139 research outputs found
ΠΠΊΠΎΠ»ΠΎΠ³ΠΈΡΠ΅ΡΠΊΠΎΠ΅ Π²ΠΎΡΠΏΠΈΡΠ°Π½ΠΈΠ΅ ΡΡΡΠ΄Π΅Π½ΡΠΎΠ² Π²ΡΠ·ΠΎΠ²
Π ΡΡΠ°ΡΡΠ΅ ΡΠ°ΡΠΊΡΡΠ²Π°ΡΡΡΡ ΡΠ΅ΠΎΡΠ΅ΡΠΈΡΠ΅ΡΠΊΠΈΠ΅ ΠΎΡΠ½ΠΎΠ²Ρ ΡΠΊΠΎΠ»ΠΎΠ³ΠΈΡΠ΅ΡΠΊΠΎΠ³ΠΎ Π²ΠΎΡΠΏΠΈΡΠ°Π½ΠΈΡ ΡΡΡΠ΄Π΅Π½ΡΠΎΠ² ΠΈ ΠΎΡΠΎΠ±Π΅Π½Π½ΠΎΡΡΠΈ ΡΠΊΠΎΠ»ΠΎΠ³ΠΈΡΠ΅ΡΠΊΠΎΠ³ΠΎ Π²ΠΎΡΠΏΠΈΡΠ°Π½ΠΈΡ: ΡΠΎΡΠΌΠΈΡΠΎΠ²Π°Π½ΠΈΠ΅ ΡΠΊΠΎΠ»ΠΎΠ³ΠΈΡΠ΅ΡΠΊΠΈΡ
ΠΏΡΠ΅Π΄ΡΡΠ°Π²Π»Π΅Π½ΠΈΠΉ; ΡΠ°Π·Π²ΠΈΡΠΈΠ΅ ΡΠΊΠΎΠ»ΠΎΠ³ΠΈΡΠ΅ΡΠΊΠΎΠ³ΠΎ ΡΠΎΠ·Π½Π°Π½ΠΈΡ ΠΈ ΡΡΠ²ΡΡΠ²; ΡΠΎΡΠΌΠΈΡΠΎΠ²Π°Π½ΠΈΠ΅ ΡΠ±Π΅ΠΆΠ΄Π΅Π½ΠΈΠΉ Π² Π½Π΅ΠΎΠ±Ρ
ΠΎΠ΄ΠΈΠΌΠΎΡΡΠΈ ΡΠΊΠΎΠ»ΠΎΠ³ΠΈΡΠ΅ΡΠΊΠΎΠΉ Π΄Π΅ΡΡΠ΅Π»ΡΠ½ΠΎΡΡΠΈ; Π²ΡΡΠ°Π±ΠΎΡΠΊΠ° Π½Π°Π²ΡΠΊΠΎΠ² ΠΈ ΠΏΡΠΈΠ²ΡΡΠ΅ΠΊ ΠΏΠΎΠ²Π΅Π΄Π΅Π½ΠΈΡ Π² ΠΏΡΠΈΡΠΎΠ΄Π΅. The article describes the theoretical foundations of environmental education students and especially environmental education: the formation of environmental performances; the development of ronmental consciousness and feelings; the formation of beliefs in the necessity of environmental performance; develop the skills and habits of behavior in nature
Synthesis, Biodistribution and In vitro Evaluation of Brain Permeable High Affinity Type 2 Cannabinoid Receptor Agonists [11C]MA2 and [18F]MA3
Abstract The type 2 cannabinoid receptor (CB2) is a member of the endocannabinoid system and is known for its important role in (neuro)inflammation. A PET-imaging agent that allows in vivo visualization of CB2 expression may thus allow quantification of neuroinflammation. In this paper, we report the synthesis, radiosynthesis, biodistribution and in vitro evaluation of a carbon-11 ([11C]MA2) and a fluorine-18 ([18F]MA3) labeled analogue of a highly potent N-arylamide oxadiazole CB2 agonist (EC50 = 0.015 nM). MA2 and MA3 behaved as potent CB2 agonist (EC50: 3 nM and 0.1 nM, respectively) and their in vitro binding affinity for hCB2 was found to be 87 nM and 0.8 nM, respectively. Also MA3 (substituted with a fluoro ethyl group) was found to have higher binding affinity and EC50 values when compared to the originally reported trifluoromethyl analogue 12. [11C]MA2 and [18F]MA3 were successfully synthesized with good radiochemical yield, high radiochemical purity and high specific activity. In mice, both tracers were efficiently cleared from blood and all major organs by the hepatobiliary pathway and importantly these compounds showed high brain uptake. In conclusion, [11C]MA2 and [18F]MA3 are shown to be high potent CB2 agonists with good brain uptake, these favorable characteristics makes them potential PET probes for in vivo imaging of brain CB2 receptors. However in view of its higher affinity and selectivity, further detailed evaluation of MA3 as a PET tracer for CB2 is warranted
Radioiodinated Phenylalkyl Malonic Acid Derivatives as pH-Sensitive SPECT Tracers
pH imaging has been a field of interest for molecular imaging for many years. This is especially important for determining tumor acidity, an important driving force of tumor invasion and metastasis formation, but also in the process of apoptosis.I]IPM was evaluated in an anti-Fas monoclonal antibody (mAb) apoptosis model. In addition a mouse RIF-1 tumor model was explored in which tumor pH was decreased from 7.0 to 6.5 by means of induction of hyperglycemia in combination with administration of meta-iodobenzylguanidine.I]IPM showed a clear pH-related uptake pattern in the RIF-1 tumor model. which allows to visualize regional acidosis. However, these compounds are not suitable for detection of apoptosis due to a poor acidosis effect
811-1 Evolution of Left Ventricular Function, Myocardial Perfusion and Metabolism in Infarct Patients After Coronary Thrombolysis
Follow-up of regional myocardial blood flow, metabolism and function was studied in a population of thrombolysed patients. Fifty one patients with an acute myocardial infarction were prospectively enrolled. All patients received thrombolytic therapy within 6 hours after the onset of symptoms. Coronary angiography, 2D-echocardiography and 13NH3/18FDG PET were performed 5 days after the acute event. Three months after the infarction, 2D-echocardiography and 13NH3/18FDG PET studies were repeated.Thirty six patients (62% with TIMI III, 7% with TIMI II) revealed a concordant decrease of flow and metabolism in the infarct area (PET match). Fifteen patients (33% with TIMI III, 13% with TIMI II) revealed a decrease of flow with preservation of metabolism (PET mismatch). Twelve patients received further treatment (PTCA or CAGB) after the first PET scan. Myocardial blood flow improved significantly in both match (71Β±17ml/min/l00g at 3 months versus 60Β±17ml/min/100 g at 5 days, p<0.01) and mismatch groups (71Β±26ml/min/l00 g at 3 months versus 63 Β±18ml/min/100 g at 5 days, p<0.05). Blood flow in remote areas did not change significantly (84Β±18mllmin/l 00 g at 3 months versus 82Β±19ml/min/l 00 gat 5 days, p=NS). In 4 patients with a match pattern at 5 days, a mismatch pattern had developed 3 months after the acute event.Functional follow-up was performed in 30 patients, 23 with a match pattern and 7 with a mismatch pattern. A variable outcome was observed: In 3 out of 7 mismatch areas contractility did not improve. On the contrary, 9 out of 23 match areas revealed functional improvement.It can be concluded that in this population of early thrombolysed patients, few mismatches were observed (29%). Flow values improved significantly in both match and mismatch groups 3 months after the acute event. In some patients, a mismatch pattern was found after 3 months, suggesting the need for further treatment. Functional outcome was variable, probably due to a variety of pathophysiologic processes such as stunning shortly after reperfusion with functional improvement after 3 months, reocclusion or progression of coronary artery disease resulting in reinfarction or hibernation
PET imaging of TSPO in a rat model of local neuroinflammation induced by intracerebral injection of lipopolysaccharide.
OBJECTIVE: The goal of this study was to measure functional and structural aspects of local neuroinflammation induced by intracerebral injection of lipopolysaccharide (LPS) in rats using TSPO microPET imaging with [(18)F]DPA-714, magnetic resonance imaging (MRI), in vitro autoradiography and immunohistochemistry (IHC) in order to characterize a small animal model for screening of new PET tracers targeting neuroinflammation.
METHODS: Rats were injected stereotactically with LPS (50 ΞΌg) in the right striatum and with saline in the left striatum. [(18)F]DPA-714 microPET, MRI, in vitro autoradiography and IHC studies were performed at different time points after LPS injection for 1 month.
RESULTS: Analysis of the microPET data demonstrated high uptake of the tracer in the LPS injected site with an affected-to-non-affected side-binding potential ratio (BPright-to-left) of 3.0 at 3 days after LPS injection. This BP ratio decreased gradually over time to 0.9 at 30 days after LPS injection. In vitro autoradiography ([(18)F]DPA-714) and IHC (CD68, GFAP and TSPO) confirmed local neuroinflammation in this model. Dynamic contrast enhanced (DCE) MRI demonstrated BBB breakdown near the LPS injection site at day 1, which gradually resolved over time and was absent at 1 month after LPS injection.
CONCLUSION: The LPS model is useful for first screening of newly developed tracers because of the easy design and the robust, unilateral inflammatory reaction allowing the use of the contralateral region as control. Additionally, this model can be used to test and follow up the benefits of anti-inflammatory therapies by non-invasive imaging
Rhenium dicarbonyl-nitrosyl complexes with imidazole
Different rhenium-dicarbonyl-nitrosyl complexes with imidazole (Im) as monodentate ligand have been synthesized and characterized, starting from [NEt4][ReCl3(CO)(2)(NO)] and [ReCl(mu-Cl)(CO)(2)(NO)](2). Whereas the complexes [ReCl2(Im)(CO)(2)(NO)] and [ReCl(IM)(2)(CO)(2)(NO)](+) were achieved in high yields, the complex [Re(Im)(3)(CO)(2)(NO)](2+) with three imidazole ligands could only be isolated after complete removal of all halide ions (with AgBF4) in low yield. The synthesis of a corresponding Tc-99m-dicarbonyl-nitrosyl complex with imidazole opens a new perspective for such compounds as potential radiopharmaceuticals and alternatives to the already established Te-99m-tricarbonyl complexes.status: publishe
Synthetic strategies for radioligands for in vivo imaging of brain cannabinoid type-1 receptors
Despite its abundant expression in the brain, the cannabinoid type-1 (CB1) receptor was discovered only in 1988. During the last decade, efforts from several research groups have made it possible to visualize the CB1 receptor in vivo to unravel its role in the brain physiology and pathology. This review discusses strategies for (radio)synthesis of radioligands for in vivo imaging of CB1 receptors
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