Abstract A new series of technetium chelating agents based on amide and mercaptide donor groups is described, exemplified by 2,3-bis(mercaptoacetamido)propanoic acid. Chelation of Tc-99 m with 2,3-bis(mercaptoacetamido)propanoic acid resulted in two components that were separable by high-performance liquid chromatography. The component that eluted first demonstrated high specificity for renal excretion with over 90% in the urine in rabbits at 35 minutes and 87% in the urine of mice at 2 hours and 1.6% or less in the intestines of mice. Excretion was rapid with the first component equal to or greater than I-131 Hippuran in the urine of rabbits at all times. The second or latter component demonstrated comparable specificity, but slower renal excretion kinetics. 2,3-Bis-(mercaptoacetamido)succinic acid forms similar chelates with technetium which are also useful as radiopharmaceuticals for the renal systems of mammals.
A compound of the formula ##STR4## wherein X is carboxyl or hydrogen, R and R' are hydrogen or lower alkyl and the Tc is Tc-99m, and water-soluble salts thereof.
Claim 2
Dependent Claim
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A compound of the formula ##STR4## wherein X is carboxyl or hydrogen, R and R' are hydrogen or lower alkyl and the Tc is Tc-99m, and water-soluble salts thereof.
Claim 3
Dependent Claim
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A compound according to claim 1 wherein R is hydrogen.
Claim 4
Dependent Claim
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A compound according to claim 1 wherein X is carboxyl.
Claim 5
Dependent Claim
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A compound according to claim 1 wherein X is hydrogen.
Claim 6
Dependent Claim
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A compound according to claim 1 wherein R' is hydrogen.
Claim 7
Dependent Claim
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A compound according to claim 1 wherein R and R' are hydrogen.
Claim 8
Dependent Claim
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A compound according to claim 1 wherein R and R' are lower alkyl.
Claim 9
Dependent Claim
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A compound according to claim 1 wherein R' is hydrogen and R is lower alkyl.