Radiolabeled technetium chelates for use in renal function determinations
Abstract
The present invention is directed to novel radiopharmaceutical imaging agents incorporating Tc-99m as a radiolabel. In particular, the novel imaging agents disclosed herein have relatively high renal extraction efficiencies, and hence are useful for conducting renal function imaging procedures. The novel Tc-99m compounds of a present invention have the following general formula: ##STR1## wherein X is S or N; and wherein Y is --H or wherein Y is ##STR2## and where R.sub.1 is --H, --CH.sub.3, or --CH.sub.2 CH.sub.3 ; R.sub.2 is --H, --CH.sub.2 CO.sub.2 H, --CH.sub.2 CONH.sub.2, --CH.sub.2 CH.sub.2 CO.sub.2 H, --CH.sub.2 CH.sub.2 CONH.sub.2, --CH.sub.3, --CH.sub.2 CH.sub.3, CH.sub.2 C.sub.6 H.sub.5, or --CH.sub.2 OH; and Z is --H, --CO.sub.2 H, --CONH.sub.2, --SO.sub.3 H, --SO.sub.2 NH.sub.2, or --CONHCH.sub.2 CO.sub.2 H; and the Tc is Tc-99m; and water-soluble salts thereof. Of the foregoing, the presently preferred Tc-99m compound of the present invention is Tc-99m-mercaptoacetylglycylglycylglycine (Tc-99m-MAGGG). The present invention is also directed to novel chelating agents that may be reacted with Tc-99m to form the foregoing compounds. Such novel chelating agents have the following general formula. ##STR3## where X and Y have the same definitions as above, and wherein Y' is --H.sub.2 when X is N, or wherein Y' is --H, or a suitablemore »
- Inventors:
-
- Edmonds, WA
- Kirkland, WA
- Las Cruces, NM
- Issue Date:
- Research Org.:
- Univ. of Utah, Salt Lake City, UT (United States)
- OSTI Identifier:
- 869364
- Patent Number(s):
- 5322929
- Assignee:
- University of Utah Research Foundation (Salt Lake City, UT)
- Patent Classifications (CPCs):
-
A - HUMAN NECESSITIES A61 - MEDICAL OR VETERINARY SCIENCE A61K - PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
C - CHEMISTRY C07 - ORGANIC CHEMISTRY C07C - ACYCLIC OR CARBOCYCLIC COMPOUNDS
- DOE Contract Number:
- AC02-83ER60140
- Resource Type:
- Patent
- Country of Publication:
- United States
- Language:
- English
- Subject:
- radiolabeled; technetium; chelates; renal; function; determinations; directed; novel; radiopharmaceutical; imaging; agents; incorporating; tc-99m; radiolabel; particular; disclosed; relatively; extraction; efficiencies; hence; useful; conducting; procedures; compounds; following; formula; str1; -h; str2; -ch; conh; oh; z; -co; -conh; -so; nh; -conhch; tc; water-soluble; salts; foregoing; presently; preferred; compound; tc-99m-mercaptoacetylglycylglycylglycine; tc-99m-maggg; chelating; reacted; form; str3; definitions; suitable; protective; -coch; -coc; nhcoch; -cocf; provides; methods; preparing; soluble salts; provides methods; imaging agents; chelating agents; chelating agent; soluble salt; radiopharmaceutical imaging; renal function; extraction efficiencies; imaging agent; agents disclosed; radiolabeled technetium; novel radiopharmaceutical; novel imaging; technetium chelates; function determinations; incorporating tc-99m; agents incorporating; /530/
Citation Formats
Fritzberg, Alan, Kasina, Sudhaker, and Johnson, Dennis L. Radiolabeled technetium chelates for use in renal function determinations. United States: N. p., 1994.
Web.
Fritzberg, Alan, Kasina, Sudhaker, & Johnson, Dennis L. Radiolabeled technetium chelates for use in renal function determinations. United States.
Fritzberg, Alan, Kasina, Sudhaker, and Johnson, Dennis L. Sat .
"Radiolabeled technetium chelates for use in renal function determinations". United States. https://www.osti.gov/servlets/purl/869364.
@article{osti_869364,
title = {Radiolabeled technetium chelates for use in renal function determinations},
author = {Fritzberg, Alan and Kasina, Sudhaker and Johnson, Dennis L},
abstractNote = {The present invention is directed to novel radiopharmaceutical imaging agents incorporating Tc-99m as a radiolabel. In particular, the novel imaging agents disclosed herein have relatively high renal extraction efficiencies, and hence are useful for conducting renal function imaging procedures. The novel Tc-99m compounds of a present invention have the following general formula: ##STR1## wherein X is S or N; and wherein Y is --H or wherein Y is ##STR2## and where R.sub.1 is --H, --CH.sub.3, or --CH.sub.2 CH.sub.3 ; R.sub.2 is --H, --CH.sub.2 CO.sub.2 H, --CH.sub.2 CONH.sub.2, --CH.sub.2 CH.sub.2 CO.sub.2 H, --CH.sub.2 CH.sub.2 CONH.sub.2, --CH.sub.3, --CH.sub.2 CH.sub.3, CH.sub.2 C.sub.6 H.sub.5, or --CH.sub.2 OH; and Z is --H, --CO.sub.2 H, --CONH.sub.2, --SO.sub.3 H, --SO.sub.2 NH.sub.2, or --CONHCH.sub.2 CO.sub.2 H; and the Tc is Tc-99m; and water-soluble salts thereof. Of the foregoing, the presently preferred Tc-99m compound of the present invention is Tc-99m-mercaptoacetylglycylglycylglycine (Tc-99m-MAGGG). The present invention is also directed to novel chelating agents that may be reacted with Tc-99m to form the foregoing compounds. Such novel chelating agents have the following general formula. ##STR3## where X and Y have the same definitions as above, and wherein Y' is --H.sub.2 when X is N, or wherein Y' is --H, or a suitable protective group such as --COCH.sub.3, --COC.sub.6 H.sub.5, --CH.sub.2 NHCOCH.sub.3, --COCF.sub.3, or --COCH.sub.2 OH when X is S. The present invention also provides methods for preparing and using the novel Tc-99m compounds.},
doi = {},
journal = {},
number = ,
volume = ,
place = {United States},
year = {1994},
month = {1}
}
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