A method for preparing a fluorine-18-labeled fluoromethyl-substituted radiopharmaceutical using a selective azide substitution reaction includes (1) obtaining a [.sup.18F]fluoride from a cyclotron through an .sup.18O(p,n).sup.18F reaction; (2) separating the [.sup.18F] fluoride using an acetonitrile reaction solution containing dissolved K.sub.2,2,2 and K.sub.2CO.sub.3 to obtain a [.sup.18F]F.sup./H.sub.2.sup.18O solution; (3) heating the [.sup.18F]F.sup./H.sub.2.sup.18O solution to obtain K.sub.2,2,2/K.sup.18F; (4) placing the K.sub.2,2,2/K.sup.18F along with a bis(tosyloxy)methane compound into a reactor and adding a reaction solvent to cause a reaction and obtain a first precursor solution; (5) cooling the first precursor solution and adding an azide reagent to cause an azide substitution reaction and obtain a [.sup.18F]fluoromethyltosylate compound; (6) adding a bioactive molecule to the [.sup.18F]fluoromethyltosylate compound to cause an alkylation reaction and obtain a second precursor solution; and (7) adding a precursor scavenger to the second precursor solution and scavenging unreacted precursors to produce a fluorine-18-labeled fluoromethyl-substituted radiopharmaceutical.

To develop a compound which is highly accumulated in cancer cells and capable of emitting an -ray and provide a pharmaceutical composition for cancer treatment including the compound.

A pharmaceutical composition for cancer treatment including a compound having a structure in which .sup.211At is introduced as a substituent into an amino acid derivative having an affinity with an amino acid transporter LAT1 or a pharmaceutically acceptable salt of the compound.

There is provided a diagnostic imaging agent for early bone metastasis from cancer, containing trans-1-amino-[.sup.18F]fluorocyclobutanecarboxylic acid or a pharmaceutically acceptable salt thereof as an active ingredient.

Systems and methods are disclosed for quantifying blood flow using time-varying kinetic modeling of high temporal-resolution dynamic positron emission tomography (PET) data. A single tracer is introduced into the body. A first set of images is acquired, via PET, of at least a portion of the body at a plurality of predetermined time intervals. Based on the first set of images, an intensity of the tracer in the at least the portion of the body is determined as a function of time. The intensity of the tracer as a function of time is modeled using a time-varying kinetic model. Based on the model, the blood flow through the at least the portion of the body is quantified. Additional images may be acquired and used to quantify additional parameter(s), such as glucose metabolism, amyloid load, etc., with the single tracer.

Methods, reporter gene constructs, and kits for using prostate-specific membrane antigen (PSMA) as an imaging reporter to image a variety of cells and tissues are provided.

The invention relates to products and methods that provide increased yields of certain radiopharmaceuticals.

The present disclosure provides compounds of formula: ##STR00001##
wherein R.sub.1, R.sub.2, and n are defined as set forth in the specification, and related aminobutanoic acids. The present disclosure also provides compositions comprising these compounds and methods for modulating ASCT2 function in a patient in need thereof.

It is intended to provide a novel amino acid organic compound which can be used as a labeling precursor compound for radioactive halogen-labeled amino acid compounds including [.sup.18F]FACBC, and which prevents methanol from remaining in the radioactive halogen-labeled amino acid compounds produced therefrom. The novel amino acid organic compound is a compound represented by the following formula:

##STR00001##

wherein n is an integer of 0 or of 1 to 4; R.sup.1 is an ethyl, 1-propyl or isopropyl substituent; X is a halogen substituent or a group represented by OR.sup.2; R.sup.2 is a straight-chain or branched-chain haloalkylsulfonic acid substituent with one to 10 carbon atoms, trialkylstannyl substituent with 3 to 12 carbon atoms, fluorosulfonic acid substituent or aromatic sulfonic acid substituent; and R.sup.3 is a protective group.

Accordingly, embodiments herein disclose a compound and method of small molecule inhibitors or ligands for diagnosis and treatment of cancers such as prostate, brain, breast, etc., and neurodegenerative diseases. A new class of PSMA inhibitors called as aminoacetamide, 1, has been designed by extensive in silico studies. A simple, mild and high yielding synthetic methodology is developed for 1 and shown to have high affinity for PSMA protein. Fluorescent conjugates 22 and 25 derived from 1 show selective uptake in prostate cancer cell lines and can be used for surgical removal of tumors during intra-operative surgery. Conjugates 31 and 34 for tagging 99mTc radioisotope were synthesized. Macrocyclic chelating cores such as DOTA, NOTA or prosthetic groups can be introduced to tag radionuclides 68Ga, 64Cu, 18F and 177Lu for diagnosis and treatment of PCa, incurable mCRPC and neurodegenerative diseases such as ALS, schizophrenia and neuropathic pain that over-express PSMA protein.

An object is to accurately calculate an index indicating a probability of an event occurring to a patient in the future. A mortality risk calculation unit acquires a heart/mediastinum ratio (H/M ratio), obtained by administering a heart function diagnostic medicine to a first subject, from subject data stored in a subject data storage unit, and calculates an index indicating a probability of a predetermined event occurring to the first subject by substituting the H/M ratio acquired from the subject data storage unit into a function defined in accordance with a history of occurrences of the predetermined event to a plurality of second subjects.