We report the first clinical PET study using [1-methyl-11C]8-dicyclopropylmethyl-1-methyl-3-propylxanthine ([11C]MPDX) for imaging adenosine A1 receptors in the human brain. The binding of [11C]MPDX evaluated quantitatively as the distribution volume by a graphical analysis was high in the striatum and thalamus, and low in the cerebellum. The distribution pattern of [11C]MPDX was coincident wit...

A method of 11C-methionine synthesis using ‘bubbling’ method is presented. 11C-methionine was synthesized via 11C methylation from L-cysteine thiolactone (2 mg) in a 300 L solution of 2:1:1 (v/v) 1 M NaOH, ethanol, and water at ambient temperature (85°C, 5 min). The radiochemical purity of radiotracer was higher than 99% and enantiomeric purity (L-11C-methionine) was 91.6 ± 0.4%. The fi nal pr...

[11C]Methyl triflate ([11C]methyl trifluoromethanesulfonate) was formed in high yield when [11C]methyl iodide in a nitrogen carrier was passed at 200 degrees C through a column containing graphitized carbon impregnated with 50% by weight of silver triflate.

BACKGROUND N,N-di-n-propyl-2-[2-(4-[11C]methoxyphenyl)-6,8-dichloroimidazol[1,2-a]pyridine-3-yl]acetamide ([11C]CB184) is a novel selective radioligand for the 18-kD translocator protein (TSPO), which is upregulated in activated microglia in the brain, and may be useful in positron emission tomography (PET). We examined the safety, radiation dosimetry, and initial brain imaging with [11C]CB184 ...

BACKGROUND Metabotropic glutamate 7 (mGlu7) receptor is a crucial target protein for the development of pharmaceuticals against central nervous system disorders. In the present study, we synthesized [11C]MMPIP, a putative radioligand for mGlu7 (binding constant KB = 30 nM), and evaluated its potential for imaging of mGlu7 via in vitro and in vivo techniques. METHODS [11C]MMPIP was synthesized...

The present study aimed to assess gadoxetate disodium contrast-enhanced (CE) positron emission tomography (PET)/magnetic resonance imaging (MRI) with 68Ga-DOTATOC and 11C-5-Hydroxy-tryptophan (11C-5-HTP) in comparison iodine CE 68Ga-DOTATOC-PET/computed (CT) for neuroendocrine tumour imaging. Detection rate reader's confidence were evaluated each separate image volume: CE-CT, CE-MRI including d...

Sodium-dependent glucose cotransporter 2 (SGLT2) is a pharmacological target of type 2 diabetes mellitus. The aim of this study was to noninvasively visualize the pharmacological action of a selective SGLT2 inhibitor ipragliflozin in the kidney using positron emission tomography (PET) imaging with 11C-methyl-d-glucoside (11C-MDG), an SGLT-specific radio-labeled substrate. PET imaging with 11C-M...

The 11C-monomethylstannate prepared from [11C]-methyl iodide and Lappert's stannylene, was subject to a palladium-mediated cross-coupling reaction with an aryl halide under ligand-free conditions, to afford easily purified 11C-methyl(hetero)arenes in high radiochemical yields.

Drug resistance is a major cause of chemotherapy failure in cancer treatment. One reason is the overexpression of the drug efflux pump P-glycoprotein (P-gp), involved in multidrug resistance (MDR). In vivo pharmacokinetic analysis of P-gp transport might identify the capacity of modulation by P-gp substrate modulators, such as cyclosporin A. Therefore, P-gp function was measured in vivo with po...

11C-LY2795050 is a novel k-selective antagonist PET tracer. The in vitro binding affinities (Ki) of LY2795050 at the k-opioid (KOR) and m-opioid (MOR) receptors are 0.72 and 25.8 nM, respectively. Thus, the in vitro KOR/MOR binding selectivity is about 36:1. Our goal in this study was to determine the in vivo selectivity of this new KOR antagonist tracer in the monkey. Methods: To estimate the ...