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Details for Patent: 5,968,476

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Details for Patent: 5,968,476

Title: Technetium-99m labeled peptides for thrombus imaging
Abstract:This invention relates to radiolabeled peptides and methods for producing such peptides. Specifically, the invention relates to specific binding peptides, methods and kits for making such peptides, and methods for using such peptides labeled with technetium-99m via a radiolabel-binding moiety covalently linked to the peptide to image thrombus sites in a mammalian body.
Inventor(s): Dean; Richard T. (Bedford, NH), Lister-James; John (Bedford, NH)
Assignee: Diatide, Inc. (Londonderry, NH)
Filing Date:Jun 07, 1995
Application Number:08/484,773
Claims:1. A complex for thrombus imaging comprising technetium-99m complexed with a reagent comprising a peptide having an amino acid sequence of from 4 to 100 amino acids and a technetium-99m binding moiety covalently linked to the peptide, wherein the peptide is selected from the group consisting of a linear peptide ligand for a GPIIb/IIIa receptor not comprising the amino acid sequence (arginine-glycine-asparate), a peptide ligand for a polymerization site of fibrin, and a cyclic peptide ligand for the GPIIb/IIIa receptor.

2. The complex of claim 1, formed by reacting the reagent with the technetium-99m in the presence of a reducing agent.

3. The complex of claim 2, wherein the reducing agent is selected from the group consisting of a dithionite ion, a stannous ion and a ferrous ion.

4. The complex of claim 1, formed by labeling the reagent with the technetium-99m by ligand exchange of a prereduced technetium-99m complex.

5. A method of labeling the reagent of claim 1, comprising the step of reacting the reagent with technetium-99m in the presence of a reducing agent.

6. The method of claim 5, wherein the reducing agent is selected from the group consisting of a dithionite ion, a stannous ion and a ferrous ion.

7. The complex of claim 1, wherein the peptide is a peptide ligand for a polymerization site of fibrin comprising multiple copies of the sequence (glycyl-prolyl-arginyl-prolyl).

8. The complex of claim 1, wherein the peptide comprises one of the following amino acid sequences:

(GPRPC.sub.Acm GC.sub.Acm C(S-maleimido)CH.sub.2 CH.sub.2 --).sub.3 N,

((GPRP).sub.2 K, or

(GPRVVERHQSA).sub.2 K.

9. The complex of claim 1, wherein the peptide comprises one of the following amino acid sequences: ##STR17##
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