skip to main content
OSTI.GOV title logo U.S. Department of Energy
Office of Scientific and Technical Information

Title: Nuclear medicine program progress report for quarter ending December 31, 1994

Abstract

1-Azabicyclo[2.2.2]oct-3-yl {alpha}-(l-fluoropentan-5-yl)-{alpha}-hydroxy-{alpha}-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 m{sub l} and M{sub 2} 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.

Authors:
; ; ; ; ; ;
Publication Date:
Research Org.:
Oak Ridge National Lab., TN (United States)
Sponsoring Org.:
USDOE, Washington, DC (United States)
OSTI Identifier:
10127348
Report Number(s):
ORNL/TM-12909
ON: DE95008100;
DOE Contract Number:  
AC05-84OR21400
Resource Type:
Technical Report
Resource Relation:
Other Information: PBD: Feb 1995
Country of Publication:
United States
Language:
English
Subject:
62 RADIOLOGY AND NUCLEAR MEDICINE; LABELLED COMPOUNDS; AFFINITY; ORGANIC FLUORINE COMPOUNDS; PROGRESS REPORT; NUCLEAR MEDICINE; RADIOCHEMISTRY; IODINE 129; FLUORINE 18; LIGANDS; COMPUTERIZED TOMOGRAPHY; BLOOD-BRAIN BARRIER; 550601; UNSEALED RADIONUCLIDES IN DIAGNOSTICS

Citation Formats

Knapp, Jr, F F, Ambrose, K R, Beets, A L, Lambert, C R, McPherson, D W, Mirzadeh, S, and Luo, H. Nuclear medicine program progress report for quarter ending December 31, 1994. United States: N. p., 1995. Web.
Knapp, Jr, F F, Ambrose, K R, Beets, A L, Lambert, C R, McPherson, D W, Mirzadeh, S, & Luo, H. Nuclear medicine program progress report for quarter ending December 31, 1994. United States.
Knapp, Jr, F F, Ambrose, K R, Beets, A L, Lambert, C R, McPherson, D W, Mirzadeh, S, and Luo, H. Wed . "Nuclear medicine program progress report for quarter ending December 31, 1994". United States.
@article{osti_10127348,
title = {Nuclear medicine program progress report for quarter ending December 31, 1994},
author = {Knapp, Jr, F F and Ambrose, K R and Beets, A L and Lambert, C R and McPherson, D W and Mirzadeh, S and Luo, H},
abstractNote = {1-Azabicyclo[2.2.2]oct-3-yl {alpha}-(l-fluoropentan-5-yl)-{alpha}-hydroxy-{alpha}-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 m{sub l} and M{sub 2} 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.},
doi = {},
journal = {},
number = ,
volume = ,
place = {United States},
year = {1995},
month = {2}
}

Technical Report:
Other availability
Please see Document Availability for additional information on obtaining the full-text document. Library patrons may search WorldCat to identify libraries that may hold this item. Keep in mind that many technical reports are not cataloged in WorldCat.

Save / Share: