• Title/Summary/Keyword: Time-activity curve

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Antihypertensive activity of KR-31081, an orally active nonpeptide AT1 receptor antagonist (안지오텐신 수용체 리간드 KR-31081의 생체 내 활성에 관한 연구)

  • Lee, Sung-Hou
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.10 no.11
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    • pp.3473-3479
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    • 2009
  • The pharmacological profile of KR-31081, a newly synthesized AT1 receptor antagonist, was evaluated in pithed rats, conscious renal hypertensive rats (RHRs) and conscious furosemide-treated beagle dogs. In pithed rats, KR-31081 (i.v.) induced a non-parallel right shift in the dose-pressor response curve to angiotensin II (ID50: 0.05 mg/kg) with a dose-dependent reduction in the maximum responses; this antagonistic effect was about 40 times more potent than losartan (ID50: 1.74 mg/kg) which showed competitive antagonism. KR-31081 did not alter the responses induced by other agonists such as norepinephrine and vasopressin. In RHRs, orally given KR-31081 produced a dose-dependent and long-lasting (>24 h) antihypertensive effect with a higher potency to losartan (ED20: 0.30 and 3.36 mg/kg, respectively). In furosemide-treated dogs, orally given KR-31081 produced a dose-dependent and long-lasting (>8h) antihypertensive effect with a rapid onset of action (time to Emax: 1-1.5 h) and 20-fold greater potency than losartan (ED20: 0.41 and 8.13 mg/kg, respectively). These results suggest that KR-31081 is a potent, orally active AT1 receptor antagonist useful for the research and diagnostic tools as an added exploratory potential.

Efficiency Analysis of Hand Cycle Utilizing Vital Sign (생체 신호를 이용한 핸드사이클의 효율성 분석)

  • Yi, Jae-Hoon
    • Journal of Digital Contents Society
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    • v.19 no.7
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    • pp.1297-1302
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    • 2018
  • Propose of this study was to compared and analyzes the cranking between the newly developed hand cycle prototype and the hign-end hand cycle that are sold on the market for the disabled athletes. For this study, 10 male subjects, who had the same type of disability, were selected from the Korea Disabled Cycle Federation. 12 infrared camera(Oqus-500) was utilized to acquire the subjects' kinematic data. we have analyzed the data of 30 seconds - 15 seconds before and after cranking. SPSS 16 was used for a statistical verification and the difference of the sports biomechanical variable between RX and the prototype was verified by utilizing pared samples t-test. The significance level at the time of the experiment was ${\alpha}=.05$. The results show that there is a need to design the hand cycle crank in a curve shape to lessen the muscle fatigue that is measured the highest between the angle of 180 to 195. In addition, comparative analysis between the existing data and the data of modified crank must be researched since the hand cycle cranking is one of the main variables in performance enhancement.

A prebiotic fiber increases the formation and subsequent absorption of compound K following oral administration of ginseng in rats

  • Kim, Kyung-Ah;Yoo, Hye Hyun;Gu, Wan;Yu, Dae-Hyung;Jin, Ming Ji;Choi, Hae-Lim;Yuan, Kathy;Guerin-Deremaux, Laetitia;Kim, Dong-Hyun
    • Journal of Ginseng Research
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    • v.39 no.2
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    • pp.183-187
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    • 2015
  • Background: Gut microflora play a crucial role in the biotransformation of ginsenosides to compound K (CK), which may affect the pharmacological effects of ginseng. Prebiotics, such as NUTRIOSE, could enhance the formation and consequent absorption of CK through the modulation of gut microbial metabolic activities. In this study, the effect of a prebiotic fiber (NUTRIOSE) on the pharmacokinetics of ginsenoside CK, a bioactive metabolite of ginsenosides, and its mechanism of action were investigated. Methods: Male Sprague-Dawley rats were given control or NUTRIOSE-containing diets (control diet + NUTRIOSE) for 2 wk, and ginseng extract or vehicle was then orally administered. Blood samples were collected to investigate the pharmacokinetics of CK using liquid chromatography-tandem mass spectrometry. Fecal activities that metabolize ginsenoside Rb1 to CK were assayed with fecal specimens or bacteria cultures. Results: When ginseng extract was orally administered to rats fed with 2.5%, 5%, or 10% NUTRIOSE containing diets, the maximum plasma concentration ($C_{max}$) and area under the plasma concentration-time curve values of CK significantly increased in a NUTRIOSE content-dependent manner. NUTRIOSE intake increased glycosidase activity and CK formation in rat intestinal contents. The CK-forming activities of intestinal microbiota cultured in vitro were significantly induced by NUTRIOSE. Conclusion: These results show that prebiotic diets, such as NUTRIOSE, may promote the metabolic conversion of ginsenosides to CK and the subsequent absorption of CK in the gastrointestinal tract and may potentiate the pharmacological effects of ginseng.

Cell-Free miR-27a, a Potential Diagnostic and Prognostic Biomarker for Gastric Cancer

  • Park, Jong-Lyul;Kim, Mirang;Song, Kyu-Sang;Kim, Seon-Young;Kim, Yong Sung
    • Genomics & Informatics
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    • v.13 no.3
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    • pp.70-75
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    • 2015
  • MicroRNAs (miRNAs) have been demonstrated to play an important role in carcinogenesis. Previous studies revealed that miRNAs are present in human plasma in a remarkably stable form that is protected from endogenous RNase activity. In this study, we measured the plasma expression levels of three miRNAs (miR-21, miR-27a, and miR-155) to investigate the usefulness of miRNAs for gastric cancer detection. We initially examined plasma miRNA expression levels in a screening cohort consisting of 15 patients with gastric cancer and 15 healthy controls from Korean population, using TaqMan quantitative real-time polymerase chain reaction. We observed that the expression level of miR-27a was significantly higher in patients with gastric cancer than in healthy controls, whereas the miR-21 and miR-155a expression levels were not significantly higher in the patients with gastric cancer. Therefore, we further validated the miR-27a expression level in 73 paired gastric cancer tissues and in a validation plasma cohort from 35 patients with gastric cancer and 35 healthy controls. In both the gastric cancer tissues and the validation plasma cohort, the miR-27a expression levels were significantly higher in patients with gastric cancer. Receiver-operator characteristic (ROC) analysis of the validation cohort, revealed an area under the ROC curve value of 0.70 with 75% sensitivity and 56% specificity in discriminating gastric cancer. Thus, the miR-27a expression level in plasma could be a useful biomarker for the diagnosis and/or prognosis of gastric cancer.

Measurement of Finger Blood Flow in Raynaud's Phenomenon by Radionuclide Angiography (레이노드 현상에서 수지혈류 측정에 관한 연구)

  • Lim, Sang-Moo;Chung, June-Key;Lee, Myung-Chul;Choi, Sung-Jae;Koh, Chang-Soon;Kim, Sang-Joon
    • The Korean Journal of Nuclear Medicine
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    • v.21 no.2
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    • pp.183-190
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    • 1987
  • In Raynaud's phenomenon, the authors measured finger blood flow after ice water exposure by analyzing the time activity curve of radionuclide angiography on both hands. The results were as follows: 1) The digital blood flow did not decrease after ice water exposure in normal subjects. 2) In the patients with Raynaud's phenomenon, there were two groups: the one had decreased digital blood flow after cold exposure, and the other had paradoxically increased digital blood flow after cold exposure. 3) There was no difference in the digital blood flow of hand in room temperature between the normal and the patients with reduced digital blood flow after cold exposure, but the digital blood flow of the hand in room temperature was markedly reduced in the patients with paradoxically increased flow after cold exposure. 4) In the static image the difference was not significant in comparision with the dynamic study, because it represents pooling of the blood in the vein rather than flow. 5) After the treatment with nifedipine, the digital blood flow increased. In conclusion, the radionuclide angiography was useful in measuring the digital blood flow in Raynaud's phenomenon, and further studies with various drugs is expected.

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The role of calmodulin in regulating calcium-permeable PKD2L1 channel activity

  • Park, Eunice Yon June;Baik, Julia Young;Kwak, Misun;So, Insuk
    • The Korean Journal of Physiology and Pharmacology
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    • v.23 no.3
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    • pp.219-227
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    • 2019
  • Polycystic kidney disease 2-like-1 (PKD2L1), polycystin-L or transient receptor potential polycystin 3 (TRPP3) is a TRP superfamily member. It is a calcium-permeable non-selective cation channel that regulates intracellular calcium concentration and thereby calcium signaling. Although the calmodulin (CaM) inhibitor, calmidazolium, is an activator of the PKD2L1 channel, the activating mechanism remains unclear. The purpose of this study is to clarify whether CaM takes part in the regulation of the PKD2L1 channel, and if so, how. With patch clamp techniques, we observed the current amplitudes of PKD2L1 significantly reduced when co-expressed with CaM and $CaM{\triangle}N$. This result suggests that the N-lobe of CaM carries a more crucial role in regulating PKD2L1 and guides us into our next question on the different functions of two lobes of CaM. We also identified the predicted CaM binding site, and generated deletion and truncation mutants. The mutants showed significant reduction in currents losing PKD2L1 current-voltage curve, suggesting that the C-terminal region from 590 to 600 is crucial for maintaining the functionality of the PKD2L1 channel. With PKD2L1608Stop mutant showing increased current amplitudes, we further examined the functional importance of EF-hand domain. Along with co-expression of CaM, ${\triangle}EF$-hand mutant also showed significant changes in current amplitudes and potentiation time. Our findings suggest that there is a constitutive inhibition of EF-hand and binding of CaM C-lobe on the channel in low calcium concentration. At higher calcium concentration, calcium ions occupy the N-lobe as well as the EF-hand domain, allowing the two to compete to bind to the channel.

A Study on the Radionuclide Cardiac Angiography in the Various Heart Diseases (각종(各種) 심질환(心疾患)에서 방사성(放射性) 동위원소(同位元素) 심혈관촬영술(心血管撮影術)에 관한 연구(硏究))

  • Chung, June-Key;Park, Sun-Yang;Ryu, Park-Young;Cho, Bo-Yeon;Kim, Byoung-Kuk;Koh, Chang-Soon
    • The Korean Journal of Nuclear Medicine
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    • v.13 no.1_2
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    • pp.7-14
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    • 1979
  • Radionuclide cardiac angiography has distinct advantages in safety, patient comfort, cost and ease of performance. This method offers diagnostic accuracy equivalent to that of cardiac catheterization. By this method the qualitative and quantitative diagnosis of the cardiac shunts are available. Also for it is repeatable with ease and more physiologic, it has application in following pre- and post-operative shunt patients. We performed the radionuclide cardiac angiographies in 147 cases of heart diseases and 26 cases of normal group. 1. The detection of left-to-right shunt was possible in 22 of 24 patients, and 2 patients were not diagnosed due to small shunt amount. (Qp/Qs<1.3) In 21 patients of right-to-left shunt, all were diagnosed by radionuclide cardiac angiography. 2. With the pulmonary time-activity curve, $C_2/C_1$ ratio was calculated. In normal control group, a range of $C_2/C_1$ ratios of $21{\sim}38%$ was established with a mean value of $28.6{\pm}4.6%$. In patients with left-to-right shunts determined by catheterization data, the range of $C_2/C_1$ ratio was $33{\sim}90%$, with a mean value of $67.8{\pm}12.2%$. 3. In 8 cases of left-to-right shunt, $Q_p/Q_s$ ratios determined by radionuclide cardiac angiography were compaired with those of cardiac catheterization. The correlation coefficient was 0.907. (P<0.001) 4. Postoperative radionuclide cardiac angiographies were done in 21 cases. 3 of 13 patients with left-to-right shunts were found to have residual shunts. 8 patients with right-to-left shunts were confirmed to have no residual shunt.

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A Study of Cesium Removal Using Prussian Blue-Alginate Beads (프러시안 블루-알지네이트 비드를 이용한 세슘 제거 연구)

  • So-on Park;Su-jung Min;Bum-kyoung Seo;Chang-hyun Roh;Sang-bum Hong
    • Journal of Radiation Industry
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    • v.18 no.1
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    • pp.89-93
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    • 2024
  • Accidents at nuclear facilities and nuclear power plants led to leaks of large amounts of radioactive substances. Of the various radioactive nuclides released, 137Cs are radioactive substances generated during the fission of uranium. Therefore, due to the high fission yield (6.09%), strong gamma rays, and a relatively long half-life (30 years), a rapid and efficient removal method and a study of adsorbents are needed. Accordingly, an adsorbent was prepared using Prussian blue (PB), a material that selectively adsorbs radioactive cesium. As a result of evaluating the adsorption performance with the prepared adsorbent, it was confirmed that 82% of the removal efficiency was obtained, and most of the cesium was rapidly adsorbed within 10 to 15 minutes. The purpose of this study was to adsorb cesium using the Prussian blue alginate bead and to compare the change in detection efficiency according to the amount of adsorbent added for quantitative evaluation. However, in this case, it is difficult to determine the detection efficiency using a standard source with the same conditions as the measurement sample, so the efficiency change of the HPGe detector according to the different heights of Prussian blue was calculated through MCNP simulation using certified standard materials (1 L, Marinelli beaker) for radioactivity measurement. It is expected to derive a relational equation that can calculate detection efficiency through an efficiency curve according to the volume of Prussian blue, quantitatively evaluate the activity at the same time as the adsorption of radioactive nuclides in actual contaminated water and use it in the field of nuclear facility operation and dismantling in the future.

A Comparative Analysis of GBEF According to Image Aquisition Method in Hepatobiliary Scan (간담도스캔의 영상수집방법에 따른 담즙배출율의 비교분석)

  • Kim, Yeong-Seon;Seo, Myeong-Deok;Lee, Wan-Kyu;Song, Jae-Beom
    • The Korean Journal of Nuclear Medicine Technology
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    • v.18 no.2
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    • pp.8-16
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    • 2014
  • Purpose The quantitative analysis of gallbladder emptying is very important in diagnosis of motility disorder of gallbladder and in biliary physiology. The GBEF obtain the statics aquisition method or the dynamic acquisition method in two ways. The purpose of this study is to compare the GBEF value of statics acquisition method and the dynamic acquisition method. And we find the best way for calculate GBEF. Materials and Methods The quantitative hepatobiliary scan with $^{99m}Tc$-mebrofenin was performed of 27 patients. Initial images were acquired statically, for 60 min after injection of the radioactive tracer. And if the gallbladder is visualized to 60 min, performed stimulation of gallbladder (1egg, 200 mL milk). After that, started acquisition of dynamic image for 30 min. After that, image of after fatty meal of the statics method were acquired on equal terms with 60 min image. The statics GBEF was calculated using the images of before fatty meal and post fatty meal by the statics method. The dynamic GBEF was calculated using the images of time of maximum bile juice uptake ($T_{max}$) and time of minimum bile juice uptake ($T_{min}$) images from the gallbladder time-activity curve. A bile juice is secreted from gallbladder while eating a fatty meal. that is named early GBEF and that was calculated using before fatty meal image of the statics method and 1 min image of the dynamic method. Results The result saw very big difference between two according to $T_{max}$. The result, were as follows. 1) In case of less than 1 min, the dynamic mean GBEF was $40.1{\pm}21.7%$, the statics mean GBEF was $51.5{\pm}23.6%$ in 16 cases. The early mean GBEF was $14.0{\pm}29.1%$. The GBEF of statics method was higher because that include secreted bile juice while performed stimulation of gallbladder. A difference of GB counts according to acquisition method and the early bile juice counts was $17.6{\pm}14.8%$ and $13.5{\pm}15.3%$. 2) In case of exceed than 1 min, the dynamic mean GBEF was $31.0{\pm}19.7%$, the statics mean GBEF was $21.3{\pm}19.4%$ in 7 cases. The early GBEF was $-6.9{\pm}4.9%$. The GBEF of dynamic method was higher because that include concentrated bile juice to $T_{max}$. A difference of GB counts according to acquisition method and the early bile juice counts was $14.3{\pm}7.3%$ and $5.9{\pm}3.9%$. Conclusion The statics method is very easy and simple, but in case of $T_{max}$ delay, the GBEF can be lower. The dynamic method is able to calculate accurately in case of $T_{max}$ delay, but in case of $T_{max}$ is less than 1 min, the GBEF can be lower because dynamic GBEF exclude secreted bile juice while performed stimulation of gallbladder. The best way to calculate GBEF is to scan with dynamic method preferentially and to choose suitable method between the two way after conform $T_{max}$ on the T-A curve of the dynamic method.

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Analysis of Left Ventricular Functional Parameters in Normal Korean Subjects by ECG Gated Blood Pool Scan (정상 한국인에서 게이트혈액풀스캔을 이용한 좌심실 심기능지표들의 분석)

  • Kang, Jae-Hwang;Park, Une-Sook;Kang, Byeong-Sun;Lim, Hyeon-Ok;Choi, Dong-Soo;Suh, Bong-Kwan;Chung, Soon-Il;Lee, Keun-Woo
    • The Korean Journal of Nuclear Medicine
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    • v.28 no.1
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    • pp.52-61
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    • 1994
  • Background : The demand for refinement in noninvasive and quantitative assessment of left ventricular (LV) function is increasing. Purpose : To assess normal values of left ventricular functional parameters during both systole and diastole by scintigraphic method using computerized triple-head gamma camera and to evaluate correlations between these parameters. Methods : ECG gated blood pool scan with $^{99m}Tc$-Human serum albumin was performed in 94 normal Korean subjects. Ejection fraction (EF), systolic parameters [peak emptying rate (PER), average emptying rate (AER), time to peak emptying rate (TPER)], and diastolic parameters [peak filling rate (PFR), average filling rate (AFR), time to peak filling rate (TPFR)] were obtained by analysis of LV time-activity curve, the correlation of these parameters to the age and sex, and the correlation between these parameters were evaluated. Results : 1) Mean value of ejection fraction in study subjects was $59.6{\pm}5.25%$ and showed no significant correlation to age (r=-0.08) and sex but showed most pronounced correlation to PFR (r=0.46, p<0.001), PER (r=0.41, p<0.001), AFR (r=0.34, p<0.001) and AER (r=0.28, p<0.01). 2) Mean values of systolic parameters were as follows: $PER=3.22{\pm}0.50$ end-diastolic volume/sec, $AER=2.22{\pm}0.45$ end-diastolic volume/sec, $TPER=103.5{\pm}29.30$ msec. They showed no significant correlation to age and sex. 3) Mean values of diastolic parameters were as follows: $PFR=2.71{\pm}0.51$ end-diastolic volume/sec, $AFR=1.83{\pm}0.44$ end-diastolic volume/sec, $TPFR=132.1{\pm}33.45$ msec. They showed strong correlation to age (r=0.70, -0.64, 0.37, p<0.001). Conclusions : Left ventricular functional parameters in normal Korean subjects were obtained reliably by computerized scintigraphic method and may be applied to the evaluation of cardiac function in diseased patients.

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