Radiolabeled technetium chelates for use in renal function determinations

Patent · Mon Jan 01 00:00:00 EST 1990

OSTI ID:867659

Fritzberg, Alan ^[1]; Kasina, Sudhakar ^[2]; Johnson, Dennis L ^[3]

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1. Edmonds, WA
2. Kirkland, WA
3. Las Cruces, NM

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: Univ. of Utah, Salt Lake City, UT (United States)
• DOE Contract Number: AC02-83ER60140
• Assignee: University of Utah Research Foundation (Salt Lake City, UT)
• Patent Number(s): US 4980147
• OSTI ID: 867659
• Country of Publication: United States
• Language: English

Related Subjects

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/