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Radiolabeled technetium chelates for use in renal function determinations

Patent ·
OSTI ID:869364
 [1];  [2];  [3]
  1. Edmonds, WA
  2. Kirkland, WA
  3. Las Cruces, NM
+ Show Author Affiliations

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.

Research Organization:
UNIVERSITY OF UTAH
DOE Contract Number:
AC02-83ER60140
Assignee:
University of Utah Research Foundation (Salt Lake City, UT)
Patent Number(s):
US 5322929
OSTI ID:
869364
Country of Publication:
United States
Language:
English

References (6)

Tissue distribution properties of technetium-99m-diamide-dimercaptide complexes and potential use as renal radiopharmaceuticals journal October 1986
Solution equilibria of copper(II) and nickel(II) complexes of glycyl peptide amides journal June 1975
Evaluation of the renal excretion characteristics of technetium-99m mercaptoacetylglycyl-D-alanylglycine in healthy volunteers journal April 1992
Reductive Deamination of Oligopeptides by Solvated Electrons in Aqueous Solution journal November 1971
Newly synthesized sulfhydryl- and imidazole-containing tripeptides with a specific copper-binding site journal August 1978
The reaction of trans-cinnamoyl-papain with a series of polyglycinamides of varying chain length journal April 1967

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