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.

Abstract: A one vial method for labeling a sulfhydryl containing antibody or antibody fragment with technetium-99m is disclosed. The method comprises contacting an antibody mixture comprised of a sulfhydryl containing antibody or antibody fragment and a reducing agent with technetium-99m in an oxidized state. In a preferred embodiment, the antibody mixture further contains a water soluble ligand. A one vial kit for labeling a sulfhydryl containing antibody or antibody fragment with technetium-99m is also disclosed.

Abstract: This invention relates to radiolabeled scintigraphic imaging agents, and methods and reagents for producing such agents. Specifically, the invention relates to specific binding compounds, including peptides, that bind to a platelet receptor that is the platelet GPIIb/IIIa receptor, methods and kits for making such compounds, and methods for using such compounds labeled with technetium-99m via a covalently-linked radiolabel-binding moiety to image thrombi in a mammalian body.

Abstract: This invention relates to therapeutic reagents and peptides, radiodiagnostic reagents and peptides, and methods for producing label radiodiagnostic agents. Specifically, the invention relates to linear peptide derivatives and analogs of somatostatin, and embodiments of such peptides radiolabeled with a radioisotope, as well as methods and kits for making, radiolabeling and using such peptides for radiodiagnostic and radiotherapeutic purposes. The invention specifically relates to linear peptide derivatives and analogues of somatostatin radiolabeled with technetium-99m and uses thereof as scintigraphic imaging agents. The invention so specifically relates to liner peptide derivatives and analogues of somatostatin radiolabeled with cytotoxic radioisotopes such as rhenium-186 (.sup.186 Re) and rhenium-188 (.sup.188 Re) for use as radiotherapeutic agents. Methods and kits for making, radiolabeling and using such peptides diagnostically and therapeutically in a mammalian body are also provide.

Abstract: This invention relates to compositions that are radiolabeled scintigraphic imaging agents, comprising a polybasic compound covalently linked to a radiolabel binding moiety and the composition further comprising a polysulfated glycan. The invention also provides methods for producing and using such compositions. Specifically, the invention relates to compositions comprised of technetium-99m (Tc-99m) labeled scintigraphic imaging agents comprising a polybasic compound having at least 5 chemical functionalities that are basic at physiological pH and a radiolabel-binding moiety, the composition further comprising a polysulfated glycan, the composition being capable of specifically binding to inflammatory sites in vivo. Methods and kits for making such compositions, and methods for using such compositions to image sites of infection and inflammation in a mammalian body, are also provided.

Abstract: This invention relates to reagents, radiolabeled reagents and methods for producing such reagents and radiolabeled reagents. Specifically, the invention relates to technetium-99m (Tc-99m) labeled peptides that specifically bind to inflammatory sites in vivo, methods and kits for making such peptides, and methods for using such peptides to image sites of infection and inflammation in a mammalian body.

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 Tc-99m binding moieties. In particular, the peptide reagents of the invention are covalently linked to a polyvalent linker moiety, so that the polyvalent linker moiety is covalently linked to a multiplicity of the specific-binding peptides, and the Tc-99m binding moieties are covalently linked to a plurality of the specific-binding peptides, the polyvalent linker moiety, or to both the specific-binding peptides and the polyvalent linker moiety.

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 Tc-99m and which can be targeted to specific sites within a mammalian body.

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 specifically provides somatostatin, somatostatin derivatives, somatostatin analogues or peptides that bind to the somatostatin receptor and contain at least 2 cysteine residues that form a disulfide or wherein the disulfide is reduced to the sulfhydryl form that are labeled with technetium-99m and that can be targeted to specific sites within a mammalian body for imaging.

Abstract: Substantially nontoxic manganese or gadolinium complexes of compounds of the formula: ##STR1## wherein n and m=1, 2, 3 or 4, y=1, 2 or 3, and x is selected from the group consisting of S, CHOH and CHSH, are useful for enhancing magnetic resonance images of body organs and tissues. Illustrative manganese and gadolinium complexes of such compounds include disodium [[(2-hydroxytrimethylene)dinitrilo]tetraaceto]manganese(II) and sodium [[(2-hydroxytrimethylene)dinitrilo]tetraaceto)gadolinium(III).

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 specifically provides somatostatin, somatostatin derivatives, somatostatin analogues or peptides that bind to the somatostatin receptor and contain at least 2 cysteine residues that form a disulfide or wherein the disulfide is reduced to the sulfhydryl form that are directly labeled with technetium-99m and that can be targeted to specific sites within a mammalian body for imaging.

Abstract: A bifunctional coupling agent for joining a sulfhydryl-containing protein or peptide and a metallic radionuclide comprising a sulfhydryl selective electrophile, a chelator containing at least one protected thiol and a organic linking radical which serves to join said electrophile and said chelator is disclosed. A radiodiagnostic precursor comprising an antibody or antibody fragment and the specified bifunctional coupling agent bound to a sulfhydryl group on the antibody or antibody fragment is also disclosed.

Abstract: The present invention provides cross-linked protein compositions consisting of two or more units of a target-specific protein joined by binding sulfhydryl groups on the target-specific protein units to a sulfhydryl-selective cross-linking agent and a method of making the compositions. These cross-linked protein compositions combine an increase in binding affinity due to the presence of multiple identical binding sites and stability to reduction conditions.

Abstract: A one vial method for labeling a protein, such as an antibody or antibody fragment, with a radiometal such as Tc-99m or a rhenium isotope, is disclosed. The method comprises contacting in a single vial a mixture comprised of a reducing agent and a protein molecule covalently bound to a sulfhydryl containing bifunctional coupling agent with Tc or Re in an oxidized state. A one vial kit for labeling a protein with Tc or Re is also disclosed.

Abstract: Methods for rapidly labeling sulfhydryl-containing antibodies or fragments with technetium or rhenium radioisotopes are disclosed. The method generally involves combining an aqueous mixture of the radiometal in an oxidized form, a reducing agent and a water-soluble polyhydroxycarbonylic acid ligand to form a stable complex of the radiometal in its reduced state and contacting the mixture with the sulfhydryl-containing antibody or fragment to produce a radiometal-labeled antibody or fragment.

Abstract: Protein conjugates comprising a protein covalently linked to at least one positively charged agent, so that the protein conjugate has an overall net positive charge in aqueous conditions at physiological pH are disclosed. The positively charged agents comprise polymers of three or more subunits selected from the group consisting of amino acids containing positively charged side chains and alkylamines. These protein conjugates have decreased blood clearance rates compared to conjugates which do not have the positively charged agents. The protein conjugates may further comprise diagnostic or therapeutic radionuclides bound to the protein or the positively charged agent through bifunctional coupling agents.

Abstract: A bifunctional coupling agent for joining a sulfhydryl containing protein or peptide and a metallic radionuclide comprising a sulfhydryl selective electrophile, a chelator containing at least one protected thiol and a organic linking radical containing at least one cleavable site which serves to join said electrophile and said chelator is disclosed. A radiodiagnostic or radiotherapeutic precursor comprising an antibody or antibody fragment and the specified bifunctional coupling agent bound to a sulfhydryl group on the antibody or antibody fragment and a radiodiagnostic or radiotherapeutic agent comprising such precursor having a metallic radionuclide bound thereto are also disclosed.

Abstract: This invention relates to bifunctional coupling agents useful in forming conjugates with biologically useful molecules, such as antibodies. These conjugates can be complexed with radionuclide metal ions to provide materials useful for in vivo diagnostic and therapeutic applications.

Abstract: A bifunctional chelating agent for joining an antibody or antibody fragment and a metallic radionuclide is disclosed. The agent consists of a derivative of 1,4,7,10-tetraazacyclododecane-1,4,7-triacetic acid or a 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid, an organic linking radical which optionally contains a cleavable group, and a function capable of reacting with a site on a protein. Radiodiagnostic or radiotherapeutic precursors comprising an antibody or antibody fragment and the above-described bifunctional chelating agent and radiodiagnostic or radiotherapeutic agent comprising a metallic radionuclide and the above mentioned precursor are also disclosed.

Abstract: A simple, rapid and efficient method for labelling sulfhydryl-containing antibodies or antibody fragments with Tc-99m, Rh-186, Rh-188, Rh-189 or Rh-191 is disclosed. Labeled antibodies produced by the method are useful for radio-immunodiagnostic and/or radio-therapeutic purposes.