Search results for "HALF-LIFE"
showing 10 items of 108 documents
[ 18 F]Fluoroethylflumazenil: a novel tracer for PET imaging of human benzodiazepine receptors
2001
5-(2'-[18F]Fluoroethyl)flumazenil ([18F]FEF) is a fluorine-18 labelled positron emission tomography (PET) tracer for central benzodiazepine receptors. Compared with the established [11C]flumazenil, it has the advantage of the longer half-life of the fluorine-18 label. After optimisation of its synthesis and determination of its in vitro receptor affinities, we performed first PET studies in humans. PET studies in seven healthy human volunteers were performed on a Siemens ECAT EXACT whole-body scanner after injection of 100-280 MBq [L8F]FEF. In two subjects, a second PET scan was conducted after pretreatment with unlabelled flumazenil (1 mg or 2.5 mg i.v., 3 min before tracer injection). A t…
Stabilization of a nutraceutical omega-3 fatty acid by encapsulation in ultrathin electrosprayed zein prolamine.
2010
Docosahexaenoic acid (DHA) is a long chain polyunsaturated fatty acid of the omega-3 series (omega-3), which exerts strong positive influences on human health. The target of this study was the stabilization by encapsulation of this bioactive ingredient in zein ultrathin capsules produced by electrospraying. The zein ultrathin DHA encapsulation was observed by ATR-FTIR spectroscopy to be more efficient against degradation under both ambient conditions and in a confined space (so-called headspace experiment). In the latter case, that more closely simulates a sealed food packaging situation, the bioactive DHA was considerably more stable. By fitting the degradation data to a specific auto-deco…
Measured and Modeled Residue Dynamics of Famoxadone and Oxathiapiprolin in Tomato Fields
2018
A reliable analytical method for the simultaneous determination of famoxadone and oxathiapiprolin dissipation kinetics as well as the metabolites of oxathiapiprolin (IN-E8S72 and IN-WR791) in tomato and soil was developed. We studied the dissipation of famoxadone and oxathiapiprolin in tomatoes grown using different kinetic curves in the area of Beijing in 2015 and 2016. Our results show that the most suitable model for two fungicides in 2015 and 2016 was first-order kinetic and second-order kinetic with the half-lives of 3.4 to 5.2 and 2.4 to 3.0 days, respectively. In addition, we applied the dynamic plant uptake model dynamiCROP and combined it with results from the field experiments to …
In vitro evaluation of poloxamer in situ forming gels for bedaquiline fumarate salt and pharmacokinetics following intramuscular injection in rats
2019
Graphical abstract
Design and synthesis of 1-aryl-5-anilinoindazoles as c-Jun N-terminal kinase inhibitors.
2012
Starting from pyrazole HTS hit (1), a series of 1-aryl-1H-indazoles have been synthesized as JNK3 inhibitors with moderate selectivity against JNK1. SAR studies led to the synthesis of 5r as double digital nanomolar JNK3 inhibitor with good in vivo exposure.
Toxicity of Dimethoate to Some Soil Animal Species in Different Soil Types
1996
Toxicity of dimethoate (insecticide) to an earthworm (Aporrectodea caliginosa tuberculata), a collembola (Folsomia candida), and an enchytraeid worm (Enchytraeus crypticus/variatus) was studied in three different soil types (artificial soil, clayey soil, and humus sandy soil). Parameters measured were survival and biomass change of the earthworms and survival and reproduction of the collembolas and enchytraeids. The degradation of dimethoate was analyzed too. Toxic effects were observed at the concentrations of some mg/kg dry soil. The biomass reduction of the earthworms occurred at lower concentrations than reduction in survival. The collembolas were more susceptible to dimethoate than the…
Pesticide toxicokinetics in fish: accumulation and elimination.
1998
Bioaccumulation of fenitrothion in the European eel (Anguilla anguilla) was studied using two sublethal concentrations of this pesticide in a flow-through test system. The pesticide concentrations used were one-tenth (0.002 ppm) and one-fifth (0.04 ppm) the 96-h LC50 of fenitrothion in this species. Steady state was reached early (2 h) when the animals were exposed to 0.02 ppm of toxicant, and after 48 h when the animals were exposed to 0.04 ppm. Toxicokinetic parameters for fenitrothion in eel muscle (K1, K2, and T1/2) were calculated for both experiments. The highest bioconcentration factor was calculated for animals exposed to 0.04 ppm of toxicant, indicating the relationship between the…
A PAS domain with an oxygen labile [4Fe-4S](2+) cluster in the oxygen sensor kinase NreB of Staphylococcus carnosus.
2008
The cytoplasmic histidine sensor kinase NreB of Staphylococcus carnosus responds to O(2) and controls together with the response regulator NreC the expression of genes of nitrate/nitrite respiration. nreBC homologous genes were found in Staphylococcus strains and Bacillus clausii, and a modified form was found in some Lactobacillus strains. NreB contains a sensory domain with similarity to heme B binding PAS domains. Anaerobically prepared NreB of S. carnosus exhibited a (diamagnetic) [4Fe-4S](2+) cluster when assessed by Mossbauer spectroscopy. Upon reaction with air, the cluster was degraded with a half-life of approximately 2.5 min. No significant amounts of Mossbauer or EPR detectable i…
Alpha decay study of 218U; a search for the sub-shell closure at Z=92
2006
Neutron-deficient uranium isotopes were studied via α spectroscopic methods. A low-lying α-decaying isomeric state was found in 218U. The new isomeric state was assigned spin and parity I π = 8+. The isomer decays by α emission with an energy E = 10678(17) keV and with a half-life T 1/2 = (0.56 -0.14 +0.26 ) ms. The known alpha-decay properties of the ground state of 218U was measured with improved statistics. The ground-state α-decay has an energy E = 8612(9) keV and a half-life T 1/2 = (0.51 -0.10 +0.17 ) ms.
44Sc-DOTA-BN[2-14]NH2 in comparison to 68Ga-DOTA-BN[2-14]NH2 in pre-clinical investigation. Is 44Sc a potential radionuclide for PET?
2011
In the present study we demonstrate the in vitro and in vivo comparison of the (44)Sc and (68)Ga labeled DOTA-BN[2-14]NH(2). (44)Sc is a positron emitter with a half life of 3.92 h. Hence it could be used for PET imaging with ligands requiring longer observation time than in the case of (68)Ga.The binding affinity of (nat)Sc-DOTA-BN[2-14]NH(2) and (nat)Ga-DOTA-BN[2-14]NH(2) to GRP receptors was studied in competition to [(125)I-Tyr(4)]-Bombesin in the human prostate cancer cell line PC-3. A preliminary biodistribution in normal rats was performed, while first microPET images were assessed in male Copenhagen rats bearing the androgen-independent Dunning R-3327-AT-1 prostate cancer tumor.The …