Home > Publications database > Preparation of a First 18F-Labeled Agonist for M1 Muscarinic Acetylcholine Receptors > print

001     877587
005     20220930130242.0
024 7 _ |a 10.3390/molecules25122880
|2 doi
024 7 _ |a 2128/25225
|2 Handle
024 7 _ |a pmid:32585815
|2 pmid
024 7 _ |a WOS:000550178600001
|2 WOS
037 _ _ |a FZJ-2020-02309
082 _ _ |a 540
100 1 _ |a Zlatopolskiy, Boris D.
|0 P:(DE-Juel1)176188
|b 0
245 _ _ |a Preparation of a First 18F-Labeled Agonist for M1 Muscarinic Acetylcholine Receptors
260 _ _ |a Basel
|c 2020
|b MDPI
336 7 _ |a article
|2 DRIVER
336 7 _ |a Output Types/Journal article
|2 DataCite
336 7 _ |a Journal Article
|b journal
|m journal
|0 PUB:(DE-HGF)16
|s 1594040031_25319
|2 PUB:(DE-HGF)
336 7 _ |a ARTICLE
|2 BibTeX
336 7 _ |a JOURNAL_ARTICLE
|2 ORCID
336 7 _ |a Journal Article
|0 0
|2 EndNote
520 _ _ |a M1 muscarinic acetylcholine receptors (mAChRs) are abundant in postsynaptic nerve terminals of all forebrain regions and have been implicated in the cognitive decline associated with Alzheimer’s disease and other CNS pathologies. Consequently, major efforts have been spent in the development of subtype-selective positron emission tomography (PET) tracers for mAChRs resulting in the development of several 11C-labeled probes. However, protocols for the preparation of 18F-labeled mAChR-ligands have not been published so far. Here, we describe a straightforward procedure for the preparation of an 18F-labeled M1 mAChR agonist and its corresponding pinacol boronate radiolabeling precursor and the non-radioactive reference compound. The target compounds were prepared from commercially available aryl fluorides and Boc protected 4-aminopiperidine using a convergent reaction protocol. The radiolabeling precursor was prepared by a modification of the Miyaura reaction and labeled via the alcohol-enhanced Cu-mediated radiofluorination. The developed procedure afforded the radiotracer in a non-decay-corrected radiochemical yield of 17 ± 3% (n = 3) and in excellent radiochemical purity (>99%) on a preparative scale. Taken together, we developed a straightforward protocol for the preparation of an 18F-labeled M1 mAChR agonist that is amenable for automation and thus provides an important step towards the routine production of a 18F-labeled M1 selective PET tracer for experimental and diagnostic applications.
536 _ _ |a 573 - Neuroimaging (POF3-573)
|0 G:(DE-HGF)POF3-573
|c POF3-573
|f POF III
|x 0
588 _ _ |a Dataset connected to CrossRef
700 1 _ |a Neumaier, Felix
|0 0000-0002-6376-6391
|b 1
700 1 _ |a Rüngeler, Till
|0 0000-0003-4574-6116
|b 2
700 1 _ |a Drewes, Birte
|0 P:(DE-Juel1)131817
|b 3
700 1 _ |a Kolks, Niklas
|0 P:(DE-Juel1)178654
|b 4
700 1 _ |a Neumaier, Bernd
|0 P:(DE-Juel1)166419
|b 5
|e Corresponding author
773 _ _ |a 10.3390/molecules25122880
|g Vol. 25, no. 12, p. 2880 -
|0 PERI:(DE-600)2008644-1
|n 12
|p 2880 -
|t Molecules
|v 25
|y 2020
|x 1420-3049
856 4 _ |u https://juser.fz-juelich.de/record/877587/files/Invoice_molecules-796745.pdf
856 4 _ |x pdfa
|u https://juser.fz-juelich.de/record/877587/files/Invoice_molecules-796745.pdf?subformat=pdfa
856 4 _ |y OpenAccess
|u https://juser.fz-juelich.de/record/877587/files/molecules-25-02880.pdf
856 4 _ |y OpenAccess
|x pdfa
|u https://juser.fz-juelich.de/record/877587/files/molecules-25-02880.pdf?subformat=pdfa
909 C O |o oai:juser.fz-juelich.de:877587
|p openaire
|p open_access
|p OpenAPC
|p driver
|p VDB
|p openCost
|p dnbdelivery
910 1 _ |a Forschungszentrum Jülich
|0 I:(DE-588b)5008462-8
|k FZJ
|b 0
|6 P:(DE-Juel1)176188
910 1 _ |a INM-5
|0 I:(DE-HGF)0
|b 1
|6 0000-0002-6376-6391
910 1 _ |a Forschungszentrum Jülich
|0 I:(DE-588b)5008462-8
|k FZJ
|b 1
|6 0000-0002-6376-6391
910 1 _ |a Forschungszentrum Jülich
|0 I:(DE-588b)5008462-8
|k FZJ
|b 3
|6 P:(DE-Juel1)131817
910 1 _ |a Forschungszentrum Jülich
|0 I:(DE-588b)5008462-8
|k FZJ
|b 4
|6 P:(DE-Juel1)178654
910 1 _ |a Forschungszentrum Jülich
|0 I:(DE-588b)5008462-8
|k FZJ
|b 5
|6 P:(DE-Juel1)166419
913 1 _ |a DE-HGF
|b Key Technologies
|l Decoding the Human Brain
|1 G:(DE-HGF)POF3-570
|0 G:(DE-HGF)POF3-573
|2 G:(DE-HGF)POF3-500
|v Neuroimaging
|x 0
|4 G:(DE-HGF)POF
|3 G:(DE-HGF)POF3
914 1 _ |y 2020
915 _ _ |a DBCoverage
|0 StatID:(DE-HGF)0200
|2 StatID
|b SCOPUS
|d 2020-01-03
915 _ _ |a DBCoverage
|0 StatID:(DE-HGF)0160
|2 StatID
|b Essential Science Indicators
|d 2020-01-03
915 _ _ |a Creative Commons Attribution CC BY 4.0
|0 LIC:(DE-HGF)CCBY4
|2 HGFVOC
915 _ _ |a DBCoverage
|0 StatID:(DE-HGF)0600
|2 StatID
|b Ebsco Academic Search
|d 2020-01-03
915 _ _ |a DBCoverage
|0 StatID:(DE-HGF)1150
|2 StatID
|b Current Contents - Physical, Chemical and Earth Sciences
|d 2020-01-03
915 _ _ |a DBCoverage
|0 StatID:(DE-HGF)0501
|2 StatID
|b DOAJ Seal
|d 2020-01-03
915 _ _ |a DBCoverage
|0 StatID:(DE-HGF)0500
|2 StatID
|b DOAJ
|d 2020-01-03
915 _ _ |a WoS
|0 StatID:(DE-HGF)0111
|2 StatID
|b Science Citation Index Expanded
|d 2020-01-03
915 _ _ |a Fees
|0 StatID:(DE-HGF)0700
|2 StatID
|d 2020-01-03
915 _ _ |a DBCoverage
|0 StatID:(DE-HGF)0150
|2 StatID
|b Web of Science Core Collection
|d 2020-01-03
915 _ _ |a OpenAccess
|0 StatID:(DE-HGF)0510
|2 StatID
915 _ _ |a Peer Review
|0 StatID:(DE-HGF)0030
|2 StatID
|b ASC
|d 2020-01-03
915 _ _ |a Article Processing Charges
|0 StatID:(DE-HGF)0561
|2 StatID
|f 2020-01-03
915 _ _ |a DBCoverage
|0 StatID:(DE-HGF)0310
|2 StatID
|b NCBI Molecular Biology Database
|d 2020-01-03
915 _ _ |a DBCoverage
|0 StatID:(DE-HGF)0300
|2 StatID
|b Medline
|d 2020-01-03
915 _ _ |a DBCoverage
|0 StatID:(DE-HGF)0320
|2 StatID
|b PubMed Central
|d 2020-01-03
915 _ _ |a DBCoverage
|0 StatID:(DE-HGF)0199
|2 StatID
|b Clarivate Analytics Master Journal List
|d 2020-01-03
920 1 _ |0 I:(DE-Juel1)INM-5-20090406
|k INM-5
|l Nuklearchemie
|x 0
980 _ _ |a journal
980 _ _ |a VDB
980 _ _ |a UNRESTRICTED
980 _ _ |a I:(DE-Juel1)INM-5-20090406
980 _ _ |a APC
980 1 _ |a APC
980 1 _ |a FullTexts

LibraryCollectionCLSMajorCLSMinorLanguageAuthor
Marc 21