摘要:
There is disclosed a radioligand labeled with a positron emitting radionuclide suitable for dynamic study in living humans with positron emission transaxial tomography. [.sup.18 F]-N-methylspiroperidol, exhibiting extremely high affinity for the dopamine receptors, provides enhanced uptake and retention in the brain concomitant with reduced radiation burden. These characteristics all combine to provide [.sup.18 F]-N-methylspiroperidol as a radioligand superior to known radioligands for mapping dopamine receptors in normal and disease states in the living brain. Additionally, a new synthetic procedure for this material is disclosed.
摘要:
There is disclosed radioligands labeled with the position emitting radionuclide [.sup.18 F] suitable for dynamic study in living humans with position emission transaxial tomography. These new [.sup.18 F]-N-fluoroalkylspiroperidols, wherein the alkyl group contains from 2-6 carbon atoms, exhibit extremely high affinity for the dopamine receptors and provide enhanced uptake and retention in the brain concomitant with reduced radiation burden. These characteristics all combine to make these new radioligands useful for mapping dopamine receptors in normal and disease states in the living brain. Additionally, a new synthetic procedure for these radioligands as well as a new procedure for preparing the radiolabeled alkyl halide alkylating reagents are also disclosed.
摘要:
Process for the production of 2-deoxy-2-fluoro-D-glucose and the corresponding .sup.18 F-compound in which methyl 4,6-O-benzylidine-3-O-methyl-2-O-trifluoromethanesulfonyl-.beta.-D-mannopyranoside is reacted with a triflating reagent, the resulting compound reacted with CsHF.sub.2, RbF or the corresponding .sup.18 F-compounds, and thereafter the alkyl groups removed by hydrolysis.
摘要:
Process for the production of 2-deoxy-2-fluoro-D-glucose and the corresponding .sup.18 F-compound by the reaction of acetyl hypofluorite or the corresponding .sup.18 F-compound with 3,4,6-tri-O-acetyl-D-glucal followed by hydrolysis. Process includes the production of the hypofluorite compound at ambient temperature.
摘要:
The novel radioactive compound .sup.18 F-4-fluoroantipyrine having high specific activity which can be used in nuclear medicine in diagnostic applications, prepared by the direct fluorination of antipyrine in acetic acid with radioactive fluorine at room temperature and purifying said radioactive compound by means of gel chromatography with ethyl acetate as eluent is disclosed. The non-radioactive 4-fluoroantipyrine can also be prepared by the direct fluorination of antipyrine in acetic acid with molecular fluorine at room temperature and purified by means of gel chromotography with ethyl acetate eluent.
摘要:
The novel compounds 1-.sup.11 C-D-glucose, 1-.sup.11 C-D-mannose, 1-.sup.11 C-D-galactose, 2-.sup.11 C-D-glucose, 2-.sup.11 C-D-mannose and 2-.sup.11 C-D-galactose which can be used in nuclear medicine to monitor the metabolism of glucose and galactose can be rapidly prepared by reaction of the appropriate aldose substrate with an alkali metal .sup.11 C-labeled cyanide followed by reduction with a Raney alloy in formic acid.
摘要:
Novel nitroaromatic compounds and immunogenic conjugates comprising a novel nitroaromatic compound and a carrier protein are disclosed. The invention further presents monoclonal antibodies highly specific for the claimed nitroaromatic compounds, the compounds' protein conjugates, the compounds' reductive byproducts, and adducts formed between the compounds and mammalian hypoxic cell tissue proteins. The invention is further directed to methods for detecting tissue hypoxia using immunohistological techniques, non-invasive nuclear medicinal methods, or nuclear magnetic resonance. Diagnostic kits useful in practicing the methods of claimed invention are also provided.
摘要:
Nitroaromatic compounds and immunogenic conjugates comprising a novel nitroaromatic compound and a carrier protein are disclosed. The invention further presents monoclonal antibodies highly specific for the claimed nitroaromatic compounds, the compounds' protein conjugates, the compounds' reductive byproducts, and adducts formed between the compounds and mammalian hypoxic cell tissue proteins. The invention is further directed to methods for detecting tissue hypoxia using immunohistological techniques, non-invasive nuclear medicinal methods, or nuclear magnetic resonance. Diagnostic kits useful in practicing the methods of claimed invention are also provided.
摘要:
Method provided for labeling a nuclear medicine for imaging tracing, comprising a labeling precursor of the HDAC inhibitor BNL-26 (C22H23N3O) and the derivatives that are separated into two classes. The first class comprises a BNL-26 (C22H23N3O) and derivatives BNL-26a (C21H21N3O), BNL-26b (C22H22N2O), and other compounds of the labeling precursors which are categorized into two parts, the first part includes BNL-26-CH2CH2OTs (C31H33N3O4S), BNL-26a-CH2CH2OTs (C30H31N3O4S), and BNL-26b-CH2CH2OTs (C31H32N2O4S), which provides labeling precursor through —CH2CH2OTs structure, and the second part includes pre-BNL-26 (C28H34N3O3B), pre-BNL-26a (C27H32N3O3B), pre-BNL-26b (C28H33N2O3B), which provides labeling precursor through 4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl structure. The second class includes BNL-26 (C22H23N3O) indole/indoline, which provides a series of derivative labeling precursors derived from a secondary amide bond.
摘要:
The present invention relates to a group of compounds for nuclear medicine imaging through F-18 labeled histone acetylation inhibitors (HDACi) of indole or indoline benzoyl amine and its derivatives, and provides a series of nuclear medicine imaging agents that bind with HDAC overexpression in vivo for diagnosis of malignant tumors discovered in the nuclear medicine imaging tracing.