Current Radiopharmaceuticals - Volume 1, Issue 2, 2008

A selective and potent iNOS inhibitor, 8-fluoro-3-(4-fluorophenyl)-3,4-dihydro-1-isoquinolinamine (IC50 =0.16 μM) has been developed recently [8]. Based on that inhibitor, a novel PET imaging tracer intended for in vivo assessment of the iNOS, the F-18 labeled 8-fluoro-3-(4-[18F]fluorophenyl)-3,4-dihydro-1-isoquinolinamine ([18F]FFDI) was synthesized. [18F]FFDI was first prepared with radiochemical yield of Read More

To illustrate the role of radiopharmaceuticals in characterizing non-hypersecreting adrenal masses, 56 patients with non-hypersecreting unilateral adrenal tumors detected on CT and/or MR underwent adrenal scintigraphy. A total of 83 radionuclide studies was acquired; in particular, 24 patients underwent nor-cholesterol scan, 23 patients had metaiodobenzylguanidine (MIBG) imaging, 26 patients had deoxyglucose (FDG) studies Read More

A case of a patient with bronchioloalveolar cell predominate lung adenocarcinoma (BAC) studied using integrated Positron Emission Tomography and Computed Tomography (PET/CT) with both 18F-fluorodeoxyglucose ([18F]FDG-PET) and [11C]Choline ([11C]Choline-PET) is described, with the aim of evaluating a new non invasive imaging method to detect and stage BAC, and providing information on tumour biology in vivo. Th Read More

The intense focus of radiochemical damage and cytotoxicity induced by Auger electron emitters is well known and provides a basis for their potential use in cancer therapy. Auger electron-emitting radionuclides decay by electron capture and/or internal conversion. The key feature of these modes of decay is the simultaneous release of low energy electrons, collectively known as Auger electrons. The unique characteri Read More

Diagnosing osteomyelitis is clinically challenging. Laboratory tests are of limited utility, and other than isolation of the offending organism, diagnostic imaging tests are of paramount importance. There are a myriad of scintigraphic tests from which to choose, and no single test is optimal for all indications. With an accuracy of more than 90%, bone scintigraphy is the radionuclide test of choice for diagnosing osteomyelitis i Read More

For radionuclide therapy of hepatocellular carcinoma, there have been many attempts to label Lipiodol (an iodinated ester of popyseed oil) with therapeutic radioisotopes, including 131I, 90Y, 186Re and 188Re. 131I-labelled Lipiodol is a commercially available radiopharmaceutical that is currently used in many countries. Nonetheless, despite encouraging results, there are some disadvantages with Iodine- 131, in particula Read More

There is strong interest in clinical research to be able to study cannabinoid subtype-1 (CB1) receptors in living human brain with positron emission tomography (PET). Here, we aimed to prepare and compare in monkey three structurally-related high potency candidate PET radioligands for CB1 receptors based on the 1,5-diarylpyrazole platform, namely [O-methyl-11C][N-(piperidin-1-yl)-5-(4- methoxyphenyl)-1-(2-bromophenyl)- Read More

A convenient remotely-controlled synthesis of no-carrier-added sodium [18F]fluoroacetate is described. Three ethyl esters 1a- 1c and three t-butyl esters 3a-3c containing either a methanesulfonyloxy- (OMs), p-toluenesulfonyloxy- (OTs) or p-nitrobenzenesulfonyloxy (ONs) leaving group were investigated as labeling precursors. The optimized radiosynthesis of n.c.a. sodium [18F]fluoroacetate was performed in two steps: (1) In Read More

The aim of this work was to develop a PET radiotracer which would enable the study of central serotonin 5-HT4 receptors in man using positron emission tomography (PET). A procedure was developed for labelling SB207145, a potent and selective 5-HT4 antagonist, with the short-lived positron emitting radionuclide 11C. Alkylation of the corresponding desmethyl compound with 11C-methyl iodide afforded [11C]SB20714 Read More

Introduction: Neuroendocrine cells of the prostate are regulatory cells containing biogenic amines and certain neuropeptides such as chromogranin A (CgA). In the present study we evaluated the usefulness of serum CgA for monitoring prostate cancer progression. CgA levels were correlated to serum Prostate Specific Antigen (PSA) levels, bone scan findings and Gleason score. Methods: In this study we evaluated 122 patients wi Read More

1-Amino-2-[3-13C]propanol hydrochloride (1) was synthesized by the coupling reaction of 2-phthalimidoacetyl chloride (2) with [13C]methylmagnesium iodide in the presence of copper iodide, followed by reduction with sodium borohydride and hydrolysis, in 64 % total yield from the 13C-source. All 13C- and 15N-isotopomers of 1-amino-2-propanol are now obtainable by using appropriate combinations of 13 Read More

Synthesis of L-[3-13C]tryptophan (2) from N,N-dimethyl[13C]formamide (4) and Dellaria's oxazinone 1 as a chiral glycine equivalent was achieved. Vilsmeier reaction of indole (5) and N,N-dimethyl[13C]formamide (4) afforded a good yield of indole-3-[13C]carbaldehyde (3), which was converted to the bromide 8. Diastereoselective alkylation of the enolate of 1 with the bromide 8 proceeded with high diastereoselectivity to give 9. Read More