Multifunctional chelators, metal complexes thereof, compositions thereof, and methods of making and use in diagnostic imaging and treatment of cellular disorders.

The present invention provides a novel radioactive compound for imaging malignant melanoma and a use thereof as a contrast agent for PET imaging.

The present application provides quinoline-3-carboxamide compounds covalently linked to a label for use in the diagnosis of an inflammatory disease at local site. The above mentioned compounds can be used to detect or image accumulation of S100A9 in the body of a subject at sites of inflammation, using in vivo non-invasive molecular imaging techniques for the detection of said compounds. Accordingly, labeled quinoline-3-carboxamide compounds can be applied to evaluate the risk of a subject of developing an inflammatory disease and to follow the progress of the disease.

Dual-modality contrast agents are disclosed herein, having the general formula:

##STR00001## R.sub.1 includes a chelating moiety that is chelated to a Mn.sup.2+ isotope. The disclosed contrast agents differentially target a wide range of malignant tumor tissues, and can be simultaneously used as contrast agents for both magnetic resonance imaging (MRI) and positron emission topography (PET) imaging. Accordingly, the disclosed contrast agent can be used in diagnosing and monitoring solid tumor cancers.

The invention discloses non-iodinated radiopaque microbeads that may be used in image guided embolization in a subject ailing with tumor. The non-iodinated radiopaque microbeads include a ceramic material doped with a CT contrast agent or a MRI contrast agent or both. The doped ceramic is blended with a polymer and the blend is electrosprayed to form the radiopaque microbeads. Further the radiopaque microbeads are radiolabeled with a radioactive isotope. Methods of synthesis of the radiopaque microspheres are also disclosed. The non-iodinated radiopaque microbeads with radiolabeling are capable of rendering an imageable computed tomography (CT) contrast or magnetic resonance imaging (MRI) contrast when administered in a subject. Also the microspheres are biodegradable and hence the treatment could be repeated in case of recurrence of the tumor in the subject.

Methods for detecting the presence and/or assessing the severity of myocardial ischemia during pharmacologic stress tests by administration of a pharmaceutical composition comprising adenosine and dipyridamole are described. The methods allow for the combined administration of dipyridamole administered as a bolus with adenosine given as an infusion, where the dosages of each of these compounds are below their respective dosages when the compounds are used as a single agent. The methods are useful for exploiting the vasodilating abilities of adenosine at doses at which side effects related to adenosine are substantially reduced while optimal coronary artery perfusion is achieved. Also presented, are compositions, unit dosage forms, and kits that are useful in performing the methods.

Provided herein are radiolabelled compounds useful for imaging GSK-3 kinase. An exemplary radiolabelled compound provided herein is useful as a radiotracer for imaging GSK-3 kinase using PET imaging. Methods for preparing the radiolabelled compounds and diagnostic methods using the radiolabelled compounds are also provided.

A system, and method, for quantitatively mapping of mitochondrial membrane potential of a tissue in a subject is provided. In some aspects, the provided method includes administering to the subject a detectably effective amount of a tracer as an emission tomography imaging agent; acquiring, using an emission tomography system, emission tomography data associated with the tissue; analyzing the emission tomography data to determine a concentration distribution of the tracer within the tissue; correlating the concentration distribution of the tracer with the membrane potential of the tissue; determining, using the correlating step, a membrane potential distribution of the tissue; and generating a report indicating the membrane potential distribution of the tissue.

The present invention relates to a compound, etc. capable of providing a radiolabeled drug that can reduce the renal accumulation thereof in the early stage after the administration thereof. [1] A compound, etc. represented by the formula (1), [2] a compound, etc. containing the compound, etc. according to the item [1] and a target molecule recognition element bonded thereto, [3] a metal complex compound, etc. containing one kind of a metal selected from a radioactive metal and a radioactive atom-labeled metal, and the compound, etc. according to the item [1] or [2], which is coordinated to the metal, [4] a drug for preparing a radiolabeled drug, containing the compound, etc. according to the item [1] or [2], [5] use of the compound, etc. according to the item [1] or [2], for producing a radiolabeled drug, [6] a radiolabeled drug containing the metal complex compound, etc. according to the item [3], and [7] a radiodiagnostic imaging agent containing the metal complex compound, etc. according to the item [3]:

##STR00001##

The present invention provides a method for the purification of .sup.227Th from a mixture comprising .sup.227Th and .sup.223Ra, said method comprising: i) preparing a first solution comprising a mixture of .sup.227Th and .sup.223Ra ions dissolved in an aqueous solution of first mineral acid; ii) loading said first solution onto a strong base anion exchange resin; iii) eluting .sup.223Ra from said strong base anion exchange resin using a second mineral acid in an aqueous solution; iv) optionally rinsing said strong base anion exchange resin using a first aqueous medium; v) eluting .sup.227Th from said strong base anion exchange resin using a third mineral acid in an aqueous solution whereby to generate a second solution comprising .sup.227Th. The invention further provides a purified .sup.227Th solution, a corresponding pharmaceutical formulation and methods of treatment of neoplastic disease.