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- W2034622039 abstract "Racemic E-1-azabicyclo[2.2.2]oct-3-yl α-(1-bromo-1-1-propen-3-yl)-α-hydroxy-α-phenylacetate (BrQNP) was prepared and evaluated in vivo as a potential candidate for imaging muscarinic acetylcholinergic receptors by Positron Emission Tomography. Initial in vivo blocking studies utilizing Z-(-,-)-[ 125 I]IQNP as a radiolabelled muscarinic probe demonstrated that a preinjection of cold E-BrQNP effectively blocks the uptake of the radiolabelled probe in the brain and heart, by 71% and 86% respectively. Z-(-,-)-[ 76 Br]BrQNP was prepared by electrophilic substitution from a tributylstannyl precursor. Peracetic acid and chloramine T were evaluated as oxidizing agents. After purification by SPE and RP-HPLC, radiolabelling yields of 85% and 95% were obtained with peracetic acid and chloramine T, respectively. The final radiochemical yield was 70% for both oxidizing agents. Rat biodistribution studies of Z-(-,-)-[ 76 Br]BrQNP showed high uptake in organs with high concentrations of muscarinic receptors (heart and brain)." @default.
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- W2034622039 date "1996-10-01" @default.
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- W2034622039 title "Z-(-,-)-[76Br]BrQNP: A high affinity PET radiotracer for central and cardiac muscarinic receptors" @default.
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- W2034622039 doi "https://doi.org/10.1002/(sici)1099-1344(199610)38:10<883::aid-jlcr902>3.0.co;2-x" @default.
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