Abstract: A method of radiolabeling a protein with a radionuclide including contacting the protein with a protected tertiary thiol-containing bifunctional chelating agent that is capable of reacting with the protein at one end of the agent and is capable of complexing with a radionuclide at the other end of the agent, to form a protein-acetyl-t-thiol-containing conjugate. The protein-acetyl-t-thiol-containing conjugate then is deprotected and admixed with a reducing agent for the radionuclide, where the radionuclide is added in a subsequent step, to form a mixture of reducing agent and protein-t-thiol-containing conjugate. This mixture then is reacted with a radionuclide whereby the radionuclide reacts with pendant sulfhydryl groups present on the protein-t-thiol-containing conjugate. Methods of radioimmunotherapy and diagnostic kits suitable for forming a composition to be administered to a human patient also are disclosed.

Abstract: This invention provides novel radiopharmaceuticals which are useful as imaging agents for the diagnosis of cardiovascular disorders, infectious disease and cancer. The radiopharmaceuticals are comprised of phosphine or arsine ligated technetium-99m labeled hydrazino or diazino modified biologically active molecules that selectively localize at sites of disease and thus allow an image to be obtained of the loci using gamma scintigraphy. This invention also provides methods for using the radiopharmaceuticals and kits comprising radiopharmaceutical precursors. The radiopharmaceuticals of this invention have the structure:[(Q).sub.d 'L.sub.n -C.sub.h '].sub.x -M.sub.t (A.sub.L1).sub.y (A.sub.L2)z ;wherein the variables are as defined herein.

Abstract: This invention relates to radiotherapeutic reagents and peptides, radiodiagnostic reagents and peptides, and methods for producing labeled radiodiagnostic and radiotherapeutic agents. Specifically, the invention relates to vasoactive intestinal peptide receptor binding peptides, derivatives and analogues of vasoactive intestinal peptide, 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 vasoactive intestinal peptide receptor binding peptide derivatives and analogues of vasoactive intestinal peptide radiolabeled with technetium-99m and uses thereof as scintigraphic imaging agents. The invention also specifically relates to vasoactive intestinal peptide receptor binding peptide derivatives and analogues of vasoactive intestinal peptide radiolabeled with cytotoxic radioisotopes such as rhenium-186 (.sup.186 Re) and rhenium-188 (.

Abstract: A compound useful for in vivo imaging of organs and tumors is provided of formula: ##STR1## wherein ##STR2## is a cobalamin, ##STR3## is derived from a corrin carboxylic acid group of said cobalamin, Y is a linking group and X is a chelating group, optionally comprising a detectable radionuclide or a paramagnetic metal ion, and n is 1-3.

Abstract: The invention provides improved formulations of .sup.117m Sn (Sn.sup.4+) DTPA which allow higher doses of .sup.117m Sn (Sn.sup.4+) to be administered than were previously possible. Methods for making pharmaceutical compositions comprising .sup.117m Sn (Sn.sup.4+) DTPA in which the amount of unchelated DTPA is minimized are disclosed along with methods of using the improved formlulations, both for palliation of bone pain associated with cancer and for treatment of osseous tumors.

Abstract: Diamine compounds useful for treating neurodegenerated diseases characterized by the lack of dopamine neurons activity or for imaging the dopamine neurons are provided. The diamine compounds or serotonin are characterized by the formula: ##STR1## wherein: l, m and n can be the same or different and are an integer of 1 to 6; X, Y and Z can be the same or different and are hydrogen, halo, haloalkyl, (C.sub.1 -C.sub.6) alkyl, aryl, (C.sub.1 -C.sub.6) alkoxy, N-alkyl, (C.sub.2 -C.sub.6) acyloxy, N-alkylene, --SH, or --SR, wherein R is from the same group as R.sub.1 and R.sub.2 and can be the same or different than R.sub.1 and R.sub.2, amino, nitro, cyano, hydroxy, --C(.dbd.O) OR.sub.6, --C(.dbd.O) NR.sub.5 R.sub.4, NR.sub.3 R.sub.2, or S(.dbd.O).sub.k R.sub.1 wherein .sub.k is 1 or 2, and R.sub.4 to R.sub.6 are independently hydrogen or (C.sub.1 -C.sub.6) alkyl;R.sub.1, and R.sub.2 can be the same or different and are hydrogen, (C.sub.1 -C.sub.6) alkyl, hydroxyalkyl or mercaptoalkyl, --C(.dbd.O) OR.sub.

Abstract: A synth .sup.99m Tc complex which contains the moiety Tc.dbd.NR, Tc--N.dbd.NY or Tc(--N.dbd.NY).sub.2 and an organic ligand which confers biological target-seeking properties on the technetium complex, where R is an aryl group, a substituted or unsubstituted alkyl group or the group --NR.sup.1 R.sup.2 ; Y is an aryl group or a substituted or unsubstituted alkyl group; and R.sup.1 and R.sup.2 are H, aryl groups or substituted or unsubstituted aliphatic or cyclic alkyl groups, and are the same or different provided that both are not hydrogen. Radiopharmaceuticals comprising this complex are also described, together with methods for the preparation of the complex.

Abstract: The present invention provides a method of imaging amyloid deposits and radiolabeled compounds useful in imaging amyloid deposits. The invention also provides a method of delivering a therapeutic agent to amyloid deposits, a method of inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of determining a compound's ability to inhibit aggregation of amyloid proteins.

Abstract: The present invention provides the synthesis and purification of a new class of compounds known as radiolabeled fusion toxins (RFT), in which both toxin and radionuclide tags are contained on the same growth factor, for example, murine granulocyte macrophage colony stimulating factor, mGM-CSF, epidermal growth factor, or murine interleukin-4, mIL-4.

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 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 covalently attached to a specific binding peptide via an amino acid side-chain of the peptide.

Abstract: Constructs including bars, capsules, beads, and sheets are configured with a radionuclide core that emits energetic particles activating a phosphorescent shell material surrounding the radionuclide core so that it emits light to administer light therapy or PDT. A biocompatible coating that is generally optically transparent encloses the radionuclide core and phosphorescent material to prevent a patient's body in which the constructs are disposed from being affected by any toxicity of the phosphorescent shell material. In a typical application of the constructs, a photoreactive agent is infused into the treatment site and selectively absorbed by abnormal tissue, for example, in a cancerous tumor. Light emitted by the phosphorescent material when activated by the energetic particles emitted from the radionuclide core administers photodynamic therapy, which destroys the abnormal tissue.

Abstract: Novel metal chelating compounds, and radiometal, e.g., technetium-99m complexes thereof. The compounds can be used to radiolabel small biologically active species with minimal effect on their biodistribution and activity. The compounds have formula (a) or (b): ##STR1## where Z is (CR.sub.2).sub.n or (CR).sub.n, n is 2 or 3, X is a ligand comprising S, N or O, each R is H or C1-C20 substituted or unsubstituted hydrocarbon group, provided that 1-3 CR.sub.2 groups represent a CO (amide) moiety, and provided that 1-3 R may each comprise a targeting group and/or a protein reactive functionality.

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, rhenium-186, or rhenium-188 and which can be targeted to specific sites within a mammalian body.

Abstract: The invention relates to radio-pharmaceutical compositions that include an inclusion complex of a cyclodextrin and a radio-halogenated fatty acid.These complexes include a cyclodextrin such as .beta.-cyclodextrin, .gamma.-cyclodextrin and their derivatives, and a radio-halogenated fatty acid, in particular a fatty acid labelled with radioactive iodine such as 16-iodo 3-methyl hexadecanoic acid suitable for the examination of the myocardium by scintigraphy.The cyclodextrin allows the fatty acid to dissolve in aqueous solution without any addition of human blood albumin, while further improving the biodistribution of the fatty acid and its stability to heat.

Abstract: This invention relates to radiolabeled peptides and methods for producing such peptides. Specifically, the invention relates to technetium-99m (Tc-99m) labeled leukocyte-binding peptides, 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: The invention relates to radiotherapy with somatostatin-derived peptides labeled with medically useful metal ions. The invention in particular provides for methods and reagents for labeling somatostatin-derived peptides with perrhenate, in which a solution including somatostatin-derived peptide analogue containing at least one disulfide bond is provided, the solution is reacted with stannous ions and with a radioisotope, wherein the stannous ions are sufficient to substantially reduce the disulfide bonds of the peptide and the radioisotope, and the radiolabeled somatostatin-derived peptide analogue recovered. Also provided are methods for regional administration of radiolabeled somatostatin-derived peptides, methods for enhanced regional retention of radiolabeled somatostatin-derived peptides, methods for treatment of arthritis using radiolabeled somatostatin derived peptides, and methods for stabilizing radiolabeled somatostatin derived peptides.

Abstract: Method for detection of a biological material in a sample. The method includes the steps of liquifying the sample (if necessary) and pouring the liquified sample into the incubation plate. The incubation plate has a generally flat horizontal surface and the surface is divided into a plurality of at least 20 recessed wells. Each well is adapted to hold an aliquot of liquid and is sized and shaped, and formed of a suitable material, to hold the aliquot within the well by surface tension. Any excess liquid from the liquified sample is poured from the surface of the plate. The method then involves incubating that incubation plate until the presence or absence of the biological material is determined.

Abstract: The invention relates to novel magnetic resonance imaging contrast agents and methods of detecting physiological signals or substances.

Abstract: Compositions of radiolabeled nucleic acids and methods for synthesis and use thereof are disclosed.