/ml). Bland–Altman plots revealed the best agreement between methods for the 90 min acquisition protocols. High hepatic accumulation and metabolism of [ 18 F]MK-9470 occur with mainly enteral excretion, which may vary considerably over time — a finding which may be of relevance in metabolite determination in quantitative brain studies. Comparisons between in vivo and ex vivo methods showed that whole-body distribution of [ 18 F]MK-9470 using positron emission tomography is a preferable alternative to ex vivo biodistribution, and requires a significantly smaller number of animals. [ABSTRACT FROM AUTHOR] |
| قاعدة البيانات: |
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