Search results for "Positron"
showing 10 items of 1346 documents
SYNTHESIS AND IN VITRO AFFINITIES OF VARIOUS MDL 100907 DERIVATIVES AS POTENTIAL 18F-RADIOLIGANDS FOR 5-HT2A RECEPTOR IMAGING WITH PET
2008
Radiolabelled piperidine derivatives such as [(11)C]MDL 100907 and [(18)F]altanserin have played an important role in diagnosing malfunction in the serotonergic neurotransmission. A variety of novel piperidine MDL 100907 derivatives, possible to label with (18)F-fluorine, were synthesized to improve molecular imaging properties of [(11)C]MDL 100907. Their in vitro affinities to a broad spectrum of neuroreceptors and their lipophilicities were determined and compared to the clinically used reference compounds MDL 100907 and altanserin. The novel compounds MA-1 (53) and (R)-MH.MZ (56) show K(i)-values in the nanomolar range towards the 5-HT(2A) receptor and insignificant binding to other 5-HT…
(18) F-labeled folic acid derivatives for imaging of the folate receptor via positron emission tomography.
2013
The folate receptor (FR) is already known as a proven target in diagnostics and therapy of cancer. Furthermore, the FR is involved in inflammatory and autoimmune diseases. The major advantage as a valuable target is its strongly limited expression in healthy tissues. Over the past two decades, several folic acid-based radiopharmaceuticals addressing the FR have been developed, and some of them show great potential for applications in clinical routine. However, most of these radiofolates were developed for single photon emission computed tomography imaging, and only a few can be used for positron emission tomography (PET) imaging. The development of suitable (18) F-labeled derivatives for PE…
Selective binding to monoamine oxidase A: in vitro and in vivo evaluation of (18)F-labeled β-carboline derivatives.
2015
In this study we synthesized four different (18)F-labeling precursors for the visualization of the monoamino oxidase A using harmol derivatives. Whereas two are for prosthetic group labeling using [(18)F]fluoro-d2-methyl tosylate and 2-[(18)F]fluoroethyl-tosylate, the other three precursors are for direct nucleophilic (18)F-labeling. Additionally the corresponding reference compounds were synthesized. The syntheses of [(18)F]fluoro-d2-methyl-harmol and 2-[(18)F]fluoroethyl-harmol were carried out using harmol as starting material. For direct nucleophilic (18)F-labeling of the tracers carrying oligoethyled spacers (PEG), a toluenesulfonyl leaving group was employed. The radiolabeling, purifi…
Efficient microwave-assisted direct radiosynthesis of [(18)F]PR04.MZ and [(18)F]LBT999: selective dopamine transporter ligands for quantitative molec…
2009
Abstract PR04.MZ 8-(4-fluoro-but-2-ynyl)-3- p -tolyl-8-aza-bicyclo[3.2.1]octane-2-carboxylic acid methyl ester ( 1 ) and LBT999 8-(( E )-4-fluoro-but-2-enyl)-3b- p -tolyl-8-aza-bicyclo[3.2.1]octane-2β-carboxylic acid methyl ester ( 2 ) are selective dopamine reuptake inhibitors, derived from cocaine. Compounds 1 and 2 were labelled with fluorine-18 at their terminally fluorinated N-substituents employing microwave enhanced direct nucleophilic fluorination. K[ 18 F]F − Kryptofix ® 222 cryptate, tetrabutyl ammonium [ 18 F]fluoride and caesium [ 18 F]fluoride were compared as fluoride sources under conventional and microwave enhanced conditions. Fluorination yields were remarkably increased un…
Synthesis of No-Carrier-Added 4-[18F]Fluorophenol from 4-Benzyloxyphenyl-(2-thienyl)iodonium Bromide
2011
4-[(18)F]Fluorophenol is a versatile synthon for the synthesis of more complex radiopharmaceuticals bearing a 4-[(18)F]fluorophenoxy moiety. In order to prepare 4-[(18)F]fluorophenol in no-carrier-added (n.c.a.) form only a nucleophilic labelling method starting from [(18)F]fluoride is suitable. In this paper a new, two step radiosynthesis starting from 4-benzyloxyphenyl-(2-thienyl)iodonium bromide and [(18)F]fluoride with subsequent deprotection is described, yielding n.c.a. [(18)F]fluorophenol in 34 to 36% radiochemical yield.
Performance evaluation of a high resolution dedicated breast PET scanner
2016
Purpose: Early stage breast cancers may not be visible on a whole-body PET scan. To overcome whole-body PET limitations, several dedicated breast positron emission tomography (DbPET) systems have emerged nowadays aiming to improve spatial resolution. In this work the authors evaluate the performance of a high resolution dedicated breast PET scanner (Mammi-PET, Oncovision). Methods: Global status, uniformity, sensitivity, energy, and spatial resolution were measured. Spheres of different sizes (2.5, 4, 5, and 6 mm diameter) and various 18 fluorodeoxyglucose (18F-FDG) activity concentrations were randomly inserted in a gelatine breast phantom developed at our institution. Several lesion-to-ba…
Development of Trackable Anticancer Agents Based on Metal Complexes
2016
Abstract The design of trackable anticancer agents is of major interest for the future development of therapeutics based on nonplatinum metal complexes such as Ru(II), Os(II), or Au(I) derivatives, and more particularly for the understanding of the mechanism of action of these metal-based drugs. This review reports the synthesis and the first biological studies of original trackable complexes, in which the metal complex was coupled to an imaging probe, such as a fluorophore (coumarin, borodipyrromethene derivative (BODIPY), porphyrin), or a chelating agent (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA)) for radioisotopic imaging PET (positron emission tomography) or SPECT …
Positronium as a probe in natural polymers: decomposition in starch
2009
Ortho-positronium (o-Ps) is used as a probe in positron annihilation lifetime spectroscopy (PALS) experiments, to characterise the behaviour of free volumes in natural starch samples, as a function of temperature (T). Up to about 540 K, the o-Ps intensity, I(3), remains constant at 26.2% while its lifetime, tau(3), is found to increase linearly. Both parameters undergo a decrease above this T, due to the onset of decomposition, which results in a shrinking of the sample pellets. The results indicate that the glass transition temperature should be above 501 K. Data from thermal gravimetry analysis (TGA) measurements are well described by supposing a first order process for the survival proba…
Search for neutralino pair production at root s = 189 GeV
2001
A search for pair-production of neutralinos at a LEP centre-of-mass energy of 189 GeV gave no evidence for a signal. This limits the neutralino production cross-section and excludes regions in the parameter space of the Minimal Supersymmetric Standard Model (MSSM).
Quantification of pulmonary blood flow (PBF): validation of perfusion MRI and nonlinear contrast agent (CA) dose correction with H(2)15O positron emi…
2009
Validation of quantification of pulmonary blood flow (PBF) with dynamic, contrast-enhanced MRI is still missing. A possible reason certainly lies in difficulties based on the nonlinear dependence of signal intensity (SI) from contrast agent (CA) concentration. Both aspects were addressed in this study. Nine healthy pigs were examined by first-pass perfusion MRI using gadolinium diethylenetriamine pentaacetic acid (Gd-DTPA) and HO positron emission tomography (PET) imaging. Calculations of hemodynamic parameters were based on a one-compartment model (MR) and a two-compartment model (PET). Simulations showed a significant error when assuming a linear relation between MR SI and CA dose in the …