Preparation and biodistribution of F-18 labeled FQNPe
- Oak Ridge National Lab., TN (United States)
1-Azabicyclo[2.2.2]oct-3-yl {alpha}-(1-fluoropentan-5-yl)-{alpha}-hydroxy-{alpha}-phenylacetate (FQNPe) is an attractive candidate for the in vivo imaging of muscarinic receptors (mAChR) by PET. Initial studies with this new agent demonstrated a high binding affinity and ability to bind to regions of the brain containing mAChR. Fluorine-18 (F-18) labeling of racemic 1 was performed using X = tosyl, triflate, or mesylate group and a decay corrected radiolabeling yields of 2.6, 33, 75%, respectively, were obtained. F-18-3 in 11 % yield (decay corrected to beginning of synthesis). Initial biodistribution studies in rats (n=5) showed F-18-3 had high cerebral uptake of 0.72 ({plus_minus}0.26) and 0.83 ({plus_minus} 0.12) injected dose/gram at 15 and 30 minutes, respectively. The F-18 labeling and biodistribution study of the (-)-quinuclidinyl (-)-acetate and (-)-quinuclidinyl (+)-acetate isomers of FQNPe are currently being pursued.
- DOE Contract Number:
- AC05-96OR22464
- OSTI ID:
- 447784
- Report Number(s):
- CONF-960659--
- Journal Information:
- Journal of Nuclear Medicine, Journal Name: Journal of Nuclear Medicine Journal Issue: Suppl.5 Vol. 37; ISSN 0161-5505; ISSN JNMEAQ
- Country of Publication:
- United States
- Language:
- English
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