{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,4,4]],"date-time":"2026-04-04T07:00:22Z","timestamp":1775286022454,"version":"3.50.1"},"reference-count":22,"publisher":"Frontiers Media SA","license":[{"start":{"date-parts":[[2022,12,23]],"date-time":"2022-12-23T00:00:00Z","timestamp":1671753600000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of China","doi-asserted-by":"publisher","id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100018534","name":"Medical Innovation Project of Fujian Province","doi-asserted-by":"publisher","id":[{"id":"10.13039\/501100018534","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":["frontiersin.org"],"crossmark-restriction":true},"short-container-title":["Front. Chem."],"abstract":"<jats:p>Macrophages have crucial roles in the pathogenesis of rheumatoid arthritis (RA). We aimed to elucidate the temporal profile of macrophage infiltration in synovitis in RA rat models using PET (positron emission tomography) imaging based a new generation of TSPO (Translocator protein, 18\u00a0kDa)-PET ligand, <jats:sup>18<\/jats:sup>F-VUIIS1008 {2-[5,7-Diethyl-2-{4-[2-(<jats:sup>18<\/jats:sup>F)fluoroethoxy]phenyl}pyrazolo(1,5-a)pyri-midin-3-yl]-N, N-diethylacetamide}. <jats:italic>In vitro<\/jats:italic> and <jats:italic>in vivo<\/jats:italic> studies were conducted using RAW264.7 macrophage cells and a rat model of RA induced by Complete Freund\u2019s Adjuvant (CFA). Our results showed <jats:sup>18<\/jats:sup>F-VUIIS1008 showed excellent stability <jats:italic>in vitro<\/jats:italic> and binding specificity to RAW264.7 cells, and rapid accumulation in the left inflammatory ankles. PET studies revealed that <jats:sup>18<\/jats:sup>F-VUIIS1008 could clearly identify the left inflammatory ankles with good contrast at 30\u2013120\u00a0min post-injection. The uptake of <jats:sup>18<\/jats:sup>F-VUIIS1008 of left inflammatory ankles was a wiggle trace with two peaks on day 7 and 29, and then, the highest peak uptake was seen on day 29 (3.00% \u00b1 0.08%ID\/g) at 60\u00a0min after injection. Tracer uptakes could be inhibited by PK11195 or VUIIS1008. Immunohistochemistry and immunofluorescence tests showed that elevated TSPO expression and infiltrated macrophages were found in the left inflammation ankles. <jats:sup>18<\/jats:sup>F-VUIIS1008 as a novel PET imaging agent showed great potential to identify temporal profile of macrophage infiltration in synovitis in RA, and deliver accurate non-invasive diagnosis and real-time monitoring of RA development.<\/jats:p>","DOI":"10.3389\/fchem.2022.1064518","type":"journal-article","created":{"date-parts":[[2022,12,23]],"date-time":"2022-12-23T05:20:26Z","timestamp":1671772826000},"update-policy":"https:\/\/doi.org\/10.3389\/crossmark-policy","source":"Crossref","is-referenced-by-count":3,"title":["Longitudinal 18F-VUIIS1008 PET imaging in a rat model of rheumatoid arthritis"],"prefix":"10.3389","volume":"10","author":[{"given":"Xinhui","family":"Su","sequence":"first","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Liangliang","family":"Wang","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Rongshui","family":"Yang","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Zhide","family":"Guo","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1965","published-online":{"date-parts":[[2022,12,23]]},"reference":[{"key":"B1","doi-asserted-by":"publisher","first-page":"679","DOI":"10.1038\/nri3495","article-title":"Mitogen-activated protein kinases in innate immunity","volume":"13","author":"Arthur","year":"2013","journal-title":"Nat. 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