Synthesis and in vivo evaluation of (O-methyl-11C) N-(3,5-dichloro-2-(methoxy)phenyl)-4-(methoxy)-3-(1-piperazinyl)benzenesulfonamid e as an imaging probe for 5-HT6 receptors.

Liu F; Majo VJ; Prabhakaran JMilak MSJohn Mann JParsey RVKumar JS

首页> 外文期刊>Bioorganic and medicinal chemistry >Synthesis and in vivo evaluation of (O-methyl-11C) N-(3,5-dichloro-2-(methoxy)phenyl)-4-(methoxy)-3-(1-piperazinyl)benzenesulfonamid e as an imaging probe for 5-HT6 receptors.

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Synthesis and in vivo evaluation of (O-methyl-11C) N-(3,5-dichloro-2-(methoxy)phenyl)-4-(methoxy)-3-(1-piperazinyl)benzenesulfonamid e as an imaging probe for 5-HT6 receptors.

机译：Synthesis and in vivo evaluation of (O-methyl-11C) N-(3,5-dichloro-2-(methoxy)phenyl)-4-(methoxy)-3-(1-piperazinyl)benzenesulfonamid e as an imaging probe for 5-HT6 receptors.

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The serotonin receptor 6 (5-HT(6)) 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)benzenesulfonamid e (SB399885), a selective and high affinity (pK(i)=9.11) 5-HT(6) antagonist, has been radiolabeled with carbon-11 by O-methylation of the corresponding desmethyl analogue with [(11)C]MeOTf in order to determine the suitability of [(11)C]SB399885 to quantify 5-HT(6)R 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 [(11)C]SB399885 was 30+/-5% (EOS) and the total synthesis time was 30min at EOB. PET studies with [(11)C]SB399885 in baboon showed fast uptake followed by rapid clearance in the brain. Highest uptake of radioactivity of [(11)C]SB399885 in baboon brain were found in temporal cortex, parahippocampal gyrus, pareital cortex, amygdala, and hippocampus. Poor brain entry and inconsistent brain uptake of [(11)C]SB399885 compared to known 5-HT(6)R distribution limits its usefulness for the in vivo quantification of 5-HT(6)R with PET.

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《Bioorganic and medicinal chemistry》 |2011年第17期|5255-5259|共5页
作者
Liu F; Majo VJ; Prabhakaran JMilak MSJohn Mann JParsey RVKumar JS;
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Division of Substance Abuse, Department of Psychiatry, Columbia University Medical Center, New York, NY, USA.;

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Synthesis and in vivo evaluation of (O-methyl-11C) N-(3,5-dichloro-2-(methoxy)phenyl)-4-(methoxy)-3-(1-piperazinyl)benzenesulfonamid e as an imaging probe for 5-HT6 receptors.

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