کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10584005 | 981314 | 2014 | 7 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Radiosyntheses and in vivo evaluation of carbon-11 PET tracers for PDE10A in the brain of rodent and nonhuman primate
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
The radiosyntheses and in vivo evaluation of four carbon-11 labeled quinoline group-containing radioligands are reported here. Radiolabeling of [11C]1-4 was achieved by alkylation of their corresponding desmethyl precursors with [11C]CH3I. Preliminary biodistribution evaluation in Sprague-Dawley rats demonstrated that [11C]1 and [11C]2 had high striatal accumulation (at peak time) for [11C]1 and [11C]2 were 6.0-fold and 4.5-fold at 60Â min, respectively. Following MP-10 pretreatment, striatal uptake in rats of [11C]1 and [11C]2 was reduced, suggesting that the tracers bind specifically to PDE10A. MicroPET studies of [11C]1 and [11C]2 in nonhuman primates (NHP) also showed good tracer retention in the striatum with rapid clearance from non-target brain regions. Striatal uptake (SUV) of [11C]1 reached 1.8 at 30Â min with a 3.5-fold striatum:cerebellum ratio. In addition, HPLC analysis of solvent extracts from NHP plasma samples suggested that [11C]1 had a very favorable metabolic stability. Our preclinical investigations suggest that [11C]1 is a promising candidate for quantification of PDE10A in vivo using PET.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 22, Issue 9, 1 May 2014, Pages 2648-2654
Journal: Bioorganic & Medicinal Chemistry - Volume 22, Issue 9, 1 May 2014, Pages 2648-2654
نویسندگان
Jinda Fan, Xiang Zhang, Junfeng Li, Hongjun Jin, Prashanth K. Padakanti, Lynne A. Jones, Hubert P. Flores, Yi Su, Joel S. Perlmutter, Zhude Tu,