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TECHNETIUM AND RHENIUM IN NUCLEAR MEDICINE

核医学中的锝和铼

基本信息

批准号：
6512439
负责人：
Alun Gareth Jones
金额：
$ 49.34万
依托单位：
HARVARD MEDICAL SCHOOL
依托单位国家：
美国
项目类别：
财政年份：
1977
资助国家：
美国
起止时间：
1977-02-01 至 2005-03-31
项目状态：
已结题

来源：
https://reporter.nih.gov/project-details/6512439
关键词：
Animalia carbonyl compound chemical structure function drug design /synthesis /production heavy metals hydrazines ligands neoplasm /cancer radionuclide diagnosis nuclear medicine radiopharmacology radiotracer serotonin receptor solid state technetium

项目摘要

DESCRIPTION (Adapted from Applicant's Abstract): The radionuclide technetium-99m continues to be the mainstay of routine clinical nuclear medicine. This research program was originally conceived on the premise that the usefulness of this radionuclide in diagnosis can only be maintained by conducting a rigorous study of the basic chemistry of the element and incorporating this knowledge into the design of new radiopharmaceuticals. This is equally true of therapeutic applications based on the use of radionuclides of its congener rhenium. In this next period the applicants proposed to concentrate primarily on two broad areas of chemistry: low valent chemistry in oxidation states (+1) and (+2), including the study of complexes continuing weak-field ligands that may provide routes into the production of new classes of complexes in aqueous media from routine precursors such as pertechnetate ion: and organohydrazine chemistry, a highly complex area that has begun to be used in certain radiopharmaceutical applications, for example, the chelate 6-hydrazinonicotinamide (HYNIC). In applications of the chemistry, the work will include an investigation of monoamide-monoamine bisthiol (MAMA or AAST) conjugated ligands targeted to 5HT-1A receptors in the brain. Factors affecting localization such as structure, choice of chelate lipophilicity, the pKa of the complex under physiological conditions, and selectivity against other receptor types will be studied. In parallel, a solid state synthesis for producing high-specific-activity samples of technetium complexes designed for receptor targeting will be explored. This is vital in circumstances where unlabeled precursor ligand could compete with the final complex for sites of occupation. The last section among the applications will focus on tumor detection. First, the 5HT-1A ligands developed for studying the brain will be evaluated for their ability to detect neuroendocrine mediated cancer of the prostate. Second, a program is being established to study small-molecule detection of cancer, in the first instance using conjugated analogs of iodinated compounds that have already bee shown by others to be avidly taken up by melanoma cells.

描述（改编自申请人摘要）：放射性核素

项目成果

期刊论文数量（6）

专著数量（0）

科研奖励数量（0）

会议论文数量（0）

专利数量（0）

Radiopharmacological studies of 99mTc-CPI: experience with isolated rat atrial tissue.

99mTc-CPI 的放射性药理学研究：离体大鼠心房组织的经验。

DOI：
10.1016/0969-8051(93)90104-3
发表时间：
1993
期刊：
Nuclear medicine and biology
影响因子：
3.1
作者：
Verdera,S;Leòn,A;Kronauge,JF;Leòn,E;Souto,B;Oliver,P;Rodriguez,A;Tamosiunas,G;Esponda,A;Jones,AG
通讯作者：
Jones,AG

Strategies for labeling monoclonal antibodies and antibody-like molecules with technetium-99m.

用 Technetium-99m 标记单克隆抗体和抗体样分子的策略。

DOI：
发表时间：
1991
期刊：
Journal of nuclear biology and medicine (Turin, Italy : 1991)
影响因子：
0
作者：
Delmon-Moingeon,LI;Mahmood,A;Davison,A;Jones,AG
通讯作者：
Jones,AG

Hexakis(carbomethoxyisopropylisonitrile) technetium(I), a new myocardial perfusion imaging agent: binding characteristics in cultured chick heart cells.

新型心肌灌注显像剂六（甲氧甲氧基异丙基异腈）锝（I）：在培养鸡心脏细胞中的结合特性。

DOI：
发表时间：
1988
期刊：
Journal of nuclear medicine : official publication, Society of Nuclear Medicine
影响因子：
0
作者：
Piwnica-Worms,D;Kronauge,JF;Holman,BL;Lister-James,J;Davison,A;Jones,AG
通讯作者：
Jones,AG

Uptake of the cation hexakis(2-methoxyisobutylisonitrile)-technetium-99m by human carcinoma cell lines in vitro.

人癌细胞系体外摄取阳离子六（2-甲氧基异丁基异腈）-technetium-99m。