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Title: Nuclear Medicine Program progress report for quarter ending September 30, 1991

Abstract

Rat tissue distribution properties of IQNP,'' a new radioiodinated cholinergic-muscarinic receptor antagonist, are described. IQNP is the acronym for 1-azabicyclo(2.2.2)oct-3-yl {alpha}-hydroxy-{alpha}-phenyl-{alpha}(1-iodo-1-propen-3-yl) acetate, which is an analogue of the QNB muscarinic antagonist in which the p-iodophenyl moiety has been replaced with the 1-iodo-1-propen-3-yl moiety. The radioiodinated IQNP analogue is easier to prepare in much higher yields than QNB and is thus a candidate for the evaluation of muscarinic receptors by external imaging techniques. Studies in rats demonstrated that IQNP shows high uptake in those cerebral regions rich in muscarinic receptors QNB-treatment of rats either 1 h before (pre) or 2 h after (post) administration of radioiodinated IQNP resulted in significant displacement or blocking of cerebral specific IQNP uptake (% dose/gm) in the cortex and striatum. These studies demonstrate that IQNP has specificity for the cholinergic-muscarinic receptor and is a good candidate for further studies. Also during this period, several agents developed in the ORNL Nuclear Medicine Program were supplied to Medical Cooperative Programs for collaborative studies including the iodine-125-labeled BMIPP and DMIPP fatty acid analogues and the IPM antibody labeling agent. Tin-117m and gold-199 were produced in the ORNL High Flux Isotope Reactor (HFIR) and supplied to the OHER-supported program inmore » the Medical Department at Brookhaven National Laboratory to aid in their research until the re-start of the High Flux Brookhaven Reactor.« less

Authors:
; ; ; ; ; ; ; ; ;
Publication Date:
Research Org.:
Oak Ridge National Lab., TN (United States)
Sponsoring Org.:
USDOE; USDOE, Washington, DC (United States)
OSTI Identifier:
5865129
Report Number(s):
ORNL/TM-11992
ON: DE92006979
DOE Contract Number:  
AC05-84OR21400
Resource Type:
Technical Report
Country of Publication:
United States
Language:
English
Subject:
62 RADIOLOGY AND NUCLEAR MEDICINE; 59 BASIC BIOLOGICAL SCIENCES; ACETATES; TISSUE DISTRIBUTION; LABELLED COMPOUNDS; NUCLEAR MEDICINE; RESEARCH PROGRAMS; ACETYLCHOLINE; ANIMAL TISSUES; CEREBELLUM; CEREBRAL CORTEX; CHEMICAL BONDS; GOLD 199; IODINATION; IODINE 125; LIGANDS; PROGRESS REPORT; RATS; TIN 117; UPTAKE; AMINES; AMMONIUM COMPOUNDS; ANIMALS; AUTONOMIC NERVOUS SYSTEM AGENTS; BETA DECAY RADIOISOTOPES; BETA-MINUS DECAY RADIOISOTOPES; BODY; BRAIN; CARBOXYLIC ACID SALTS; CENTRAL NERVOUS SYSTEM; CEREBRUM; CHEMICAL REACTIONS; DAYS LIVING RADIOISOTOPES; DISTRIBUTION; DOCUMENT TYPES; DRUGS; ELECTRON CAPTURE RADIOISOTOPES; ESTERS; EVEN-ODD NUCLEI; GOLD ISOTOPES; HALOGENATION; HEAVY NUCLEI; INTERMEDIATE MASS NUCLEI; INTERNAL CONVERSION RADIOISOTOPES; IODINE ISOTOPES; ISOMERIC TRANSITION ISOTOPES; ISOTOPES; MAMMALS; MEDICINE; NERVOUS SYSTEM; NEUROREGULATORS; NUCLEI; ODD-EVEN NUCLEI; ORGANIC COMPOUNDS; ORGANS; PARASYMPATHOMIMETICS; QUATERNARY COMPOUNDS; RADIOISOTOPES; RODENTS; STABLE ISOTOPES; TIN ISOTOPES; TISSUES; VERTEBRATES; 550601* - Medicine- Unsealed Radionuclides in Diagnostics; 550604 - Medicine- Unsealed Radionuclides in Therapy- (1980-); 550201 - Biochemistry- Tracer Techniques

Citation Formats

Knapp, Jr, F F, Ambrose, K R, Callahan, A P, McPherson, D W, Mirzadeh, S, Srivastava, P C, Hasan, A, Lambert, C R, Lambert, S J, and Rice, D E. Nuclear Medicine Program progress report for quarter ending September 30, 1991. United States: N. p., 1992. Web. doi:10.2172/5865129.
Knapp, Jr, F F, Ambrose, K R, Callahan, A P, McPherson, D W, Mirzadeh, S, Srivastava, P C, Hasan, A, Lambert, C R, Lambert, S J, & Rice, D E. Nuclear Medicine Program progress report for quarter ending September 30, 1991. United States. doi:10.2172/5865129.
Knapp, Jr, F F, Ambrose, K R, Callahan, A P, McPherson, D W, Mirzadeh, S, Srivastava, P C, Hasan, A, Lambert, C R, Lambert, S J, and Rice, D E. Sat . "Nuclear Medicine Program progress report for quarter ending September 30, 1991". United States. doi:10.2172/5865129. https://www.osti.gov/servlets/purl/5865129.
@article{osti_5865129,
title = {Nuclear Medicine Program progress report for quarter ending September 30, 1991},
author = {Knapp, Jr, F F and Ambrose, K R and Callahan, A P and McPherson, D W and Mirzadeh, S and Srivastava, P C and Hasan, A and Lambert, C R and Lambert, S J and Rice, D E},
abstractNote = {Rat tissue distribution properties of IQNP,'' a new radioiodinated cholinergic-muscarinic receptor antagonist, are described. IQNP is the acronym for 1-azabicyclo(2.2.2)oct-3-yl {alpha}-hydroxy-{alpha}-phenyl-{alpha}(1-iodo-1-propen-3-yl) acetate, which is an analogue of the QNB muscarinic antagonist in which the p-iodophenyl moiety has been replaced with the 1-iodo-1-propen-3-yl moiety. The radioiodinated IQNP analogue is easier to prepare in much higher yields than QNB and is thus a candidate for the evaluation of muscarinic receptors by external imaging techniques. Studies in rats demonstrated that IQNP shows high uptake in those cerebral regions rich in muscarinic receptors QNB-treatment of rats either 1 h before (pre) or 2 h after (post) administration of radioiodinated IQNP resulted in significant displacement or blocking of cerebral specific IQNP uptake (% dose/gm) in the cortex and striatum. These studies demonstrate that IQNP has specificity for the cholinergic-muscarinic receptor and is a good candidate for further studies. Also during this period, several agents developed in the ORNL Nuclear Medicine Program were supplied to Medical Cooperative Programs for collaborative studies including the iodine-125-labeled BMIPP and DMIPP fatty acid analogues and the IPM antibody labeling agent. Tin-117m and gold-199 were produced in the ORNL High Flux Isotope Reactor (HFIR) and supplied to the OHER-supported program in the Medical Department at Brookhaven National Laboratory to aid in their research until the re-start of the High Flux Brookhaven Reactor.},
doi = {10.2172/5865129},
journal = {},
number = ,
volume = ,
place = {United States},
year = {1992},
month = {2}
}