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 suitable protectivemore »
- Inventors:
-
- Edmonds, WA
- Kirkland, WA
- Las Cruces, NM
- Publication Date:
- Research Org.:
- Univ. of Utah, Salt Lake City, UT (United States)
- OSTI Identifier:
- 867659
- Patent Number(s):
- US 4980147
- Assignee:
- University of Utah Research Foundation (Salt Lake City, UT)
- 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; is-h; str2; -h; -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; /424/999/
Citation Formats
Fritzberg, Alan, Kasina, Sudhakar, and Johnson, Dennis L. Radiolabeled technetium chelates for use in renal function determinations. United States: N. p., 1990.
Web.
Fritzberg, Alan, Kasina, Sudhakar, & Johnson, Dennis L. Radiolabeled technetium chelates for use in renal function determinations. United States.
Fritzberg, Alan, Kasina, Sudhakar, and Johnson, Dennis L. 1990.
"Radiolabeled technetium chelates for use in renal function determinations". United States. https://www.osti.gov/servlets/purl/867659.
@article{osti_867659,
title = {Radiolabeled technetium chelates for use in renal function determinations},
author = {Fritzberg, Alan and Kasina, Sudhakar 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 = {},
url = {https://www.osti.gov/biblio/867659},
journal = {},
number = ,
volume = ,
place = {United States},
year = {Mon Jan 01 00:00:00 EST 1990},
month = {Mon Jan 01 00:00:00 EST 1990}
}