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Details for Patent: 5,681,541

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Details for Patent: 5,681,541

Title: Technetium-99m labeled radiopharmaceutical kit for imaging
Abstract:The invention relates to radiolabeled imaging of a mammalian body. The invention in particular provides for reagents labeled with technetium-99m for such imaging. The invention provides peptides which bind technetium-99m and which can be targeted to specific sites within a mammalian body.
Inventor(s): Dean; Richard T. (Bedford, NH)
Assignee: Diatide, Inc. (Londonderry, NH)
Filing Date:Jun 05, 1995
Application Number:08/464,456
Claims:1. A kit for preparing a radiopharmaceutical that is a scintigraphic imaging agent for imaging target sites within a mammalian body, said kit comprising a sealed vial containing a predetermined quantity of a reagent for preparing the scintigraphic imaging agent, wherein the reagent comprises, in combination:

(a) a specific binding peptide comprising 3 to 100 amino acids that specifically binds to the target site to be imaged and

(b) a technetium-99 m binding moiety of the formula

wherein Cp is a cysteine amino acid residue and (aa) is any amino acid and wherein the technetium-99 m binding moiety is covalently bound to the specific binding peptide to comprise the reagent, and a sufficient amount of reducing agent to label said reagent with technetium-99 m.

2. A kit according to claim 1 wherein the reagent comprises a specific binding peptide and a Cp(aa)Cp moiety that are covalently linked through from about one to about ninety amino acids.

3. A kit according to claim 1 wherein the reagent comprises a technetium-99 m binding moiety wherein the sidechain sulfur atom of the cysteine residue of the technetium-99 m binding moiety is protested by a protecting group of the formula

wherein R is a lower alkyl having 1 to 6 carbon atoms, phenyl, or phenyl substituted with lower alkyl, hydroxy, lower alkoxy, carboxy, or lower alkoxycarbonyl, or 2-,3-,4- pyridyl.

4. A kit according to claim 1 wherein the reagent comprises a technetium-99 m binding moiety having the formula: ##STR8##

5. A kit according to claim 1 wherein the reagent comprises a specific binding peptide selected from the group consisting of peptides having the formula:
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