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N-Methyl Amine-substituted Fluoxetine Derivatives: New Dopamine Transporter Inhibitors
Young Sil Yoon,Taesup Cho,Sung-Hwa Yoon,Churl Ki Min,Changho Lee 대한약학회 2009 Archives of Pharmacal Research Vol.32 No.12
Transport of dopamine (DA) by the dopamine transporter from the synaptic cleft into the presynaptic terminals plays a key role in terminating dopaminergic neurotransmission. The binding of psychostimulants to their recognition sites on the DA transporter leads to an inhibition of DA transport and a subsequent rising of the dopamine contents in the synaptic cleft is ascribed to a mode of psychostimulation. Discovery of dopamine transporter inhibitors would be useful with regard to substituting for cocaine and minimizing its abuse. Recently, a number of fluoxetine analogues were synthesized, especially focusing on the substitution of N-methyl amine group through modifying the structure of the fluoxetine, N-methyl-3-[p-trifluoromethylphenoxy]-3-phenylpropylamine, widely used as an antidepressant. Among them, the pharmacological properties of FD-2, (R)-N-ethanol-3-(4-trifluorophenoxy)-3-phenyl propaneamine and FD-4, N-(R)-3-trifluorophenoxy-3-phenylpropane-imidazole with a higher affinity for the DA transporter were characterized in terms of dopamine transporter inhibition expecting for useful cocaine substitutes. Effects of the compounds on [H3]dopamine uptake, [I125]RTI-55 binding, and DA transporter-associated currents were examined with the ligand binding assays and voltage clamping technique in human embryonic kidney (HEK)-293 cells where the recombinant human DA transporter (hDAT) was stably expressed. Our results showed that (i) fluoxetine was potent in inhibiting both the uptake of [H3]DA (IC50 = 0.21 ± 0.032 mM, n = 3) and the [I125]RTI-55 binding (IC50 = 0.23 ± 0.012 mM, n = 10); (ii) N-methyl amine substituted fluoxetine analogues, FD-2 and FD-4 were equally or more potent than fluoxetine itself in terms of inhibition of [H3]DA uptake (IC50 FD-2: 0.077 ± 0.0032 mM (n = 3); FD-4: 0.26 ± 0.13 mM (n = 3), inhibition of [I125]RTI-55 binding, and reduction in DA transporter-associated currents, suggesting that these analogues could be a new class of dopamine transporter inhibitors.
Changho Lee,Taejoo Lee,Yoon Suk Choi 대한금속·재료학회 2023 METALS AND MATERIALS International Vol.29 No.11
Machine learning of the creep rupture life dataset, which consists of test temperatures, stresses and rupture lives, receivedless attention in the community due to numerous physics-based and empirical models already available for the prediction ofthe creep rupture life, and a limited number (typically about 10 to 40) of available creep rupture life data points consideredto be too small to be trained for the reliable prediction. A simple data analytics approach was developed for the quick andreliable assessment of the creep rupture life. The proposed approach involves linear regression as a major algorithm and thefour features [two generic features (temperature (T) and stress (σ)) and two physics-informed features (ln σ and −1/T)], andexhibited superior creep rupture life predictions (validated by the 41 creep datasets of ferritic Cr steels) without any violationof creep phenomenology and data overfitting. In particular, the proposed approach was extremely useful to assess thefidelity of the Laron–Miller relation for a given creep rupture life dataset and to find an optimum Larson–Miller constantthat minimizes a deviation from the ideal Larson–Miller relation. An analytical model was also developed based on curvefitting of Larson–Miller parameters calibrated by the optimum Larson–Miller constant. The proposed analytical model gaveadditional improvement in creep rupture life prediction, particularly for creep datasets, of which creep rupture lives wereslightly less predicted by the data analytics approach. The two proposed models provided a synergistic effect in creep rupturelife prediction when interactively used.
尹相旭,金昌浩 동국대학교 농림과학연구소 1989 農林科學 論文集 Vol.13 No.-
This study was carried out to analyze the forest vegetational structure and the topographical distribution of trees in Mt. Odae national park. Eighteen sites, nine sites of the ridge part and nine sites of the glen part, were selected in the experimental forest of Mt. Odae. The result obtained are as follows : 1) Q. mongolica and Carpinus laxiflora showed the most high Importance Value in the ridge part and the glen part, respectively. For herbs, Arudinella hirta showed the most high Summed Dominance Ration in all the area, Festuca ovina the second high ratio in the ridge part, and Matteuccia struthiopteris the second in the glen part. 2) Species Diversity was most high in Plot 9 where was the intersection region of two vegetational types of the arid and the humid. Plot 10, the community of P. densiflora and Plot 16, the community of Carpinus laxiflora were completely different vegetational structure and topographical situation showing Similaraty Index of 0%. 3) As a result of analyzing Importance Values of each tree crown layers, thee age, D. B. H., succession of forest community of the area might be progressed toward Q. mongolica community in the ridge part and Carpinus laxiflora in the glen part for the present.
Extraction Optimization for Phlorotannin Recovery from the Edible Brown Seaweed Ecklonia Cava
Yoon, Minseok,Kim, Jin-Soo,Um, Min Young,Yang, Hyejin,Kim, Jiyoung,Kim, Yun Tai,Lee, Changho,Kim, Seon-Bong,Kwon, Sangoh,Cho, Suengmok Taylor Francis 2017 JOURNAL OF AQUATIC FOOD PRODUCT TECHNOLOGY Vol.26 No.7