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Design, synthesis and evaluation of 2-deoxy-2-iodovinyl-branched carbohydrates as potential brain imaging agents

Description: Radioiodinated carbohydrates such as 2-deoxy-2-iodo-D-glucose and 3-deoxy-3-iodo-D-glucose undergo facile chemical or in vivo deiodination which precludes their use as radiotracers of glucose metabolism in tissues. To overcome the problems resulting from in vivo deiodination, we explored the concept of stabilizing radioiodide on a model carbohydrate, (E)-C-3-iodovinyl-D-allose (10) as an iodovinyl moiety. This agent did not exhibit brain specificity but showed low in vivo deiodination which dem… more
Date: January 1, 1986
Creator: Goodman, M. M.; Callahan, A. P. & Knapp, F. F. Jr.
Partner: UNT Libraries Government Documents Department
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Telluro amino acids-synthesis, characterization and properties of a new and potentially useful class of compounds. [Chemical preparation of /sup 123 mm/Te-labeled amino acids for use in nuclear medicine]

Description: The Te-123m nuclide emits 159 keV photons suggesting that agents labeled with this nuclide would be attractive candidates for tissue imaging. Amino acids labeled with Te-123m are of particular interest since some of these compounds would be isosteric with the sulfur analogs and might behave similarly in vivo. Such agents could possibly be useful for pancreatic imaging and for other biomedical applications. The goal of this investigation was to develop a general chemical method for the preparati… more
Date: January 1, 1978
Creator: Knapp, Furn F., Jr.; Ambrose, K. R. & Callahan, A. P.
Partner: UNT Libraries Government Documents Department
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Production of tungsten-188 and osmium-194 in a nuclear reactor for new clinical generators

Description: Rhenium-188 and iridium-194 are potential candidates for radioimmunotherapy with monoclonal antibodies directed against tumor-associated antigens. Both nuclei are short-lived and decay by high energy {Beta}{minus} emission. In addition, both nuclei emit {gamma}-rays with energy suitable for imaging. An important characteristics is availability of {sup 188}Re and {sup 194}Ir from decay of reactor-produced parents ({sup 188}W and {sup 194}Os, respectively) in convenient generator systems. The {su… more
Date: January 1, 1991
Creator: Mirzadeh, S.; Knapp, F. F. Jr. & Callahan, A. P.
Partner: UNT Libraries Government Documents Department
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Production capabilities in US nuclear reactors for medical radioisotopes

Description: The availability of reactor-produced radioisotopes in the United States for use in medical research and nuclear medicine has traditionally depended on facilities which are an integral part of the US national laboratories and a few reactors at universities. One exception is the reactor in Sterling Forest, New York, originally operated as part of the Cintichem (Union Carbide) system, which is currently in the process of permanent shutdown. Since there are no industry-run reactors in the US, the n… more
Date: November 1, 1992
Creator: Mirzadeh, S.; Callahan, A. P.; Knapp, F. F. Jr. & Schenter, R. E.
Partner: UNT Libraries Government Documents Department
open access

Production capabilities in US nuclear reactors for medical radioisotopes

Description: The availability of reactor-produced radioisotopes in the United States for use in medical research and nuclear medicine has traditionally depended on facilities which are an integral part of the US national laboratories and a few reactors at universities. One exception is the reactor in Sterling Forest, New York, originally operated as part of the Cintichem (Union Carbide) system, which is currently in the process of permanent shutdown. Since there are no industry-run reactors in the US, the n… more
Date: November 1, 1992
Creator: Mirzadeh, S.; Callahan, A. P.; Knapp, F. F. Jr. & Schenter, R. E.
Partner: UNT Libraries Government Documents Department
open access

The development of new radionuclide generator systems for nuclear medicine applications

Description: Radioisotope generator systems have traditionally played a central role in nuclear medicine in providing radioisotopes for both research and clinical applications. In this paper, the development of several tungsten-188/rhenium-188 prototype generators which provide rhenium-188 for radioimmunotherapy (RAIT) is discussed. The authors have recently demonstrated that carrier-free iridium-194 can be obtained from the activated carbon system from decay of reactor-produced osmium-194 for potential RAI… more
Date: January 1, 1991
Creator: Knapp, F. F., Jr.; Callahan, A. P.; Mirzadeh, S.; Brihaye, C. & Guillaume, M.
Partner: UNT Libraries Government Documents Department
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High-level production of C-11-carboxyl-labeled amino acids. [For use in tumor and pancreatic imaging]

Description: Carbon-11-labeled amino acids have significant potential as agents for positron tomographic functional imaging. We have developed a rapid, high-temperature, high-pressure modification of the Buecherer--Strecker amino acid synthesis and found it to be quite general for the production of C-11-carboxyl-labeled neutral amino acids. Production of C-11-carboxyl-labeled DL-tryptophan requires certain modifications in the procedure. Twelve different amino acids have been produced to date by this techni… more
Date: January 1, 1979
Creator: Washburn, L. C.; Sun, T. T.; Byrd, B. L.; Hayes, R. L.; Butler, T. A. & Callahan, A. P.
Partner: UNT Libraries Government Documents Department
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Nuclear Medicine Program progress report for quarter ending March 31, 1993

Description: We have exploring the possibility of measuring urinary radioactivity as an index of pancreatic lipase activity after oral administration of a new triglyceride containing a radioactive iodine-1 25-labeled fatty acid moiety. The new agent, 1,2-dipalmitoyl-3[15-(p-iodophenyl)pentandecan-l-oyl]-racglycerol (1,2-Pal-3-IPPA), was prepared by the thallation-iodide displacement method. Following oral gavage of the radioiodinated triglyceride to rats, about 30% of the administered activity was excreted … more
Date: April 1, 1993
Creator: Knapp, F. F. Jr.; Ambrose, K. R.; Beets, A. L.; Callahan, A. P.; McPherson, D. W.; Mirzadeh, S. et al.
Partner: UNT Libraries Government Documents Department
open access

Nuclear Medicine Program progress report for quarter ending March 31, 1993

Description: We have exploring the possibility of measuring urinary radioactivity as an index of pancreatic lipase activity after oral administration of a new triglyceride containing a radioactive iodine-1 25-labeled fatty acid moiety. The new agent, 1,2-dipalmitoyl-3[15-(p-iodophenyl)pentandecan-l-oyl]-racglycerol (1,2-Pal-3-IPPA), was prepared by the thallation-iodide displacement method. Following oral gavage of the radioiodinated triglyceride to rats, about 30% of the administered activity was excreted … more
Date: April 1, 1993
Creator: Knapp, F. F. Jr.; Ambrose, K. R.; Beets, A. L.; Callahan, A. P.; McPherson, D. W.; Mirzadeh, S. et al.
Partner: UNT Libraries Government Documents Department
open access

Nuclear Medicine Program progress report for quarter ending September 30, 1992

Description: The radioiodination and in vivo evaluation of p-iodocaramiphen a muscarinic antagonist which binds with high affinity to the M[sub 1] receptor subtype in vitro are described. Biodistribution studies in female Fischer rats demonstrated that [[sup 125]I]-piodocaraminphen had significant cerebral localization, but the uptake did not demonstrate specific uptake in those cerebral regions rich in muscarinic receptors, and radioactivity washed out rapidly from the brain. In addition there was no signi… more
Date: December 1, 1992
Creator: Knapp, F. F., Jr.; Ambrose, K. R.; Beets, A. L.; Callahan, A. P.; McPherson, D. W.; Mirzadeh, S. et al.
Partner: UNT Libraries Government Documents Department
open access

Nuclear Medicine Program progress report for quarter ending September 30, 1992

Description: The radioiodination and in vivo evaluation of p-iodocaramiphen a muscarinic antagonist which binds with high affinity to the M{sub 1} receptor subtype in vitro are described. Biodistribution studies in female Fischer rats demonstrated that [{sup 125}I]-piodocaraminphen had significant cerebral localization, but the uptake did not demonstrate specific uptake in those cerebral regions rich in muscarinic receptors, and radioactivity washed out rapidly from the brain. In addition there was no signi… more
Date: December 1, 1992
Creator: Knapp, F. F. Jr.; Ambrose, K. R.; Beets, A. L.; Callahan, A. P.; McPherson, D. W.; Mirzadeh, S. et al.
Partner: UNT Libraries Government Documents Department
open access

Nuclear Medicine Program Progress Report for Quarter Ending December 31, 1992

Description: 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 absolut… more
Date: March 1993
Creator: Knapp, F. F., Jr.; Ambrose, K. R.; Beets, A. L.; Callahan, A. P.; McPherson, D. W.; Mirzadeh, S. et al.
Partner: UNT Libraries Government Documents Department
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Nuclear medicine program progress report for quarter ending December 31, 1993

Description: The results of preliminary in vivo metabolic studies of the iodine-125-labeled E-(R,R)-IQNP in rats are described. The E-(R,R) isomer demonstrates highly selective and specific localization in cerebral regions rich in the m{sub 1} and m{sub 4} muscarinic-cholinergic receptor subtypes and is a good candidate for potential human studies. Since the external evaluation of receptor-ligand complexes requires that only uptake of the unmetabolized agent is measured, these studies were performed to eval… more
Date: February 1, 1994
Creator: Knapp, F. F. Jr.; Ambrose, K. R.; Beets, A. L.; Callahan, A. P.; Luo, H.; McPherson, D. W. et al.
Partner: UNT Libraries Government Documents Department
open access

Nuclear Medicine Program progress report, quarter ending March 31, 1992

Description: We describe the design synthesis and initial animal testing of a new iodine-131-labeled triglyceride analogue for the potential evaluation of clinical pancreatic insufficiency. The new agent is 1,2-dipalmitoyl-3-[(15-p-iodophenyl)pentadecanoyl] rac-glycerol(1,2-Pal-3-IPPA). Following oral administration of the iodine-125-labeled agent to rats, 34.5+8.8% of the administered activity was excreted in the urine within one day, demonstrating that radioiodinated IPPA is absorbed in the intestine afte… more
Date: July 1, 1992
Creator: Knapp, F. F. Jr.; Ambrose, K. R.; Callahan, A. P.; McPherson, D. W.; Mirzadeh, S.; Hasan, A. et al.
Partner: UNT Libraries Government Documents Department
open access

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

Description: 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… more
Date: March 1, 1993
Creator: Knapp, F. F., Jr.; Ambrose, K. R.; Beets, A. L.; Callahan, A. P.; McPherson, D. W.; Mirzadeh, S. et al.
Partner: UNT Libraries Government Documents Department
open access

Nuclear Medicine Program progress report, quarter ending March 31, 1992

Description: We describe the design synthesis and initial animal testing of a new iodine-131-labeled triglyceride analogue for the potential evaluation of clinical pancreatic insufficiency. The new agent is 1,2-dipalmitoyl-3-((15-p-iodophenyl)pentadecanoyl) rac-glycerol(1,2-Pal-3-IPPA). Following oral administration of the iodine-125-labeled agent to rats, 34.5+8.8% of the administered activity was excreted in the urine within one day, demonstrating that radioiodinated IPPA is absorbed in the intestine afte… more
Date: July 1, 1992
Creator: Knapp, F. F. Jr.; Ambrose, K. R.; Callahan, A. P.; McPherson, D. W.; Mirzadeh, S.; Hasan, A. et al.
Partner: UNT Libraries Government Documents Department
open access

Nuclear Medicine Program progress report for quarter ending June 30, 1993

Description: The ``IQNP`` agent is an antagonist for the cholinergic-muscarinic receptor. Since the IQNP molecule has two asymmetric centers and either cis or trans isomerism of the vinyl iodide, there are eight possible isomeric combinations. In this report, the systematic synthesis, purification and animal testing of several isomers of radioiodinated ``IQNP`` are reported. A dramatic and unexpected relation between the absolute configuration at the two asymmetric centers and the stereochemistry of the vin… more
Date: July 1, 1993
Creator: Knapp, F. F. Jr.; Ambrose, K. R.; Beets, A. L.; Callahan, A. P.; Hsieh, B. T.; McPherson, D. W. et al.
Partner: UNT Libraries Government Documents Department
open access

Nuclear medicine program progress report for quarter ending December 31, 1991

Description: This report presents information on (1) a new improved synthesis of carrier-free rhenium-188-labeled Re(V) dimercaptosuccinic acid (DMSA) complex as a potential therapeutic agent for treatment of thyroid medullary carcinoma; and (2) the synthesis and evaluation of a series of iodine-125-labeled analogues of altanserine for imaging of serotonin receptors.
Date: April 1, 1992
Creator: Knapp, F. F., Jr.; Ambrose, K. R.; Callahan, A. P.; McPherson, D. W.; Mirzadeh, S.; Srivastava, P. C. et al.
Partner: UNT Libraries Government Documents Department
open access

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

Description: 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… more
Date: February 1, 1992
Creator: Knapp, F. F., Jr.; Ambrose, K. R.; Callahan, A. P.; McPherson, D. W.; Mirzadeh, S.; Srivastava, P. C. et al.
Partner: UNT Libraries Government Documents Department
open access

Nuclear medicine program progress report for quarter ending December 31, 1991

Description: This report presents information on (1) a new improved synthesis of carrier-free rhenium-188-labeled Re(V) dimercaptosuccinic acid (DMSA) complex as a potential therapeutic agent for treatment of thyroid medullary carcinoma; and (2) the synthesis and evaluation of a series of iodine-125-labeled analogues of altanserine for imaging of serotonin receptors.
Date: April 1, 1992
Creator: Knapp, F. F. Jr.; Ambrose, K. R.; Callahan, A. P.; McPherson, D. W.; Mirzadeh, S.; Srivastava, P. C. et al.
Partner: UNT Libraries Government Documents Department
open access

Nuclear Medicine Program Progress Report for Quarter Ending September 30, 1991

Description: 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 candida… more
Date: February 1, 1992
Creator: Knapp, F. F., Jr.; Ambrose, K. R.; Callahan, A. P.; McPherson, D. W.; Mirzadeh, S.; Srivastava, P. C. et al.
Partner: UNT Libraries Government Documents Department
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