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• W2937529510 abstract "The reference standards halo-GSK1482160 (F-, Br-, and I-) and their corresponding precursors desmethyl-halo-GSK1482160 (F-, Br-, and I-) were synthesized from (S)-1-methyl-5-oxopyrrolidine-2-carboxylic acid or (S)-5-oxopyrrolidine-2-carboxylic acid and 2-halo-3-(trifluoromethyl)benzylamine (F-, Br-, and I-) in one step with 45-93% yields. The target tracers [11C]halo-GSK1482160 (F-, Br-, and I-) were prepared from desmethyl-halo-GSK1482160 (F-, Br-, and I-) with [11C]CH3OTf under basic conditions (NaOH-Na2CO3, solid, w/w 1:2) through N-[11C]methylation and isolated by HPLC combined with SPE in 40-50% decay corrected radiochemical yield. The radiochemical purity was >99%, and the molar activity (AM) at end of bombardment (EOB) was 370-740 GBq/μmol. The potency of halo-GSK1482160 (F-, Br-, and I-) in comparison with GSK1482160 (Cl-) was determined by a radioligand competitive binding assay using [11C]GSK1482160, and the binding affinity Ki values for halo-GSK1482160 (F-, Br-, and I-) and GSK1482160 (Cl-) are 54.2, 2.5, 1.9 and 3.1 nM, respectively." @default.
• W2937529510 created "2019-04-25" @default.
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• W2937529510 date "2019-06-01" @default.
• W2937529510 modified "2023-10-14" @default.
• W2937529510 title "Synthesis and in vitro biological evaluation of new P2X7R radioligands [11C]halo-GSK1482160 analogs" @default.
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• W2937529510 doi "https://doi.org/10.1016/j.bmcl.2019.04.018" @default.
• W2937529510 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/31005444" @default.
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