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Structure-Activity Relationship and Functional Evaluation of Cannabinoid Type-1 Receptor

  • Shujie Wang;Xinru Tian;Suresh Paudel;Sungho Ghil;Choon-Gon Jang;Kyeong-Man Kim
    • Biomolecules & Therapeutics
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    • v.32 no.4
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    • pp.442-450
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    • 2024
  • The type-1 cannabinoid receptor (CB1R) is a potential therapeutic target in several pathological conditions, including neuropsychological disorders and neurodegenerative diseases. Owing to their structural diversity, it is not easy to derive general structure-activity relationships (SARs) for CB1R ligands. In this study, CB1R ligands were classified into six structural families, and the corresponding SAR was determined for their affinities for CB1R. In addition, we determined their functional activities for the activation of extracellular signal-regulated kinases (ERKs). Among derivatives of indol-3-yl-methanone, the highest ligand affinity was observed when a pentyl and a naphthalenyl group were attached to the N1 position of the indole ring and the carbon site of the methanone moiety, respectively. In the case of adamantane indazole-3-carboxamide derivatives, the presence of fluorine in the pentyl group, the substituent at the N1 position of the indazole ring, strongly increased the affinity for CB1R. For (naphthalen-1-yl) methanone derivatives, the presence of 4-alkoxynaphthalene in the methanone moiety was more beneficial for the affinity to CB1R than that of a heterocyclic ring. The functional activities of the tested compounds, evaluated through ERK assay, were correlated with their affinity for CB1R, suggesting their agonistic nature. In conclusion, this study provides valuable insight for designing novel ligands for CB1R, which can be used to control psychiatric disorders and drug abuse.

Inhalation Configuration Detection for COVID-19 Patient Secluded Observing using Wearable IoTs Platform

  • Sulaiman Sulmi Almutairi;Rehmat Ullah;Qazi Zia Ullah;Habib Shah
    • KSII Transactions on Internet and Information Systems (TIIS)
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    • v.18 no.6
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    • pp.1478-1499
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    • 2024
  • Coronavirus disease (COVID-19) is an infectious disease caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) virus. COVID-19 become an active epidemic disease due to its spread around the globe. The main causes of the spread are through interaction and transmission of the droplets through coughing and sneezing. The spread can be minimized by isolating the susceptible patients. However, it necessitates remote monitoring to check the breathing issues of the patient remotely to minimize the interactions for spread minimization. Thus, in this article, we offer a wearable-IoTs-centered framework for remote monitoring and recognition of the breathing pattern and abnormal breath detection for timely providing the proper oxygen level required. We propose wearable sensors accelerometer and gyroscope-based breathing time-series data acquisition, temporal features extraction, and machine learning algorithms for pattern detection and abnormality identification. The sensors provide the data through Bluetooth and receive it at the server for further processing and recognition. We collect the six breathing patterns from the twenty subjects and each pattern is recorded for about five minutes. We match prediction accuracies of all machine learning models under study (i.e. Random forest, Gradient boosting tree, Decision tree, and K-nearest neighbor. Our results show that normal breathing and Bradypnea are the most correctly recognized breathing patterns. However, in some cases, algorithm recognizes kussmaul well also. Collectively, the classification outcomes of Random Forest and Gradient Boost Trees are better than the other two algorithms.

Effect of Non-Agricultural Facilities on Water Quality and Contamination in Rural Area (농촌용수 수질관리를 위한 비농업시설의 영향 연구)

  • Lee, Byung-Sun;Um, Jae-Yeon;Kim, Yang-Bin;Woo, Nam-Chil;Nam, Kyoung-Phile;Lee, Jong-Min
    • Journal of Soil and Groundwater Environment
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    • v.14 no.2
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    • pp.1-9
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    • 2009
  • This study was objected to identify the effect on water quality and contamination by non-agricultural facilities in 'A' reservoir watershed located in OO city, Kyounggi-do, Korea. Ground- and stream water samples showed (Na+K)-Cl, Ca(Cl, SO$_4$) and Ca-Cl type in an illegally discharging area of sewage and a densely industrial area indicating water contamination. Stream water of an illegally discharging area of sewage had high COD, T-N and T-P. In this area, direct incoming of sewage into stream water was induced ground water system by well pumping, and it made a progress of ground water contaminations with those components. Groundwater of a densely industrial area showed high concentrations of T-N, NO$_3$N. From a nitrogen isotope analysis, stream water of an illegally discharging area of sewage has ${\delta}^{15}N-NO_3$values of 0.7%0 was strongly affected by nitrogen originated from agrochemicals, and a densely industrial area of 19.7%0 from septic system. Ground- and stream water of a livestock fanning area were contaminated with NH$_3$-N and Mn, which was affected by intensive livestock facilities. SAR-conductivity plot indicates the water does not pose either alkalinity or salinity hazard for irrigation. COD, T-N, T-P, NO$3$-N, NH$_3$N and Mn concentrations from contaminated areas were diminished by mixing with 'A' reservoir water. There were no water contaminations in silver towns, vacationlands around reservoir and golf links. Consequently, it should be made a plan of systematic managements for past and- present possible contaminants and sewage systems in preventing water contamination by non-agricultural facilities.

The Protective Effect of Lonicerae flos Extract on Cultured C6 Glioma Cells Damaged by Aluminum of Dementia Inducer (치매유발제인 알루미늄으로 손상된 배양 C6 Glioma 세포에 대한 금은화 추출물의 보호 효과)

  • Jung, Jai-Yun;Jung, In-Ju;Jekal, Seung-Joo
    • Korean Journal of Clinical Laboratory Science
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    • v.49 no.3
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    • pp.271-278
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    • 2017
  • This study was performed to evaluate the cytotoxicity of aluminum chloride ($AlCl_3$), and the protective effect of Lonicerae flos (LF) extract on $AlCl_3-induced$ cytotoxicity in the cultured C6 glioma cells. Here, the cell viability and antioxidative effects, such as DPPH-radical scavenging activity, superoxide anion scavenging activity, and lipid peroxidation (LP), were assessed. $AlCl_3$ significantly decreased the cell viability in a dose-dependent manner; the $XTT_{50}$ value was measured at $128.8{\mu}M$ of $AlCl_3$. The cytotoxicity of $AlCl_3$ was determined as highly toxic the y Borenfreund and Puerner's toxic criteria. The butylated hydroxytoluene (BHT) and antioxidant both significantly increased the cell viability, which was damaged by $AlCl_3-induced$ cytotoxicity in these cultures. In the protective effect of LF extract on $AlCl_3-induced$ cytotoxicity, the LF extract significantly increased the superoxide anion scavenging activity and inhibitory activity of LP, as well as the DPPH-radical scavenging activity. From these results, it is suggested that the oxidative stress may have been involved in the cytotoxicity of $AlCl_3$, and LP extract effectively protected $AlCl_3-induced$ cytotoxicity through the antioxidative effects. Conclusively, the natural resources, like LP extract, may be a putative therapeutic agent for the treatment of dementia induced by allergen like aluminum correlated with the oxidative stress.

Influences of Discharge Waters from Wastewater Treatment Plants on Rice (Oryza sativa L.) Growth and Percolation Water Salinity (폐수처리장 방류수 관개가 벼생육 및 침출수 염농도에 미치는 영향)

  • Shin, Joung-Du;Lee, Jong-Sik;Kim, Won-Il;Lee, Chang-Eun;Yun, Sun-Gang;Eom, Ki-Cheol
    • Korean Journal of Soil Science and Fertilizer
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    • v.36 no.1
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    • pp.24-31
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    • 2003
  • Objective of this study was to assess rice growth and percolation water salinity under the irrigation of the discharge waters from the municipal wastewater treatment plant and from the industrial wastewater treatment plant as alternative water resources during transplanting season. Three kinds of waters were irrigated; the discharge water from an industrial wastewater treatment plant (DIWT), the discharge water from the municipal wastewater treatment plant (DMWT), and groundwater. Concentrations of $COD_{er}$, $NH_4{^+}_-N$, $Mn^{2+}$, and $Ni^+$ in DIWT, SS content and $PO_4-P$ concentrations in DMWT were higher than those of reuse water criteria of other country for agricultural irrigation. The plant height in the irrigation of DMWT was shorter by 2 cm than the groundwater irrigation except for 10 days irrigation. However, the number of tillerings was not significantly different between DMWT and the groundwater. For the harvest index, there were no significant difference between DMWT and DIWT for 20 days irrigation, but slightly higher in DIWT than that of DMWT for 30 days irrigation regardless of soil types. The salinity of percolation water in the rhizosphere with irrigation of DIWT had more twofold than DMWT, but SAR value from DMWT had no significantly different from the groundwater irrigation. The average $EC_i$ values in the rooting zone irrigated with DIWT and DMWT for 30 days after rice transplanting were 4.7 and $3.4dS\;m^{-1}$ in clay loam soil, and were 3.5 and $2.5dS\;m^{-1}$ in sandy loam soil, respectively. There was dramatic decrease in $EC_i$ value at 30 days after rice transplanting even though $EC_i$ of DIWT had more twofold than DMWT. However, $EC_i$ from DMWT had no significant difference from the groundwater. Therefore, it might be considered that there was limited possibility to irrigate DMWT to overcome drought injury of rice transplanting season in paddy field.

A Study on Automated Lineament Extraction with Respect to Spatial Resolution of Digital Elevation Model (수치표고모형 공간해상도에 따른 선구조 자동 추출 연구)

  • Park, Seo-Woo;Kim, Geon-Il;Shin, Jin-Ho;Hong, Sang-Hoon
    • Korean Journal of Remote Sensing
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    • v.34 no.3
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    • pp.439-450
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    • 2018
  • The lineament is a linear or curved terrain element to discriminate adjacent geological structures in each other. It has been widely used for analysis of geology, mineral exploration, natural disasters, and earthquake, etc. In the past, the lineament has been extracted using cartographic map or field survey. However, it is possible to extract more efficiently the lineament for a very wide area thanks to development of remote sensing technique. Remotely sensed observation by aircraft, satellite, or digital elevation model (DEM) has been used for visual recognition for manual lineament extraction. Automatic approaches using computer science have been proposed to extract lineament more objectively. In this study, we evaluate the characteristics of lineament which is automatically extracted with respect to difference of spatial resolution of DEM. We utilized two types of DEM: one is Shuttle Radar Topography Mission (SRTM) with spatial resolution of about 90 m (3 arc sec), and the other is the latest world DEM of TerraSAR-X add-on for Global DEM with 12 m spatial resolution. In addition, a global DEM was resampled to produce a DEM with a spatial resolution of 30 m (1 arc sec). The shaded relief map was constructed considering various sun elevation and solar azimuth angle. In order to extract lineament automatically, we used the LINE module in PCI Geomatica software. We found that predominant direction of the extracted lineament is about $N15-25^{\circ}E$ (NNE), regardless of spatial resolution of DEM. However, more fine and detailed lineament were extracted using higher spatial resolution of DEM. The result shows that the lineament density is proportional to the spatial resolution of DEM. Thus, the DEM with appropriate spatial resolution should be selected according to the purpose of the study.

Clinical Assessment and Cephalometric Characteristics of Patients with Condylar Resorption in Teenagers (10대 하악과두흡수 환자의 임상적 평가 및 악안면 골격형태에 대한 연구)

  • Chun, Yong-Hyun;Hur, Yun-Kyung;Jung, Jae-Kwang;Chae, Jong-Moon;Choi, Jae-Kap
    • Journal of Oral Medicine and Pain
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    • v.35 no.1
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    • pp.61-73
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    • 2010
  • The aim of this study was to investigate clinical assessment and cephalometric characteristics in 10s patients with condylar resorption, who visited in the Department of Oral Medicine Kyungpook National University Hospital at 2006, by use of panorama, transcranial view and lateral cephalometric radiograph. The results were as follows; 1. Clinical assessment 1) Total number of patients were 59. Female was 47 and male was 12, Females were predominant and patient's age ranged from 12 to 19. 2) Most of the patients had Grade II condyle resorption. 3) The number of who had Class I occlusion was 27, which was the largest group. The number of patients with openbite was 20. Average overjet was 3.58mm and average overbite was 0.97mm. 4) Most of the patients had parafunctional habit. 5) The patients of showing the pain in condylar resortion was 41 and the case of not showing the pain was 18. 6) Treatment duration of 23 patients were less than 1 month, 28 patients were treated with supported therapy. 2. Cephalometric Characteristics 1) A 16-year-old female patients showed smaller SNA, SNB and larger articular angle significantly as compared with those of normal group. 2) A 17-year-old female patients showed smaller SN, SAr, TPFH, ramus height and larger SN-GoMe, FMA, articular angle significantly as compared with those of normal group. 3) Over 18 years old female patients showed smaller SN, SNB, TPFH, ramus height and larger ANB, FMA, SN-GoMe, LAFH, articular angle, gonial angle significantly as compared with those of normal group. 4) Over 18 years old male patients showed smaller SN, TPFH, ramus height and larger FMA, SN-GoMe, LAFH, articular angle, gonial angle significantly as compared with those of normal group. 5) There was no significant difference between 10s and normal group in mandibular body length.

A Study on Batch-Type Remote Plasma Dry Cleaning Process for Native Oxide Removal (배치식 플라즈마 세정 설비를 이용한 자연산화막 제거 공정)

  • Park, Jae-Young;Yi, Wook-Yeol;Hyung, Yong-Woo;Nam, Seok-Woo;Lee, Hyeon-Deok;Song, Chang-Lyong;Kang, Ho-Kyu;Roh, Yong-Han
    • Proceedings of the Korean Institute of Electrical and Electronic Material Engineers Conference
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    • 2004.11a
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    • pp.247-251
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    • 2004
  • 반도체 소자의 제조에 있어 실리콘 표면에 성장한 자연산화막을 제거하기 위해 일반적으로 습식 세정 기술이 이용되어 왔다. 하지만 소자의 최소 선폭(design rule)이 nano급으로 고집적화 됨에 따라 contact hole 바닥의 자연산화막을 깨끗이 제거하는데 있어서 그 한계를 나타나고 있다. 이에 대한 효과적인 대안 공정으로 가스 건식 세정 기술이 연구되고 있다. 본 논문에서는 한 번에 50매 이상의 웨이퍼를 처리함으로써 생산성 측면에서 월등한 배치식 설비에서 원거리 플라즈마(remote plasma) 장치에서 2.450Hz의 마이크로웨이브(${\mu}$-wave)에 의해 형성시킨 수소라디칼과 $NF_3$ 가스를 이용하여 실리콘에 결함을 주지 않고 자연산화막을 선택적으로 제거하는 공정에 대해 고찰하였다. AFM을 이용한 표면분석, TEM을 이용한 물성분석, 그리고 ToF-SIMS 및 XPS를 이용한 화학 분석을 습식 및 건식 세정을 비교 평가한 결과, 건식 세정 공정이 실리콘 표면에 결함을 주지 않고 자연산화막을 제거 할 수 있음을 확인하였다. 산화막$(SiO_2)$, 질화막$(Si_3N_4)$, 그리고 다결정 실리콘(Poly-Si) 등의 각 막질별 식각 특성을 고찰하였으며, $NH_3$의 캐리어 가스인 $N_2$의 주입량을 조절함으로써 수소라디칼 형성 효율의 개선이 가능하였으며, 이로부터 게이트와 소스/드레인 사이를 절연하기 위해 이용되는 질화막의 식각 선택비를 2배 정도 개선할 수 있었다. nano급 소자에 실장하여 평가한 결과에서 불산(HF)에 의한 습식 세정 방식에 비하여 약 $20{\sim}50%$ 정도의 contact 저항 감소 효과가 있음이 확인되었다.두 소자 모두 $40mA/cm^2$ 에서 이상적인 화이트 발란스와 같은(0.33,0.33)의 색좌표를 보였다.epsilon}_0=1345$의 빼어난 압전 및 유전특성과 $330^{\circ}C$의 높은 $T_c$를 보였고 그 조성의 vibration velocity는 약4.5 m/s로 나타났다.한 관심이 높아지고 있다. 그러나 고 자장 영상에서의 rf field 에 의한 SAR 증가는 중요한 제한 요소로 부각되고 있다. 나선주사영상은 SAR 문제가 근원적으로 발생하지 않고, EPI에 비하여 하드웨어 요구 조건이 낮아 고 자장에서의 고속영상방법으로 적합하다. 본 논문에서는 고차 shimming 을 통하여 불균일도를 개선하고, single shot 과 interleaving 을 적용한 multi-shot 나선주사영상 기법으로 $100{\times}100$에서 $256{\times}256$의 고해상도 영상을 얻어 고 자장에서 초고속영상기법으로 다양한 적용 가능성을 보였다. 연구에서 연구된 $[^{18}F]F_2$가스는 친핵성 치환반응으로 방사성동위원소를 도입하기 어려운 다양한 방사성의 약품개발에 유용하게 이용될 수 있을 것이다.었으나 움직임 보정 후 영상을 이용하여 비교한 경우, 결합능 변화가 선조체 영역에서 국한되어 나타나며 그 유의성이 움직임 보정 전에 비하여 낮음을 알 수 있었다. 결론: 뇌활성화 과제 수행시에 동반되는 피험자의 머리 움직임에 의하여 도파민 유리가 과대평가되었으며 이는 이 연구에서 제안한 영상정합을 이용한 움직임 보정기법에 의해서 개선되었다. 답이 없는 문제, 문제 만들기, 일반화가 가능한 문제 등으로 보고, 수학적 창의성 중 특히 확산적 사고에 초점을 맞추어 개방형 문제가 확

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Clinical Assessment, Panoramic and MRI Findings and Cephalometric Characteristics of Patients with Condylar Resorption (과두흡수환자의 자기공명영상 사진 평가 및 악안면 골격형태에 대한 연구)

  • Jang, Heon-Su;Hur, Yun-Kyung;Kim, Kyun-Yo;Ko, Yu-Jeong;Chae, Jong-Moon;Choi, Jae-Kap
    • Journal of Oral Medicine and Pain
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    • v.34 no.4
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    • pp.409-420
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    • 2009
  • The aim of this study was to investigate clinical assessment, panorama & MRI findings and cephalometric characteristics in 42 patients with condylar resorption, who visited in the Department of Oral Medicine Kyungpook National University Hospital at 2006. The results were as follows; 1. Clinical assessment 1) Female was 34 and male was 8, females were predominant. Distribution of age showed as follows; 10s was 14, 20s was 13, 30s was 7, 40s was 3, 50s was 4 and 60s was 1 patient. 10s and 20s were predominant. 2) Most of the patients had parafunctional habit. 2. Findings of panorama & MRI 1) Most of the patients had degree of Grade II condylar resorption by panorama taking. 2) Most of the patients had disc dislocation and belonged to the degree of stage IV by MRI taking. 3. Cephalometric Characteristics 1) SN, SAr and saddle angle in female patients were significantly smaller and SN in male patients showed only significantly smaller than normal group. 2) SNA showed no difference from the normal group in both patients. SNB was smaller and ANB was lager in female patients than normal group. 3) SN-GoMe and FMA increased in patients. 4) Total posterior facial height & ramus height were significantly smaller. 5) Mandibular body length did not show any significant difference.

Analysis of Sea Route to the Jangbogo Antarctic Research Station by using Passive Microwave Sea Ice Concentration Data (수동 마이크로파 해빙 면적비 자료를 이용한 남극 장보고 과학기지로의 항해경로 분석)

  • Kim, Yeonchun;Ji, Yeonghun;Han, Hyangsun;Lee, Joohan;Lee, Hoonyol
    • Korean Journal of Remote Sensing
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    • v.30 no.5
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    • pp.677-686
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    • 2014
  • Sea ice covers wide area in Terra Nova Bay in East Antarctica where the Jangbogo Antarctic Research Station was built in 2014, which affects greatly on the sailing of an icebreaker research vessel. In this study, we analyzed the optimum sea route and sailable period of the icebreaker to visit the Jangbogo Antarctic Research Station by using sea ice concentration data observed by passive microwave sensors such as Special Sensor Microwave/Imager (SSM/I) and Special Sensor Microwave Imager/Sounder (SSMIS) for the last decade, and by using sea route of the Araon, an icebreaker of Republic of Korea, from 2010 to 2012. It is found that Araon sailed in the route of sea ice concentration up to 78%. Sailing speed of the Araon decreased due to increasing sea ice concentration. However, Araon maintained the speed close to the average speed for the entire sailing period (~11 kn) in the route of sea ice concentration up to 70%. Therefore, we confirm that the Araon can sail typically in the route which shows sea ice concentration below 70%. We derived annually available sailing period in recent 10 years for the sea route of the Araon in 2010, 2011 and 2012, which is defined as the period showing sea ice concentration below 70% through the route. Maximum sailable period was analyzed to be 61 and 62 days for the route of the Araon in 2010 and 2011, respectively. However, the typical sailing in the routes was unavailable in some years because sea ice concentration was higher than 70% through the routes. Meanwhile, the sailable period for the routes of the Araon in 2012 was observed in every year, which was a minimum of 15 days and is a maximum of 89 days. Therefore, we could suggest that optimum route of icebreaker to visit the Jangbogo Antarctic Research Station is the route of the Araon in 2012. High resolution images from SAR or optical sensors are necessary to investigate sea ice condition near shoreline of Jangbogo research station due to several kilometers of low resolution of sea ice concentration.