Abstract: A process is provided for producing a labeled precursor which is useful for production of a radioactive fluorine-labeled amino acid compound. In the reaction step for introducing a leaving group to a mixture of syn-form and anti-form of FACBC, a base is allowed to present in the reaction system to produce a syn-leaving group adduct, which is unreactive with the base and is highly stable, and an anti-leaving group adduct which can react with the base to form a water-soluble compound. By employing a purification method utilizing such a difference in solubility, the syn-leaving group adduct can be separated selectively. The base may be a linear- or branched-chain primary to tertiary alkylamine having 1 to 10 carbon atoms, a nitrogen-containing heterocyclic compound with 2 to 20 carbon atoms, and a nitrogen-containing hetero aromatic compound with 2 to 20 carbon atoms.

Abstract: A method of detecting a neurodegenerative disease includes (a) a standardization step of creating a first image by applying anatomical standardization to a brain nuclear medical image; (b) a conversion step of creating a second image by converting the pixel value of each pixel of an image based on the first image into a z score or a t value; (c) an addition step of calculating the sum of the pixel values of individual pixels in a predetermined region of interest in the second image; and (d) a detection step of obtaining the results of the detection of the neurodegenerative disease through an operation of comparison of the sum with a predetermined threshold.

Abstract: A process for the production of [18F]-TAFDG can produce [18F]-TAFDG in a high radiofluorination yield. A process for the production of an organic compound labeled with radioactive fluorine includes the steps of preparing a reaction solution containing [18F]fluoride ions, a phase transfer catalyst, potassium ions, 1,3,4,6-tetra-O-acetyl-2-O-trifluoromethanesulfonyl-?-D-mannopyranose as a labeling precursor compound and a solvent, and giving a reaction condition to the reaction solution to obtain 1,3,4,6-tetra-O-acetyl-2-[18F]fluoro-2-deoxyglucose, in which the solvent contains water.

Abstract: A compound represented by the following formula or a salt thereof: wherein each of A1, A2, A3 and A4 independently represents a carbon or nitrogen; R1 is a group selected from the group consisting of hydrogen, hydroxyl group, carboxyl group, sulfuric acid group, amino group, nitro group, cyano group, non-radioactive halogen substituents, alkyl substituents with 1-4 carbon atoms and alkoxy substituents with 1-4 carbon atoms; and R2 is a radioactive halogen substituent, provided at least one of A1, A2, A3 and A4 represents a carbon, and R1 binds to a carbon represented by A1, A2, A3 or A4, is effective as an image diagnosis probe targeting amyloid and as well as a diagnostic agent for Alzheimer's disease including the compound represented by the above formula or a salt thereof.

Abstract: The present invention provides a compound which has affinity with amyloid, shows sufficiently rapid clearance from normal tissues and is suppressed in toxicity such as mutagencity. Provided is a compound represented by the following formula (1) or a salt thereof: wherein A1, A2, A3 and A4 independently represents a carbon or nitrogen; R1 is a halogen substituent; R2 is a halogen substituent; and m is an integer of 0 to 2, provided that at least one of R1 and R2 is a radioactive halogen substituent, at least one of A1, A2, A3 and A4 represents a carbon, and R1 binds to a carbon represented by A1, A2, A3 or A4 as well as a low-toxic diagnostic agent comprising a compound represented by the preceding formula or a salt thereof.

Abstract: A process is provided for producing [18F]FACBC, which can reduce the production amount of impurities.

Abstract: An image processing method is provided as one for creating a fused image automatically and with high overlapping accuracy. An image processing method according to an embodiment of the present invention includes (a) a voxel normalization step of equalizing voxel sizes and numbers of voxels in respective effective fields of view of a first 3D image based on a plurality of first tomographic images obtained from an arbitrary part of a subject and a second 3D image based on a plurality of second tomographic images obtained from the same part, thereby creating a first normalized 3D image corresponding to the first 3D image and a second normalized 3D image corresponding to the second 3D image; and (b) a fused image creation step of creating a fused image, using the first normalized 3D image and the second normalized 3D image.

Abstract: It is intended to provide a labeling precursor compound used for selectively producing radioactive halogen-substituted syn-1-amino-3-cyclobutane-carboxylic acids, and to provide a process for producing a radioactive halogen-substituted syn-1-amino-3-cyclobutane-carboxylic acid using the labeling precursor compound. A labeling precursor is used in which a phthalimide group is used as a protective group for protecting the amino group. The syn-form of the radioactive halogen-substituted 1-amino-3-cyclobutane-carboxylic acid can be selectively produced by labeling the labeling precursor with a radioactive halogen followed by deprotecting.

Abstract: A process for the production of [18F]fluoro-2-deoxyglucose can produce [18F]fluoro-2-deoxyglucose in a high and stable yield of synthesis. A process for the production of a compound labeled with radioactive fluorine includes the preparing a reaction solution by adding, under a hermetic condition, TATM and an inert organic solvent to a mixture containing [18F]fluoride ions, a phase transfer catalyst and potassium ions, giving a reaction condition to the reaction solution under a hermetic condition to obtain [18F]-TAFDG, and subjecting the obtained [18F]fluoro-2-deoxyglucose to a deprotection process and, optionally, to a purification process to obtain [18F]fluoro-2-deoxyglucose.

Abstract: 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 [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: wherein n is an integer of 0 or of 1 to 4; R1 is an ethyl, 1-propyl or isopropyl substituent; X is a halogen substituent or a group represented by —OR2; R2 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 R3 is a protective group.

Abstract: A radiopharmaceutical for diagnostic imaging containing as an active ingredient a technetium-99m nitride heterocomplex comprising technetium-99m nitride and two different ligands coordinated therewith, i.e., a bisphosphinoamine compound as a ? electron acceptor and a bidentate ligand as a ? electron donor and represented by the following formula (I): [99mTc(N)(PNP)(XY)]+ (I)wherein 99mTc(N) is technetium-99m nitride, PNP is a bisphosphinoamine compound and XY is a bidentate ligand, is markedly accumulated in heart and adrenal glands and hence is useful for radiodiagnostic imaging of heart and adrenal glands.

Abstract: A process for diagnostic imaging of heart or adrenal glands of a human being comprises administering to the human being a radiopharmaceutical containing as an active ingredient a technetium-99m nitride heterocomplex comprising technetium-99m nitride and two different ligands coordinated therewith, i.e., a bisphosphinoamine compound and a bidentate ligand and represented by the formula (1): [99mTc(N)(PNP)(XY)]+. In this formula, 99mTc(N) is technetium-99m nitride, PNP is a bisphosphinoamine compound and XY is a bidentate ligand as described in the specification. The compound of the formula is markedly accumulated in heart and adrenal glands and hence is used for radiodiagnostic imaging of heart and adrenal glands.

Abstract: It is intended to provide a radioactive diagnostic imaging agent comprising a radioactive halogen-labeled compound as an active ingredient, in which the active ingredient is prevented from radiolysis and its stability is improved. This is achieved by adding a biologically-acceptable sugar or sugar alcohol to the radioactive diagnostic imaging agent in an amount effective to prevent radiolysis. The amount of the sugar or sugar alcohol to be added is preferably 10 (mmol/L)/GBq/mL or more, and more preferably 50 (mmol/L)/GBq/mL or more. The sugar is preferably selected from the group consisting of erythrose, threose, ribose, arabinose, xylose, lyxose, allose, altrose, glucose, mannose, gulose, idose, galactose, talose, erythrulose, ribulose, xylulose, psicose, fructose, sorbose, and tagatose. The sugar alcohol is preferably selected from the group consisting of erythritol, xylitol, sorbitol, and mannitol.

Abstract: By preliminarily dissolving a basic organic compound in an aqueous solvent in which a peptide usable in metal-labeling is to be dissolved, the solubility of the peptide is improved and thus metal-labeling can be carried out without heating. A composition for medical use containing a peptide usable in metal-labeling and a basic organic compound acceptable as a pharmaceutical additive can be utilized as a preparation useful in image diagnosis, radiotherapy and so on.

Abstract: The image correction method according to an embodiment of the present invention includes the steps of: (a) generating an absorption correction map by replacing a CT value of each pixel of a CT image with a corresponding linear absorption coefficient and replacing the linear absorption coefficient in a bone region with the linear absorption coefficient of water or a soft biological tissue; and (b) generating a corrected image by multiplying a value of each pixel of a nuclear medical image obtained with respect to substantially the same tomographic plane as a plane in which the CT image has been obtained by a corresponding pixel of the absorption correction map.

Abstract: A compound that comprises Met-Leu-Phe or Nle-Leu-Phe serving as the leukocyte-binding site of a formyl peptide receptor (FPR), a binding part comprising Ser or Thr that increases the binding ratio to monocytes and lymphocytes in all leukocytes, a group that can be labeled with a radioactive metal or a paramagnetic metal, and spacers binding the three moieties together shows binding properties specific to all leukocytes, i.e., neutrophils, monocytes and lymphocytes both in vivo and in vitro. Owing to this characteristic, this compound is highly useful in SPECT image diagnosis, PET image diagnosis, MRI image diagnosis and the like, for imaging sites of inflammation.

Abstract: The present invention provides a radiation detector capable of detecting the radioactive substance accumulated in the tissue inside a body by inserting a detection unit into blood vessels. In the radiation detector of the present invention, comprising a detection unit (2) having a bar-type scintillator (4) which emits light by an incidence of radiation so as to transmit the light from the scintillator through an optical fiber, the detection unit is formed in a size capable of being inserted into the tubules while fine convexoconcaves are provided on the peripheral surface of the scintillator.

Abstract: The present invention relates to a method for readily determining the binding site on plasma protein and binding displacement effect of a drug having binding affinity to plasma protein, and application of the method to clinical diagnosis. That is to say, the present invention provides a method for determining the binding site with plasma protein of a first drug, comprising reacting the first drug for which the binding site with plasma protein is to be determined, with a second drug of which the binding site with plasma protein is known and plasma protein, and determining the change in the ratio of the first drug freed due to the binding of the plasma protein with the second drug.

Abstract: An agent which comprises, as an active ingredient, a radiolabeled compound as represented by the following formula or a pharmaceutically acceptable salt thereof: wherein R1 denotes hydrogen, or a linear- or branched-chain alkyl group having 1–8 carbon atoms, R2 denotes hydrogen, hydroxyl or a halogen substituent, R3 denotes hydrogen or fluorine substituent, R4 denotes oxygen, sulfur, or a methylene substituent, and R5 denotes a radioactive halogen substituent. The agent is stable in vivo, and either stays in cells or is incorporated in DNA, thus serving for diagnosis of tissue proliferation activity or treatment of proliferative disease.

Abstract: An agent which comprises, as an active ingredient, a radiolabeled compound as represented by the following formula or a pharmaceutically acceptable salt thereof: wherein R1 denotes hydrogen, or a linear- or branched-chain alkyl group having 1–8 carbon atoms, R2 denotes hydrogen, hydroxyl or a halogen substituent, R3 denotes hydrogen or fluorine substituent, R4 denotes oxygen, sulfur, or a methylene substituent, and R5 denotes a radioactive halogen substituent. The agent is stable in vivo, and either stays in cells or is incorporated in DNA, thus serving for diagnosis of tissue proliferation activity or treatment of proliferative disease.