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Nuclear medicine program progress report for quarter ending December 31, 1992 [electronic resource]

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Bibliographic Details
Online Access: Online Access
Corporate Author: Oak Ridge National Laboratory (Researcher)
Format: Government Document Electronic eBook
Language:English
Published: Washington, D.C. : Oak Ridge, Tenn. : United States. Dept. of Energy ; distributed by the Office of Scientific and Technical Information, U.S. Dept. of Energy, 1993.
Subjects:
Organometallic Compounds.
Blood.
Nuclear Medicine.
Iodine 131.
Parasympathomimetics.
Progress Report.
Iodine 125.
Cerebral Cortex.
Heart.
Chemical Preparation.
Rats.
Labelling.
Cerebellum.
Tissue Distribution.
Autoradiography.
Tin Compounds.
Iodination.
Radiopharmaceuticals.
Radiology And Nuclear Medicine.
Description
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-ylα-hydroxy-α-(1-iodo-l-propen-3-yl)-α-phenylacetate (̀̀IQNP̀̀). 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 ̀̀È̀ (trans) isomer cleared rapidly from the receptor-rich areas of rat brain, the ̀̀Z̀̀ (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 ̀̀IQNP̀̀ were supplied through a collaborative program with the Brookhaven National Laboratory for high resolution autoradiographic studies in rat tissues.
Item Description:Published through the Information Bridge: DOE Scientific and Technical Information.
03/01/1993.
"ornl/tm--12312"
"DE93011789"
Lambert, C.R.; Knapp, F.F. Jr.; Hasan, A.; Ambrose, K.R.; Mirzadeh, S.; Callahan, A.P.; Beets, A.L.; McPherson, D.W.
Physical Description:11 p. : digital, PDF file.
Type of Report and Period Covered Note:Quarterly;

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