Institute of Nuclear Energy Research, Atomic Energy Council, Executive Yuan

Institute of Nuclear Energy Research, Atomic Energy Council, Executive Yuan, R.o.c

Hung-Man Yu

Wuu-Jyh Lin

Mei-Hui Wang

Chuan-Yi Chien

Kun-Liang Lin

Yuan-Chuan Lee

Reiko Takasaka Lee

Ping-Yen Wang

Jyun-Hong Chen

Mao-Chi Weng

Jen-Tsung Wang

Chun-Hao Tseng

Chun-Hung Yang

Chia-Yu Hu

Chien-Jen Chen

Rui-Yu Chen

Yan-Feng Jiang

The present invention provides a hexa-lactoside-triazanonane triacetic acid (NOTA) derivative, a method for radiolabeling a hexa-lactoside positron emission tomography (PET) imaging agent for a liver receptor with Ga-68, and a hexa-lactoside PET imaging agent for a liver receptor. The hexa-lactoside-NOTA derivative is a conjugate of six chains of lactose with NOTA obtained by conjugating hexa-lactoside to a chelating agent p-thiocyanate-benzyl-triazanonane diacetic acid-glutamic acid in the presence of triethyl amine/dimethyl formamide as a solvent. The radiolabeling method comprises labeling with Ga-68 at room temperature. According to the present invention, the labeling effect is stable, the labeling efficiency of the labeled product is greater than 95%, the labeled product is highly stable and the radiochemical purity is still greater than 90% after 4 hours.

Hexa-lactoside-triazanonane triacetic acid (NOTA) derivative, method for radiolabeling hexa-lactoside positron emission tomography (PET) imaging agent for liver receptor with Ga-68, and hexa-lactoside PET imaging agent for liver receptor

The present invention relates to a hydroxamic acid-based contrast agent containing an isotope of fluorine, which comprises a compound having a structure of Formula (III):  wherein Rrepresents radioactive fluorine-18 (F) or isotope fluorine-19 (F), and Rrepresents hydroxyamine &#x2014;(NH)OH. The hydroxamic acid-based contrast agent containing an isotope of fluorine provided in the present invention has the capability of selectively inhibiting histone deacetylase (HDAC) subtypes 8/6/3, and specifically targets to the focus of spinocerebellar ataxia with over-activation of HDAC. By labeling with the radioisotope fluorine-18, a positron emission tomography (PET) image is obtained with the hydroxamic acid-based contrast agent containing radioisotope fluorine-18, whereby spinocerebellar ataxia is effectively detected. Therefore, the hydroxamic acid-based contrast agent containing an isotope of fluorine provided in the present invention is potentially useful as a probe for early diagnosis and evaluation of the therapeutic effect of spinocerebellar ataxia.

Hydroxamic acid type contrast agent containing radioisotope fluoride, preparation method and application thereof

Disclosed herein are a multivalent saccharide complex, a radioactive multivalent saccharide complex contrast agent and use thereof. The multivalent saccharide complex has a chelator, a linker, and glucose, and is configured to diagnose and evaluate the therapeutic effect of cancers.

Multivalent saccharide complex, radioactive multivalent saccharide complex contrast agent, and use thereof

Disclosed herein is a bispecific peptide conjugate comprising an epidermal growth factor receptor (EGFR) targeting peptide, an &#x3b1;v&#x3b2;3 integrin targeting peptide, and a linker, where the linker is conjugated respectively to the EGFR targeting peptide and the &#x3b1;v&#x3b2;3 integrin targeting peptide.

Bispecific peptide conjugate and radioactive bispecific peptide imaging agent

A test indicator for quantifying remaining liver function is provided. A novel liver receptor imaging agent with liver targeting property is utilized to develop a method for quantifying remaining liver function to serve as test indicator for judging the liver failure outcome in clinic, particularly for judging the necessity of liver transplantation for patients with liver failure or liver disease. The radioactivity uptake of the test indicator was negatively correlated with the extent of liver reserve. The cutoff value of liver reserve for liver transplantation is also disclosed.

Quantification method for remaining liver function and novel liver receptor imaging agent

A novel gall bladder image agent which includes a radio-labelled MAG3-tri-galactosamine, and its preparation method, which includes reacting mercaptoacetyltriglycine (MAG3)-tri-galactosamine, SnF2 and Tc-99m in the presence of a phosphate buffer solution (at pH of from 10.0&#x2dc;12.0) to obtain Tc-99m-MAG3-tri-galactosamine, when the MAG3-tri-galactosamine is MAG3-DCM-Lys(Gah-GalNAc)3 (where DCM represents a dicarboxymethyl group, and Gah represents a glycine-aminohexyl group), it obtains a labelling yield of at least 90%, and its specific radioactivity is at least 7.0&#xd7;109 Bq/mg.

Gall bladder imaging agent and its preparation method

The present invention is related to a pharmaceutical composition for a liver-receptor imaging injection, the pharmaceutical composition including a bi-functional compound which has a ASGPR specificity, wherein the bi-functional compound includes a backbone of alpha-amino acid (or the derivatives thereof) and a poly-galactosamine chain (or a poly-lactose chain) connected to the alpha-amino acid. Thereby, the pharmaceutical composition can quantify potential of liver storage ability and evaluate severity of the course of liver disease. A liver-receptor imaging injection using the same and the one-step dispensing method thereof are also provided to improve defects of iodine-labeled and overcome disadvantages of the reduced labeling-yield and the instability after autoclave sterilization.

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Taoyuan, Taiwan

Hung-Man Yu