• 동의생리병리학회지
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• 제31권6호
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• pp.341-347
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• 2017

To investigate the effect of Corni Fructus(CF) water extracts on the relaxation of the corpus cavernosum, organ bath studies, histochemical and immunohistochemical methods were used and obtained the following results. In the organ bath study, the maximal contraction of the corpus cavernosum tissue by PE showed a significant relaxation effect at $3.0mg/m{\ell}$ of CF water extract. When ${\text\tiny{L}}$-NNA was pretreated corpuscular relaxation effect of CF water extract was significantly inhibited compared without ${\text\tiny{L}}$-NNA pretreatment. In $Ca^{2+}$-free solution, the increase of contraction due to $Ca^{2+}$ influx significantly inhibited in the pretreatment compared with no pretreatment of CF water extract. Histochemical and immunohistochemical studies showed that the ratio of smooth muscle to collagen fiber was increased in the CF group compared to the PE group in the corpus cavernosum, and the eNOS positive reaction increased and the PDE5 positive reaction decreased. These results suggest that CF extract has increased NO production through activation of eNOS and inhibited the action of PDE5 to block the extracellular $Ca^{2+}$ influx, thereby relaxing the smooth muscle of the corpus cavernosum.

• The Korean Journal of Physiology and Pharmacology
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• 제10권3호
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• pp.149-154
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• 2006

Selective inhibition of phosphodiesterase (PDE) 5 opened a new therapeutic approach for cardiovascular disorders. Therefore, the effect of PDE5 inhibition on the cardiac function should thoroughly be defined. The purpose of the present study was to define the effects of sildenafil, a selective inhibitor of PDE5, on the atrial cGMP efflux, atrial dynamics, and the release of atrial natriuretic peptide (ANP). By perfusing rabbit left atria to allow atrial pacing, changes in atrial stroke volume and pulse pressure, transmural extracellular fluid translocation, cGMP efflux, and ANP secretion were measured. SIN-I, an NO donor and soluble (s) guanylyl cyclase (GC) activator, and C-type natriuretic peptide (CNP), an activator of particulate (p) GC activator, were used. Sildenafil increased basal levels of cGMP efflux slightly but not significantly. Sildenafil in a therapeutic dose increased atrial dynamics (for atrial stroke volume, $2.84{\pm}1.71%$, n=12, vs $-0.71{\pm}0.86%$, n=21; p<0.05) and decreased ANP release ($-9.02{\pm}3.36%$, n=14, vs $1.35{\pm}3.25%$, n=23; p < 0.05), however, it had no effect on the SIN-1- or CNP-induced increase of cGMP levels. Furthermore, sildenafil in a therapeutic dose accentuated SIN-1-induced, but not CNP-induced, decrease of atrial pulse pressure and ANP release. These data indicate that PDE5 inhibition with sildenafil has a minor effect on cGMP levels, but has a distinct effect on pGC-cGMP- and sGC-cGMP-induced contractile and secretory function.

• 공업화학
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• 제5권3호
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• pp.466-477
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• 1994

흡습성, 유연성 및 대전방지 효능을 지닌 것으로 알려진 PEG 600과 에퍼클로로히드린을 $BF_3$ 촉매로서 반응시켜 PEG 600-diglycidyl ether(PDE)를 합성하였다. 다음 PDE에 높은 전도성의 지방족 아민이며 경화제인 트리에틸렌테트라민으로서 공반응시켜 수용성인 긴 사슬의 폴리아민(PDET)을 얻고, PDET의 겔화방지와 수용액 안정성을 좋게 하기 위하여 아세트산프로 양이온화시켜 수용성의 제4급 암모늄 폴리아민(PDETA)을 합성하였다. 위에서 각각 합성된 PDET-2, -5, -6과 PDETA-2, -4에 각각 물을 첨가하여 대전방지제 PDET-2A, -5A, -6A, PDETA-2A, -4A를 제조하였다. 제조된 대전방지제를 PET 직물에 단독 혹은 수지병용으로 처리한 후 세탁횟수에 따른 표면전기저항과 반감기 특성의 시험결과, PDETA-2A와 -4A는 50회 세탁 후에도 대전방지 성능에 큰 변화가 없어서 내구성 대전방지제임을 확인하였다. 또한 세탁전의 표면전기저항 간이 각각 $1{\times}10^7{\Omega}$, $2{\times}10^7{\Omega}$이었고, 반감기 특성값은 0.8초와 1.1초로 나타나 양호한 대전방지제임이 입증되었다.

• Biomolecules & Therapeutics
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• 제28권4호
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• pp.328-336
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• 2020

Diabetes mellitus affects the colonic motility developing gastrointestinal symptoms, such as constipation. The aim of the study was to examine the role of intracellular signaling pathways contributing to colonic dysmotility in diabetes mellitus. To generate diabetes mellitus, the rats were injected by a single high dose of streptozotocin (65 mg/kg) intraperitoneally. The proximal colons from both normal and diabetic rats were contracted by applying an electrical field stimulation with pulse voltage of 40 V in amplitude and pulse duration of 1 ms at frequencies of 1, 2, 4, and 6 Hz. The muscle strips from both normal rats and rats with diabetes mellitus were pretreated with different antagonists and inhibitors. Rats with diabetes mellitus had lower motility than the control group. There were significant differences in the percentage of inhibition of contraction between normal rats and rats with diabetes mellitus after the incubation of tetrodotoxin (neuronal blocker), atropine (muscarinic receptor antagonist), prazosin (α₁ adrenergic receptor antagonist), DPCPX (adenosine A1 receptor antagonist), verapamil (L-type Ca²⁺ channel blocker), U73122 (PLC inhibitor), ML-9 (MLCK inhibitor), udenafil (PDE₅ inhibitor), and methylene blue (guanylate cyclase inhibitor). The protein expression of p-MLC and PDE₅ were decreased in the diabetic group compared to the normal group. These results showed that the reduced colonic contractility resulted from the impaired neuronal conduction and decreased muscarinic receptor sensitivity, which resulted in decreased phosphorylation of MLC via MLCK, and cGMP activity through PDE₅.

• Mass Spectrometry Letters
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• 제3권2호
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• pp.50-53
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• 2012

After success of sildenafil for the treatment of erectile dysfunction, a large number of its analogues have been approved from FDA. Recently, the illegal dietary supplements which include sildenafil, vardenafil, tadalafil, or analogues of these drugs as ingredient have been widely distributed. Therefore, the determination of the residue of synthetic phosphodiesterase- 5 (PDE-5) inhibitors in dietary supplements is highly required due to indiscriminate and unintentional overdose caused nausea, chest pains, fainting and irregular heartbeat. In this paper, we report a rapid and sensitive analytical method for the simultaneous determination of nine phosphodiesterase-5 inhibitors by liquid chromatography-high resolution mass spectrometry. The present method was found to be accurate and reproducible with 40 ${\mu}g$/g of the limit of quantification for the nine PDE-5 inhibitors. The developed method can be successfully applied to the analysis of the seven illegal dietary supplements.

• 한국토양환경학회지
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• 제5권1호
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• pp.3-12
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• 2000

다영역 모델은 Preferential 흐름에 대한 해석을 위하여 토양을 여러개의 공극군으로 나누고 각 토양의 수리학적 특성을 이용하여 토양내의 흐름을 표현한 방정식이다. 이 모델을 유한차분법을 이용하여 수치적으로 풀이할 때 해의 정확도와 일관성을 분석하기위해 수정등가편미분방정식(MEPDE)을 구하고, 안정성을 분석하기위해 Von Neumann법을 이용한다. 수정등가편미분방정식을 이용하여 얻은 유한차분계에 대한 평가는 모델방정식에 대하여 일관성이 있는 것으로 나타났고 모델방정식에 대한 유한차분법은 2차의 정확도를 얻었다. 모델방정식의 안정성 해석은 Von Neumann방법을 이용하여 진폭도와 위상지연을 구하고 이를 분석하였다. 유한차분계의 진폭비는 Peclet수의 변화에 관계없이 비분산적이었으며 Peclet수가 1.0일때 가장 큰 값을 나타냈고, 위상지연은 참값에 대한 빈도요소보다 더 느리게 파동함을 나타냈다. 모델방정식의 안정성 해석 결과, 모델의 영역분해는 보다 정확한 결과를 얻기 위해서 Peclet수는 1.0보다 작고 Courant수는 3.0보다 작은 범위 안에서 분해하는 것이 좋은 것으로 분석된다.

• BMB Reports
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• 제31권2호
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• pp.170-176
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• 1998

Phosphatidylethanolamine N-methyltransferase (PEMT) is known to be a membrane-associated protein. However, cytosolic PEMT was detected when sufficient amounts of exogenous phospholipids were added in the incubation media. The methylation of phospholipids was measured by the incorporation of the $[^3H]-methyl$ group from S-adenosylmethionine and the methylated phospholipids were analyzed by thinlayer chromatography. The essence of the assay condition for the cytosolic enzyme was the inclusion of 200 ${\mu}g$ of each substrate, phosphatidylethanolamine (PE), phosphatidyl N-monomethylethanolamine (PME) and phosphatidyl N,N-dimethylethanolamine (PDE), in the reaction mixture of 100 ${\mu}l$. The subcellular fractionation of brain PEMT activities revealed that approximately 38.1 % for PME, 39.5% for PDE, and 22.4% for PC formation was present in the cytosolic fraction. The general properties of cytosolic PEMT were characterized and compared with those of neuronal nuclei PEMT.

• 한국정보디스플레이학회:학술대회논문집
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• 한국정보디스플레이학회 2009년도 9th International Meeting on Information Display
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• pp.725-727
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• 2009

Lowering the dielectric constant is one of the important issues for the efficiency and the power consumption in the plasma display panel (PDP) industry. This study examined the effect of the addition of ceramic filler (up to 10% of crystalline and amorphous silica, respectively) to a $B_2O_3$-ZnO- $P_2O_5$ glass matrix on the dielectric, coefficient of thermal expansion, etching behaviors and residual stress for the barrier ribs in plasma display panels. The dielectric constant of barrier ribs is affected by containing two types of $SiO_2$ filler for the barrier rib composition in PDP.

• East Asian mathematical journal
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• 제38권5호
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• pp.603-610
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• 2022

In [6, 7] they introduced a new finite element method for accurate numerical solutions of Poisson equations with corner singularities. They consider the Poisson equations with homogeneous boundary conditions, compute the finite element solutions using standard FEM and use the extraction formula to compute the stress intensity factor(s), then they posed new PDE with a regular solution by imposing the nonhomogeneous boundary condition using the computed stress intensity factor(s), which converges with optimal speed. From the solution they could get an accurate solution just by adding the singular part. They considered a partial differential equation with the input function f ∈ L²(Ω). In this paper we consider a PDE with the input function f ∈ H¹(Ω) and find the corresponding singular and dual singular functions. We also induce the corresponding extraction formula which are the basic element for the approach.

• 대한약학회:학술대회논문집
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• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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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)