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Translational possibility of [18F]Mefway to image serotonin 1A receptors in humans: Comparison with [18F]FCWAY in rodents

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dc.contributor.author김철훈-
dc.contributor.author유영훈-
dc.date.accessioned2015-12-28T11:11:12Z-
dc.date.available2015-12-28T11:11:12Z-
dc.date.issued2014-
dc.identifier.issn0887-4476-
dc.identifier.urihttps://ir.ymlib.yonsei.ac.kr/handle/22282913/138883-
dc.description.abstractPurpose: To compare the cerebral uptake and binding potential of [18 F]FCWAY and [18 F]Mefway in the rodent to assess their potential for imaging serotonin 1A (5-HT1A ) receptors. Materials and Methods: In vitro liver microsomal studies were performed to evaluate the degree of defluorination. Dynamic positron emission tomography (PET) studies were then conducted for 2 h with or without an anti-defluorination agent. The regions of interest were the hippocampus and frontal cortex (5-HT1A target regions) and the cerebellum (5-HT1A nontarget region). The in vivo kinetics of the radioligands were compared based on the brain uptake values and target-to-nontarget ratio. We also performed a comparison of binding potential (BPND ) as a steady-state binding parameter. Finally, binding affinities to 5-HT1A receptors were assessed in Chinese hamster ovary cells (CHO-K1) cells expressing human recombinant 5-HT1A receptors. Results: The radiochemical yield of [18 F]Mefway was slightly higher than that of [18 F]FCWAY (19 vs. 15%). With regard to metabolic stability against defluorination, both compounds exhibited similar stability in rat liver microsomes, but [18 F]Mefway displayed higher stability in the human microsome (defluorination ratio at 30 min: 32 vs. 29 in rat liver microsomes, 31 vs. 64 in human liver microsomes for [18 F]Mefway and [18 F]FCWAY, respectively). There were no significant differences in brain uptake, the target-to-nontarget ratios, and the BPND (at hippocampus, peak brain uptakes: 6.9 vs. 8.5, target-to-nontarget ratios: 6.9 vs. 8.5, BPND : 5.2 vs. 6.2 for [18 F]Mefway and [18 F]FCWAY). The binding affinity of [18 F]Mefway was considerably higher than that of [18 F]FCWAY (IC50 : 1.5 nM vs. 2.2 nM). Conclusion: [18 F]Mefway exhibits favorable characteristics compared to [18 F]FCWAY in rodents, and may be a promising radioligand for use in human subjects.-
dc.description.statementOfResponsibilityopen-
dc.format.extent595~603-
dc.relation.isPartOfSYNAPSE-
dc.rightsCC BY-NC-ND 2.0 KR-
dc.rights.urihttps://creativecommons.org/licenses/by-nc-nd/2.0/kr/-
dc.titleTranslational possibility of [18F]Mefway to image serotonin 1A receptors in humans: Comparison with [18F]FCWAY in rodents-
dc.typeArticle-
dc.contributor.collegeCollege of Medicine (의과대학)-
dc.contributor.departmentDept. of Pharmacology (약리학)-
dc.contributor.googleauthorJae Yong Choi-
dc.contributor.googleauthorByoung Soo Kim-
dc.contributor.googleauthorChul Hoon Kim-
dc.contributor.googleauthorDong Goo Kim-
dc.contributor.googleauthorSang Jin Han-
dc.contributor.googleauthorKyochul Lee-
dc.contributor.googleauthorKyeong Min Kim-
dc.contributor.googleauthorGwangil An-
dc.contributor.googleauthorTae Hyun Choi-
dc.contributor.googleauthorSun Dong Yoo-
dc.contributor.googleauthorYoung Hoon Ryu-
dc.identifier.doi10.1002/syn.21771-
dc.admin.authorfalse-
dc.admin.mappingfalse-
dc.contributor.localIdA01057-
dc.contributor.localIdA02485-
dc.relation.journalcodeJ02710-
dc.identifier.eissn1098-2396-
dc.identifier.urlhttp://onlinelibrary.wiley.com/doi/10.1002/syn.21771/abstract-
dc.subject.keywordserotonin 1A receptors-
dc.subject.keyword[18F]Mefway-
dc.subject.keyword[18F]FCWAY-
dc.subject.keywordmicroPET-
dc.contributor.alternativeNameKim, Chul Hoon-
dc.contributor.alternativeNameRyu, Young Hoon-
dc.contributor.affiliatedAuthorKim, Chul Hoon-
dc.contributor.affiliatedAuthorRyu, Young Hoon-
dc.rights.accessRightsfree-
dc.citation.volume68-
dc.citation.number12-
dc.citation.startPage595-
dc.citation.endPage603-
dc.identifier.bibliographicCitationSYNAPSE, Vol.68(12) : 595-603, 2014-
dc.identifier.rimsid54990-
dc.type.rimsART-
Appears in Collections:
1. College of Medicine (의과대학) > Dept. of Nuclear Medicine (핵의학교실) > 1. Journal Papers
1. College of Medicine (의과대학) > Dept. of Pharmacology (약리학교실) > 1. Journal Papers

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