• Title/Summary/Keyword: PDE-5

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TOLERANCE AND PHARMACOKINETICS OF SINGLE-DOSE DA-8159, A SELECTIVE PDE5 INHIBITOR, IN HEALTHY MALES

  • Bahang , Mi-Young;Kang, Kyung-Koo;Ahn, Byoung-Ok;Shim, Hyun-Joo;Kim, Soon-Hae;Yoo, Moo-Hi;Kim, Won-Bae;Paick, Jae-Seung
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.249.2-250
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    • 2002
  • Tolerance and pharmacolinetics after single-dose administration of DA-8159, a new selective PDE5 inhibitor under phase 1 study, were examined in 42 healthy male volunteers in a six-period, double-blinded placebo-controlled study. Participants received single oral tablet of DA-8159 (12.5 to 300mg) or placebo. Adverse effects and pharmacokinetic parameters were monitored during experiments. DA-8159 was well tolerated and the frequency of adverse events was dose-related. (omitted)

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Effect of Phyto-Extract Fermented Mixture (MP119) on the Sexual Functions and on the Toxicities of Cadmium (식물추출복합발효물(MP119)이 성기능에 미치는 영향 및 카드뮴 독성에 대한 효과)

  • Jang, Young-Sun;Jeong, Jong-Moon
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.38 no.12
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    • pp.1724-1731
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    • 2009
  • This study was aimed to investigate the effect of phyto-extract fermented mixture (MP119) on the male sexual functions. The MP119 was evaluated for anti-impotency and anti-hypertensive effects via ACE (angiotensin converting enzyme) or PDE (phosphodiesterase) inhibition assay. $IC_{50}$ values of MP119 against ACE and PDE were 241.3${\pm}$35.5 ppm and 372.2${\pm}$33.8 ppm, respectively. To investigate the effect of testosterone expression by MP119, we performed cell media test using mouse Leydig-derived TM3 cells. Production of testosterone in TM3 cell was increased by MP119. Also, NO (nitric oxide) production of HUVEC (human umbilical vein endothelial cell) was increased when MP119 was added to the cultures. Forty male ICR mice were divided into 4 groups. MP119 was orally intubated for 7 days to group 1 and 3, and same volume of vehicle to group 2 and 4 as controls. After that, group 3 and 4 were intraperitoneally injected cadmium chloride at a single dose of 2 mg/kg. On the 8th experimental day, weights of testis, epididymis and seminal vesicle, number of sperm, concentrations of serum testosterone and cGMP were determined. The number of sperm, the concentrations of testosterone and cGMP were significantly increased in two experimental groups (group 1, 3). These results suggest that MP119 enhanced the sexual function of male mice, and could protect the sexual organs from the cadmium chloride as one of the endocrine disrupters.

Pharmacokinetics of KR-30075, A Potent Phosphodiesterase III Inhibitor in Rats (포스포디에스테라제 III의 저해물인 KR-30075의 흰쥐에서의 약물속도론)

  • Lee, Kwang-Pyo;Kim, Hyo-Jin;Kwon, Kwang-Il;Cho, Song-Ja
    • YAKHAK HOEJI
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    • v.36 no.3
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    • pp.259-268
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    • 1992
  • A procedure for the determination of KR-30075 and its metabolites in plasma and urine by high performance liquid chromatography is described. For the study of pharmacokinetic properties of KR-30075, a new PDE III inhibitor, the plasma concentration and urinary excretion after an oral administration of KR-30075 (4 mg/kg) in the male rat (Sprague Dawley) were determined by high performance liquid chromatography. The best extraction efficiency of KR-30075 and KR-30072 is obtained with ethyl ether adjusted to pH 4.0. Retention times of both KR-30072 and KR-30075 were within 5 min and resolution was complete at the flow rate of 1.0 ml/min. The sensitivity and specificity of this HPLC assay appears to be satisfactory for the pharmacokinetic study of KR-30075 and its metabolites. One-compartment open model with first-order absorption was applied to evaluate the pharmacokinetic parameters of KR-30075 according to Minimum AIC Estimation. $T_{max}$ was 1 hr, $C_{max}$ was $0.789{\pm}0.31\;{\mu}g/ml$ and elimination half $T_{1/2}$ was 6.31 min after oral administration of 4 mg/kg KR-30075 to male rats.

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An improved block matching algorithm for fast motion estimation (고속 움직임 추정을 위한 개선된 블록 정합 방식)

  • 문용호
    • The Journal of Korean Institute of Communications and Information Sciences
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    • v.28 no.5C
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    • pp.539-547
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    • 2003
  • According to the PDE scheme, it is desirable to make the value of SAD to be rapidly increased in motion estimation. In this paper, we propose a new block matching algorithm based on the combination of a new scan and search order. In the proposed scan order, a current block is divided by the frequency that is estimated by summing the difference between the mean and the values of the pixels. And then the calculation of SAD is performed from the highest frequency area. In the proposed search order based on DC difference between the current and the candidate block, candidate blocks with low DC are early checked in motion estimation. Simulation results show that the proposed method achieves about 6% computational gain compared with the conventional methods.

Improved measurement uncertainty of photon detection efficiency for single pixel Silicon photomultiplier

  • Yang, Seul Ki;Lee, Hye-Young;Jeon, Jina;Kim, Sug-Whan;Lee, Jik;Park, Il H.
    • The Bulletin of The Korean Astronomical Society
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    • v.37 no.2
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    • pp.210.1-210.1
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    • 2012
  • We report technique used for improved measurement uncertainties for Photon detection efficiency(PDE) of $1mm^2$ single pixel SiPM. It consists of 470nm LED light source, two 2-inch integrating sphere and two NIST calibrated silicon photodiodes that have ${\pm}2.4%$ calibration error. With raytracing simulation of our experimental setup, we predict number of photon into SiPM and measurement uncertainty. For MPPC, Hamamatsu suggested PDE(1600 micro pixel) including crosstalk and afterpulse is 23.5% at 470 nm. By using new low calibration error photodiode and raytracing simulation, our simulation result has ${\pm}3%$ measurement uncertainty. The technical detail of measurement, simulation are presented with the results and implication.

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Application of Light-emitting-diodes to Annular-type Photocatalytic Reactor for Removal of Indoor-level Benzene and Toluene

  • Jo, Wan-Kuen;Kang, Hyun-Jung;Kim, Kun-Hwan
    • Journal of Environmental Science International
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    • v.21 no.5
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    • pp.563-572
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    • 2012
  • Unlike water applications, the photocatalytic technique utilizing light-emitting-diodes as an alternative light source to conventional lamp has rarely been applied for low-level indoor air purification. Accordingly, this study investigated the applicability of UV-LED to annular-type photocatalytic reactor for removal of indoor-level benzene and toluene at a low concentration range associated with indoor air quality issues. The characteristics of photocatalyst was determined using an X-ray diffraction meter and a scanning electron microscope. The photocatalyst baked at $350^{\circ}C$ exhibited the highest photocatalytic degradation efficiencies(PDEs) for both benzene and toluene, and the photocatalysts baked at three higher temperatures(450, 550, and $650^{\circ}C$) did similar PDEs for these compounds. The average PDEs over a 3-h period were 81% for benzene and close to 100% for toluene regarding the photocatalyst baked at $350^{\circ}C$, whereas they were 61 and 74% for benzene and toluene, respectively, regarding the photocatalyst baked at $650^{\circ}C$. As the light intensity increased from 2.4 to 3.5 MW $cm^{-1}$, the average PDE increased from 36 to 81% and from 44% to close to 100% for benzene and toluene, respectively. In addition, as the flow rate increased from 0.1 to 0.5 L $min^{-1}$, the average PDE decreased from 81% to close to zero and from close to 100% to 7% for benzene and toluene, respectively. It was found that the annular-type photocatalytic reactor inner-inserted with UV-LEDs can effectively be applied for the decomposition of low-level benzene and toluene under the operational conditions used in this study.

The change of signaling pathway on the electrical stimulated contraction in streptozotocin-induced bladder dysfunction of rats

  • Han, Jong Soo;Min, Young Sil;Kim, Gil Hyung;Chae, Sang-hyun;Nam, Yoonjin;Lee, Jaehwi;Lee, Seok-Yong;Sohn, Uy Dong
    • The Korean Journal of Physiology and Pharmacology
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    • v.22 no.5
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    • pp.577-584
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    • 2018
  • Bladder dysfunction is a common complication of diabetes mellitus (DM). However, there have been a few studies evaluating bladder smooth muscle contraction in DM in the presence of pharmacological inhibitors. In the present study, we compared the contractility of bladder smooth muscle from normal rats and DM rats. Furthermore, we utilized pharmacological inhibitors to delineate the mechanisms underlying bladder muscle differences between normal and DM rats. DM was established in 14 days after using a single injection of streptozotocin (65 mg/kg, intraperitoneal) in Sprague-Dawley rats. Bladder smooth muscle contraction was induced electrically using electrical field stimulation consisting of pulse trains at an amplitude of 40 V and pulse duration of 1 ms at frequencies of 2-10 Hz. In this study, the pharmacological inhibitors atropine (muscarinic receptor antagonist), U73122 (phospholipase C inhibitor), DPCPX (adenosine $A_1$ receptor antagonist), udenafil (PDE5 inhibitor), prazosin (${\alpha}_1$-receptor antagonist), verapamil (calcium channel blocker), and chelerythrine (protein kinase C inhibitor) were used to pretreat bladder smooth muscles. It was found that the contractility of bladder smooth muscles from DM rats was lower than that of normal rats. In addition, there were significant differences in percent change of contractility between normal and DM rats following pretreatment with prazosin, udenafil, verapamil, and U73122. In conclusion, we suggest that the decreased bladder muscle contractility in DM rats was a result of perturbations in $PLC/IP_3$-mediated intracellular $Ca^{2+}$ release and PDE5 activity.

Uncovering Candidate Pathogenicity Genes in Erwinia pyrifoliae YKB12327 via Tn5-insertion Mutagenesis

  • Hualin Nie;Mi-Hyun Lee;Sanghee Lee;Seo-Rin Ko;Young-Soo Hong;Jae Sun Moon;Jun Myoung Yu;Ah-Young Shin;Suk-Yoon Kwon
    • Research in Plant Disease
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    • v.30 no.3
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    • pp.268-277
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    • 2024
  • Erwinia pyrifoliae is a gram-negative bacterial pathogen that commonly causes black shoot blight in pear and apple tree. Although the pathogenicity of this bacterial species is very similar to E. amylovora, there is no specific explanation of its pathogenic genes and mechanisms. In this study, our investigation into E. pyrifoliae pathogenicity involved generating seven YKB12327 mutant strains using Tn5 transposon mutagenesis. Observations revealed weakened growth rate and loss of pathogenicity in these mutants. Whole-genome sequencing and alignment analysis identified transposon insertions within the coding sequences of five strains and in the intergenic region of two strains. Annotation analysis elucidated genes directly or indirectly associated with pathogenicity. Notably, mutant strain MT16 displayed a transposon insertion mutation in the cyclic-di-GMP phosphodiesterase (pdeF) gene, a key player in bacterial signaling, governing microbial behavior and adaptation to environmental changes. Our findings provide insights into the genetic regulation of E. pyrifoliae pathogenicity, suggesting potential avenues for further research aimed at understanding and controlling this bacterial pathogen by targeting pdeF to mitigate apple black shoot blight disease.