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Novel radiolabeled vanilloid with enhanced specificity for human transient receptor potential vanilloid 1(TRPV1)
DC Field | Value | Language |
---|---|---|
dc.contributor.author | Pearce, Larry V. | - |
dc.contributor.author | Ann, Jihyae | - |
dc.contributor.author | Jung, Aeran | - |
dc.contributor.author | Thorat, Shiyaii A. | - |
dc.contributor.author | Herold, Brienna K. A. | - |
dc.contributor.author | Habtemichael, Amelework D. | - |
dc.contributor.author | Blumberg, Peter M. | - |
dc.contributor.author | Lee, Jeewoo | - |
dc.creator | 이지우 | - |
dc.date.accessioned | 2019-04-25T02:05:02Z | - |
dc.date.available | 2020-04-05T02:05:02Z | - |
dc.date.created | 2018-01-25 | - |
dc.date.created | 2018-01-25 | - |
dc.date.issued | 2017-10 | - |
dc.identifier.citation | Journal of Medicinal Chemistry, Vol.60 No.19, pp.8246-8252 | - |
dc.identifier.issn | 0022-2623 | - |
dc.identifier.uri | https://hdl.handle.net/10371/150134 | - |
dc.description.abstract | Transient receptor potential vanilloid 1 (TRPV1) has emerged as a promising therapeutic target. While radiolabeled resiniferatoxin (RTX) has provided a powerful tool for characterization of vanilloid binding to TRPV1, TRPV1 shows 20-fold weaker binding to the human TRPV1 than to the rodent TRPV1. We now describe a tritium 13 radiolabeled synthetic vanilloid antagonist, 1-((2-(4-(methyl-[H-3])piperidin-1-yl-4-[H-3])-6-(trifluoromethyl)pyridin-3-yl)-methyl)-3-(3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-8-yl)urea ([H-3]MPOU), that embodies improved absolute affinity for human TRPV1 and improved synthetic accessibility. | - |
dc.language | 영어 | - |
dc.language.iso | en | en |
dc.publisher | American Chemical Society | - |
dc.title | Novel radiolabeled vanilloid with enhanced specificity for human transient receptor potential vanilloid 1(TRPV1) | - |
dc.type | Article | - |
dc.identifier.doi | 10.1021/acs.jmedchem.7b00859 | - |
dc.citation.journaltitle | Journal of Medicinal Chemistry | - |
dc.identifier.wosid | 000413131400021 | - |
dc.identifier.scopusid | 2-s2.0-85031303255 | - |
dc.description.srnd | OAIID:RECH_ACHV_DSTSH_NO:T201724911 | - |
dc.description.srnd | RECH_ACHV_FG:RR00200001 | - |
dc.description.srnd | ADJUST_YN: | - |
dc.description.srnd | EMP_ID:A003772 | - |
dc.description.srnd | CITE_RATE:6.253 | - |
dc.description.srnd | DEPT_NM:약학과 | - |
dc.description.srnd | EMAIL:jeewoo@snu.ac.kr | - |
dc.description.srnd | SCOPUS_YN:Y | - |
dc.citation.endpage | 8252 | - |
dc.citation.number | 19 | - |
dc.citation.startpage | 8246 | - |
dc.citation.volume | 60 | - |
dc.description.isOpenAccess | N | - |
dc.contributor.affiliatedAuthor | Lee, Jeewoo | - |
dc.identifier.srnd | T201724911 | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.subject.keywordPlus | ANALGESIC AGENTS | - |
dc.subject.keywordPlus | AGONIST ACTIVITY | - |
dc.subject.keywordPlus | CAPSAICIN RECEPTOR | - |
dc.subject.keywordPlus | ANTAGONISTS | - |
dc.subject.keywordPlus | ANALOGS | - |
dc.subject.keywordPlus | RESINIFERATOXIN | - |
dc.subject.keywordPlus | SENSITIVITY | - |
dc.subject.keywordPlus | ACTIVATION | - |
dc.subject.keywordPlus | POTENCY | - |
dc.subject.keywordPlus | DOCKING | - |
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