Cited 3 times in
Translational possibility of [18F]Mefway to image serotonin 1A receptors in humans: Comparison with [18F]FCWAY in rodents
DC Field | Value | Language |
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dc.contributor.author | 김철훈 | - |
dc.contributor.author | 유영훈 | - |
dc.date.accessioned | 2015-12-28T11:11:12Z | - |
dc.date.available | 2015-12-28T11:11:12Z | - |
dc.date.issued | 2014 | - |
dc.identifier.issn | 0887-4476 | - |
dc.identifier.uri | https://ir.ymlib.yonsei.ac.kr/handle/22282913/138883 | - |
dc.description.abstract | Purpose: 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.statementOfResponsibility | open | - |
dc.format.extent | 595~603 | - |
dc.relation.isPartOf | SYNAPSE | - |
dc.rights | CC BY-NC-ND 2.0 KR | - |
dc.rights.uri | https://creativecommons.org/licenses/by-nc-nd/2.0/kr/ | - |
dc.title | Translational possibility of [18F]Mefway to image serotonin 1A receptors in humans: Comparison with [18F]FCWAY in rodents | - |
dc.type | Article | - |
dc.contributor.college | College of Medicine (의과대학) | - |
dc.contributor.department | Dept. of Pharmacology (약리학) | - |
dc.contributor.googleauthor | Jae Yong Choi | - |
dc.contributor.googleauthor | Byoung Soo Kim | - |
dc.contributor.googleauthor | Chul Hoon Kim | - |
dc.contributor.googleauthor | Dong Goo Kim | - |
dc.contributor.googleauthor | Sang Jin Han | - |
dc.contributor.googleauthor | Kyochul Lee | - |
dc.contributor.googleauthor | Kyeong Min Kim | - |
dc.contributor.googleauthor | Gwangil An | - |
dc.contributor.googleauthor | Tae Hyun Choi | - |
dc.contributor.googleauthor | Sun Dong Yoo | - |
dc.contributor.googleauthor | Young Hoon Ryu | - |
dc.identifier.doi | 10.1002/syn.21771 | - |
dc.admin.author | false | - |
dc.admin.mapping | false | - |
dc.contributor.localId | A01057 | - |
dc.contributor.localId | A02485 | - |
dc.relation.journalcode | J02710 | - |
dc.identifier.eissn | 1098-2396 | - |
dc.identifier.url | http://onlinelibrary.wiley.com/doi/10.1002/syn.21771/abstract | - |
dc.subject.keyword | serotonin 1A receptors | - |
dc.subject.keyword | [18F]Mefway | - |
dc.subject.keyword | [18F]FCWAY | - |
dc.subject.keyword | microPET | - |
dc.contributor.alternativeName | Kim, Chul Hoon | - |
dc.contributor.alternativeName | Ryu, Young Hoon | - |
dc.contributor.affiliatedAuthor | Kim, Chul Hoon | - |
dc.contributor.affiliatedAuthor | Ryu, Young Hoon | - |
dc.rights.accessRights | free | - |
dc.citation.volume | 68 | - |
dc.citation.number | 12 | - |
dc.citation.startPage | 595 | - |
dc.citation.endPage | 603 | - |
dc.identifier.bibliographicCitation | SYNAPSE, Vol.68(12) : 595-603, 2014 | - |
dc.identifier.rimsid | 54990 | - |
dc.type.rims | ART | - |
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