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Title: 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 » 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.« less

Inventors:
 [1];  [2];  [3]
  1. Edmonds, WA
  2. Kirkland, WA
  3. 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}
}