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Potential mGAT4 inhibitors derived from the lead substance (S)-SNAP-5114 have been synthesized and characterized for their inhibitory potency. Variations from the parent compound included the substitution of one of its aromatic 4-methoxy and 4-methoxyphenyl groups, respectively, with a more polar moiety, including a carboxylic acid, alcohol, nitrile, carboxamide, sulfonamide, aldehyde or ketone function, or amino acid partial structures. Furthermore, it was investigated how the substitution of more than one of the aromatic 4-methoxy groups affects the potency and selectivity of the resulting compounds. Among the synthesized test substances (S)-1-{2-[(4-formylphenyl)bis(4-methoxyphenyl)-methoxy]ethyl}piperidine-3-carboxylic acid, that features a carbaldehyde function in place of one of the aromatic 4-methoxy moieties of (S)-SNAP-5114, was found to have a pIC50 value of 5.89±0.07, hence constituting a slightly more potent mGAT4 inhibitor than the parent substance while showing comparable subtype selectivity.  相似文献   
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An automated system for integrated electrophysical and optical studies of semiconductor nanoheterostructures, which operates in a wide temperature range from 15 to 475 K, is designed. The setup is intended to measure the temperature and frequency admittance and electroluminescence spectra of light-emitting diode and laser chips formed on substrates of diameter up to 50.2 mm, and the distribution of parameters over the wafer. The setup includes the closed-cycle helium cryogenic station, LCR meter, and temperature controller. The characterization results of nanoheterostructures with InGaN/GaN multiple quantum wells, which are used for creating highly efficient white and blue light-emitting diodes, are presented.  相似文献   
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The influence of the thermal cycling conditions on the thermal-cycling creep of a TN-1 alloy and the related irreversible deformations is studied. The conditions under which an anomalous increase in the irreversible deformations begins are determined. The structural mechanism of the irreversible deformations of an equiatomic alloy is shown to be analogous to the structural mechanism of metal creep at high temperatures: it predominantly has a dislocation character. It is proposed to use the effect of anomalous increase in the deformation of materials with reversible martensitic transformations for forming parts made of these materials at low temperatures.  相似文献   
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Intended learning outcomes (ILOs) indicate what learners will be able to achieve after they are taught. Traditionally, ILOs are expressed as plain text or unstructured documents. What if all ILOs of a specific course of study can be conceptualized through a structured diagrammatic technique? It was hypothesized that learners can benefit from this conceptualization in learning, especially in self‐regulated learning. The aim of this study was to investigate whether the ILOs represented in unstructured or structured formats can facilitate learners to identify learning paths. The results revealed that the mean ratings of all learning paths were statistically significantly higher with structured ILOs.  相似文献   
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