Fluorine-18 radiolabelling and in vitro / in vivo metabolism of [18F]D4-PBR111

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dc.contributor.authorWyatt, NAen_AU
dc.contributor.authorSafavi-Naeini, Men_AU
dc.contributor.authorWotherspoon, ATLen_AU
dc.contributor.authorArthur, Aen_AU
dc.contributor.authorNguyen, APen_AU
dc.contributor.authorParmar, Aen_AU
dc.contributor.authorHamze, Hen_AU
dc.contributor.authorDay, CMen_AU
dc.contributor.authorZahra, Den_AU
dc.contributor.authorMatesic, Len_AU
dc.contributor.authorDavis, Een_AU
dc.contributor.authorRahardjo, GLen_AU
dc.contributor.authorYepuri, NRen_AU
dc.contributor.authorShepherd, Ren_AU
dc.contributor.authorMurphy, RBen_AU
dc.contributor.authorPham, TQen_AU
dc.contributor.authorNguyen, VHen_AU
dc.contributor.authorCallaghan, PDen_AU
dc.contributor.authorHolden, PJen_AU
dc.contributor.authorGrégoire, MCen_AU
dc.contributor.authorDarwish, TAen_AU
dc.contributor.authorFraser, BHen_AU
dc.date.accessioned2021-09-08T00:02:13Zen_AU
dc.date.available2021-09-08T00:02:13Zen_AU
dc.date.issued2019-05-26en_AU
dc.date.statistics2021-08-31en_AU
dc.descriptionVolume 62, Supplement 1 of the Journal of Labelled Compounds & Pharmaceuticals is comprised of the Abstracts from ISRS 2019.en_AU
dc.description.abstractObjectives The purinergic receptor P2X ligand-gated ion channel type 7 (P2X7R) is an adenosine triphosphate (ATP)-gated ion-channel, and P2X7R is a key player in inflammation. P2X7R is an emerging therapeutic target in central nervous system (CNS) diseases including Alzheimer's disease (AD) and Parkinson's disease (PD), because P2X7R also plays a pivotal role in neuroinflammation. P2X7R represents a potential molecular imaging target for neuroinflammation via biomedical imaging technique positron emission tomography (PET), and several radioligands targeting P2X7R have been developed and evaluated in animals. In our previous work, we have developed and characterized [11C]GSK1482160 as a P2X7R radioligand for neuroinflammation,2 clinical evaluation of [11C]GSK1482160 in healthy controls and patients is currently underway, and the estimation of radiation dosimetry for [11C]GSK1482160 in normal human subjects has been reported.3 Since the half-life (t1/2) of radionuclide carbon-11 is only 20.4 min, it is attractive for us to develop derivatives of [11C]GSK1482160, which can be labeled with the radionuclide fluorine-18 (t1/2, 109.7 min), and a fluorine-18 ligand would be ideal for widespread use.4 To this end, a series of [18F]fluoroalkyl including [18F]fluoromethyl (FM), [18F]fluoroethyl (FE), and [18F]fluoropropyl (FP) derivatives of GSK1482160 have been prepared and examined as new potential P2X7R radioligands. © 2019 The Authorsen_AU
dc.description.sponsorshipThe authors gratefully acknowledge the support of the Australian Institute of Nuclear Scientists and Engineers (AINSE) for the provision of post‐graduate student scholarships. The authors gratefully acknowledge the support of the Australian National Imaging Facility (NIF).en_AU
dc.identifier.citationWyatt, N. A., Safavi-Naeini, M., Wotherspoon, A., Arthur, A., Nguyen, A. P., Parmar, A., Hamze, H., Day, C. M., Zahra, D., Matesic, L., Davis, E., Rahardjo, G. L., Yepuri, N. R., Shepherd, R. K., Murphy, R. B., Pham, T. Q., Nguyen, V. H., Callaghan, P. D., Holden, P. J., Grégoire, M.-C., Darwish, T.A. & Fraser, B. H. (2019). Fluorine-18 radiolabelling and in vitro / in vivo metabolism of [18F]D4-PBR111. Poster presented at the 23rd International Symposium on Radiopharmaceutical Sciences (ISRS 2019), Beijing, China, 26 to 31 May 2019. In Journal of Labelled Compounds and Radiopharmaceuticals 62(S1), S123-S588. doi:10.1002/jlcr.3725en_AU
dc.identifier.conferenceenddate31 May 2019en_AU
dc.identifier.conferencename23rd International Symposium on Radiopharmaceutical Sciences (ISRS 2019)en_AU
dc.identifier.conferenceplaceBeijing, Chinaen_AU
dc.identifier.conferencestartdate26 May 2019en_AU
dc.identifier.issn1099-1344en_AU
dc.identifier.issueS1en_AU
dc.identifier.journaltitleJournal of Labelled Compounds and Radiopharmaceuticalsen_AU
dc.identifier.paginationS123-S588en_AU
dc.identifier.urihttps://doi.org/10.1002/jlcr.3725en_AU
dc.identifier.urihttps://apo.ansto.gov.au/dspace/handle/10238/11622en_AU
dc.identifier.volume62en_AU
dc.language.isoenen_AU
dc.publisherJohn Wiley & Sons, Incen_AU
dc.subjectFluorine 18en_AU
dc.subjectProteinsen_AU
dc.subjectLigandsen_AU
dc.subjectInflammationen_AU
dc.subjectTracer techniquesen_AU
dc.subjectRatsen_AU
dc.titleFluorine-18 radiolabelling and in vitro / in vivo metabolism of [18F]D4-PBR111en_AU
dc.typeConference Posteren_AU
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