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Knapp, F.F. Jr.; Ambrose, K.R.; Beets, A.L.; Lambert, C.R.; McPherson, D.W.; Mirzadeh, S.; Luo, H.
Oak Ridge National Lab., TN (United States). Funding organisation: USDOE, Washington, DC (United States)1995
Oak Ridge National Lab., TN (United States). Funding organisation: USDOE, Washington, DC (United States)1995
AbstractAbstract
[en] 1-Azabicyclo[2.2.2]oct-3-yl α-(l-fluoropentan-5-yl)-α-hydroxy-α-phenylacetate (PQNPe) has been prepared and evaluated as a new candidate for the determination of muscarinic cholinergic receptor density by positron emission tomography (PET). The results of in vitro binding assays demonstrated that FONPe has high affinity for ml and M2 muscarinic receptor subtypes. Pretreatment of female Fisher rats with unlabeled FQNPe one hour prior to the intravenous administration of radioiodinated Z-(R,R)-IQNP, a high affinity muscarinic ligand, demonstrated FONPE significantly blocked the uptake of radioactivity in the brain and heart measured three hours post-injection of the radiolabeled ligand. These results demonstrate that this new fluoro analogue of QNB has high affinity for the muscarinic receptor and is able to effectively pass the blood-brain-barrier and localize in tissues rich in muscarinic receptors. The fluorine-18-labeled analogue thus represents an important target ligands for evaluation as potential receptor imaging agents in conjunction with PET. During this period several radioisotopes were provided to collaborators. Tungsten-188/rhenium-188 generators were provided as part of a CRADA project
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Feb 1995; 23 p; CONTRACT AC05-84OR21400; Also available from OSTI as DE95008100; NTIS; US Govt. Printing Office Dep
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Report
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Progress Report
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BETA DECAY RADIOISOTOPES, BETA-MINUS DECAY RADIOISOTOPES, BETA-PLUS DECAY RADIOISOTOPES, CHEMISTRY, DOCUMENT TYPES, FLUORINE ISOTOPES, HOURS LIVING RADIOISOTOPES, INTERMEDIATE MASS NUCLEI, INTERNAL CONVERSION RADIOISOTOPES, IODINE ISOTOPES, ISOMERIC TRANSITION ISOTOPES, ISOTOPES, LIGHT NUCLEI, MEDICINE, NUCLEI, ODD-EVEN NUCLEI, ODD-ODD NUCLEI, ORGANIC COMPOUNDS, ORGANIC HALOGEN COMPOUNDS, RADIOISOTOPES, TOMOGRAPHY, YEARS LIVING RADIOISOTOPES
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