کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10588126 | 981445 | 2011 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and in vivo evaluation of [O-methyl-11C] N-[3,5-dichloro-2-(methoxy)phenyl]-4-(methoxy)-3-(1-piperazinyl)benzenesulfonamide as an imaging probe for 5-HT6 receptors
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Synthesis and in vivo evaluation of [O-methyl-11C] N-[3,5-dichloro-2-(methoxy)phenyl]-4-(methoxy)-3-(1-piperazinyl)benzenesulfonamide as an imaging probe for 5-HT6 receptors Synthesis and in vivo evaluation of [O-methyl-11C] N-[3,5-dichloro-2-(methoxy)phenyl]-4-(methoxy)-3-(1-piperazinyl)benzenesulfonamide as an imaging probe for 5-HT6 receptors](/preview/png/10588126.png)
چکیده انگلیسی
The serotonin receptor 6 (5-HT6) is implicated in the pathophysiology of cognitive diseases, schizophrenia, anxiety and obesity and in vivo studies of this receptor would be of value for studying the pathophysiology of these disorders. Therefore, N-[3,5-dichloro-2-(methoxy)phenyl]-4-(methoxy)-3-(1-piperazinyl)benzenesulfonamide (SB399885), a selective and high affinity (pKi = 9.11) 5-HT6 antagonist, has been radiolabeled with carbon-11 by O-methylation of the corresponding desmethyl analogue with [11C]MeOTf in order to determine the suitability of [11C]SB399885 to quantify 5-HT6R in living brain using PET. Desmethyl-SB399885 was prepared, starting from 1-(2-methoxyphenyl) piperazine hydrochloride, in excellent yield. The yield obtained for radiolabeling of [11C]SB399885 was 30 ± 5% (EOS) and the total synthesis time was 30 min at EOB. PET studies with [11C]SB399885 in baboon showed fast uptake followed by rapid clearance in the brain. Highest uptake of radioactivity of [11C]SB399885 in baboon brain were found in temporal cortex, parahippocampal gyrus, pareital cortex, amygdala, and hippocampus. Poor brain entry and inconsistent brain uptake of [11C]SB399885 compared to known 5-HT6R distribution limits its usefulness for the in vivo quantification of 5-HT6R with PET.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 19, Issue 17, 1 September 2011, Pages 5255-5259
Journal: Bioorganic & Medicinal Chemistry - Volume 19, Issue 17, 1 September 2011, Pages 5255-5259
نویسندگان
Fei Liu, Vattoly J. Majo, Jaya Prabhakaran, Matthew S. Milak, J. John Mann, Ramin V. Parsey, J.S. Dileep Kumar,