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Details for Patent: 5,922,303

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Details for Patent: 5,922,303

Title: Technetium-99M labeled peptides for imaging
Abstract:This invention relates to radiolabeled peptides and methods for producing such peptides. Specifically, the invention relates to peptides, methods and kits for making such peptides, and methods for using such peptides to image sites in a mammalian body labeled with technetium-99m (Tc-99m) via a radiolabel-binding moiety which forms a neutral complex with Tc-99m.
Inventor(s): Dean; Richard T. (Bedford, NH), Buttram; Scott (Derry, NH), McBride; William (Manchester, NH), Lister-James; John (Bedford, NH), Civitello; Edgar R. (Londonderry, NH)
Assignee: Diatide, Inc. (Londonderry, NH)
Filing Date:Jun 06, 1995
Application Number:08/468,964
Claims:1. A kit for preparing a radiopharmaceutical preparation, said kit comprising a sealed vial containing:

a) a predetermined quantity of a peptide reagent comprising a specific binding peptide covalently linked to a radiolabel-binding moiety, wherein the moiety forms an electrically neutral complex when complexed with a radioisotope; and

b) a sufficient amount of a reducing agent to label the reagent with technetium-99m.

2. The kit of claim 1, wherein the moiety is selected from the group consisting of: ##STR8## wherein X=H or a protecting group; (amino acid)=any amino acid; ##STR9## wherein X=H or a protecting group; (amino acid)=any amino acid; ##STR10## wherein each R is independently H, CH.sub.3 or C.sub.2 H.sub.5 ; each (pgp).sup.S is independently a thiol protecting group or H;

m, n and p are independently 2 or 3;

A=linear or cyclic lower alkyl, aryl, heterocyclyl, a combination thereof or a substituted derivative thereof; and ##STR11## wherein each R is independently H, CH.sub.3 or C.sub.2 H.sub.5 ; each (pgp).sup.S is independently a thiol protecting group or H;

m, n and p are independently 2 or 3;

A=linear or cyclic lower alkyl, aryl, heterocyclyl, a combination thereof or a substituted derivative thereof;

V=H or COOH;

R'=H or peptide

and wherein when V=H, R'=peptide and when R'=H, V=--CO--peptide.

3. The kit of claim 1, wherein the peptide is selected from the group consisting of:

formyl-MLF;

(VGVAPA).sub.3 amide;

(VPGVG).sub.4 amide;

RALVDTLKFVTQAEGAKamide (SEQ ID NO: 1);

RALVDTEFKVKQEAGAKamide (SEQ ID NO: 2);

PLARITLPDFRLPEIAIPamide (SEQ ID NO: 3);

GQQHHLGGAKAGDV (SEQ ID NO: 4);

PLYKKIIKKLLES (SEQ ID NO: 5);

LRALVDTLKamide (SEQ ID NO: 6);

GGGLRALVDTLKamide (SEQ ID NO: 7);

GGGLRALVDTLKFVTQAEGAKamide (SEQ ID NO: 8);

GGGRALVDTLKALVDTLamide (SEQ ID NO: 9);

GHRPLDKKREEAPSLRPAPPPISGGGYR (SEQ ID NO: 10);

PSPSPIHPAHHKRDRRQamide (SEQ ID NO: 11);

GGGF.sub.D.Cpa.YW.sub.D KTFTamide ##STR12## [[SYNRGDSTC(S-maleimido)CH.sub.2 CH.sub.2 -].sub.3 N] {SYNRGDSTC(S-maleimido)CH.sub.2 CH.sub.2 -}.sub.3 N;

GCGGGLRALVDTLKamide (SEQ ID NO: 13);

GCYRALVDTLKFVTQAEGAKamide (SEQ ID NO: 14); and

GC(VGVAPG).sub.3 amide.
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