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Title: Nuclear medicine program progress report for quarter ending December 31, 1992

Abstract

We describe the synthesis of the cis- and trans-iodovinyl isomers of the new ORNL cholinergic-muscarinicreceptorligand, 1 -azabicyclo[2.2-2]oct-3-yl[alpha]-hydroxy-[alpha]-(1-iodo-l-propen-3-yl)-[alpha]-phenylacetate ( IQNP''). This agent is prepared in high radiochemical yield, and the racemic mixture shows high specificity and selectivity for the cerebral and myocardial receptors. Since two chiral centers are present in this molecule, it is important to evaluate the importance of the absolute configuration of the two centers on receptor specificity. The tributyltin substrates were carefully separated by column chromatography, converted to the iodine-125 analogues by iododestannylation, and evaluated in rats in vivo. While the E'' (trans) isomer cleared rapidly from the receptor-rich areas of rat brain, the Z'' (cis) isomer showed high uptake in these areas but also high concentration in the cerebellum. In contrast, the E,Z-isomeric mixture showed good uptake and retention in the receptor rich areas. Also described in this report is a description of neutron flux measurements in the hydraulic tube position at the ORNL High Flux Isotope Reactor (HFIR). Also during this period, samples of [l-125]- and [l-131]-labeled racemic IQNP'' were supplied through a collaborative program with the Brookhaven National Laboratory for high resolution autoradiographic studies in rat tissues.

Authors:
; ; ; ; ; ; ;
Publication Date:
Research Org.:
Oak Ridge National Lab., TN (United States)
Sponsoring Org.:
USDOE; USDOE, Washington, DC (United States)
OSTI Identifier:
6567857
Report Number(s):
ORNL/TM-12312
ON: DE93011789
DOE Contract Number:  
AC05-84OR21400
Resource Type:
Technical Report
Country of Publication:
United States
Language:
English
Subject:
62 RADIOLOGY AND NUCLEAR MEDICINE; 38 RADIATION CHEMISTRY, RADIOCHEMISTRY, AND NUCLEAR CHEMISTRY; PARASYMPATHOMIMETICS; IODINATION; LABELLING; RADIOPHARMACEUTICALS; CHEMICAL PREPARATION; AUTORADIOGRAPHY; BLOOD; CEREBELLUM; CEREBRAL CORTEX; HEART; IODINE 125; IODINE 131; NUCLEAR MEDICINE; ORGANOMETALLIC COMPOUNDS; PROGRESS REPORT; RATS; TIN COMPOUNDS; TISSUE DISTRIBUTION; ANIMALS; AUTONOMIC NERVOUS SYSTEM AGENTS; BETA DECAY RADIOISOTOPES; BETA-MINUS DECAY RADIOISOTOPES; BIOLOGICAL MATERIALS; BODY; BODY FLUIDS; BRAIN; CARDIOVASCULAR SYSTEM; CENTRAL NERVOUS SYSTEM; CEREBRUM; CHEMICAL REACTIONS; DAYS LIVING RADIOISOTOPES; DISTRIBUTION; DOCUMENT TYPES; DRUGS; ELECTRON CAPTURE RADIOISOTOPES; HALOGENATION; INTERMEDIATE MASS NUCLEI; INTERNAL CONVERSION RADIOISOTOPES; IODINE ISOTOPES; ISOTOPES; LABELLED COMPOUNDS; MAMMALS; MATERIALS; MEDICINE; NERVOUS SYSTEM; NUCLEI; ODD-EVEN NUCLEI; ORGANIC COMPOUNDS; ORGANS; RADIOISOTOPES; RODENTS; SYNTHESIS; VERTEBRATES; 550604* - Medicine- Unsealed Radionuclides in Therapy- (1980-); 550601 - Medicine- Unsealed Radionuclides in Diagnostics; 400703 - Radiochemistry & Nuclear Chemistry- Radioisotope Production

Citation Formats

Knapp, Jr, F F, Ambrose, K R, Beets, A L, Callahan, A P, McPherson, D W, Mirzadeh, S, Hasan, A, and Lambert, C R. Nuclear medicine program progress report for quarter ending December 31, 1992. United States: N. p., 1993. Web. doi:10.2172/6567857.
Knapp, Jr, F F, Ambrose, K R, Beets, A L, Callahan, A P, McPherson, D W, Mirzadeh, S, Hasan, A, & Lambert, C R. Nuclear medicine program progress report for quarter ending December 31, 1992. United States. doi:10.2172/6567857.
Knapp, Jr, F F, Ambrose, K R, Beets, A L, Callahan, A P, McPherson, D W, Mirzadeh, S, Hasan, A, and Lambert, C R. Mon . "Nuclear medicine program progress report for quarter ending December 31, 1992". United States. doi:10.2172/6567857. https://www.osti.gov/servlets/purl/6567857.
@article{osti_6567857,
title = {Nuclear medicine program progress report for quarter ending December 31, 1992},
author = {Knapp, Jr, F F and Ambrose, K R and Beets, A L and Callahan, A P and McPherson, D W and Mirzadeh, S and Hasan, A and Lambert, C R},
abstractNote = {We describe the synthesis of the cis- and trans-iodovinyl isomers of the new ORNL cholinergic-muscarinicreceptorligand, 1 -azabicyclo[2.2-2]oct-3-yl[alpha]-hydroxy-[alpha]-(1-iodo-l-propen-3-yl)-[alpha]-phenylacetate ( IQNP''). This agent is prepared in high radiochemical yield, and the racemic mixture shows high specificity and selectivity for the cerebral and myocardial receptors. Since two chiral centers are present in this molecule, it is important to evaluate the importance of the absolute configuration of the two centers on receptor specificity. The tributyltin substrates were carefully separated by column chromatography, converted to the iodine-125 analogues by iododestannylation, and evaluated in rats in vivo. While the E'' (trans) isomer cleared rapidly from the receptor-rich areas of rat brain, the Z'' (cis) isomer showed high uptake in these areas but also high concentration in the cerebellum. In contrast, the E,Z-isomeric mixture showed good uptake and retention in the receptor rich areas. Also described in this report is a description of neutron flux measurements in the hydraulic tube position at the ORNL High Flux Isotope Reactor (HFIR). Also during this period, samples of [l-125]- and [l-131]-labeled racemic IQNP'' were supplied through a collaborative program with the Brookhaven National Laboratory for high resolution autoradiographic studies in rat tissues.},
doi = {10.2172/6567857},
journal = {},
number = ,
volume = ,
place = {United States},
year = {1993},
month = {3}
}