• 제목/요약/키워드: n uptake inhibition

검색결과 64건 처리시간 0.034초

5-HT 흡수억제성 항우울제들이 가토혈소판의 [$^3H$]Imipramine과 [$^3H$]Paroxetine Binding, [$^3H$]5-HT 흡수, 및 5-HT함량에 미치는 영향 (Effects of Chronic Treatments with 5-HT Uptake Inhibitors on the [$^3H$]Imipraine and [$^3H$]Paroxetine Binding, [$^3H$]5-HT Uptake, and 5-HT Content of the Rabbit Platelet)

  • 원경식;이민수;신경호;전보권;곽동일
    • 생물정신의학
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    • 제1권1호
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    • pp.88-97
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    • 1994
  • Many evidences are compatible with the correlation between the inhibition of [$^3H$] imipramine([$^3H$]IMI) and [$^3H$]paroxetine([$^3H$]PAT) binding to the 5-hydroxytryptamine(5-HT) transporter complex and the 5-HT uptake of 5-HT neurons and platelets, and most antidepressants have been shown to inhibit the [$^3H$]IMI and [$^3H$]PAT binding and the neuronal 5-HT uptake. However, several paradoxical research findings led to doubt about the pharmacological significance of the [$^3H$]IMI and [$^3H$]PAT binding sites. This study was carried to clarify the correlation between the [$^3H$]IMI and [$^3H$]PAT binding parameters and the tissue 5-HT content or/and [$^3H$]5-HT uptake in the rabbit platelet, which contains 40 times ad much 5-HT as that of human platelet and shows the 10 fold higher $B_{max}$ of the 5-HT transporter binding to a 5-HT uptake inhibitor. The rabbits were treated for 28 days with amitriptyline(4mg/kg/day : AP), fluoxetine(0.5mg/kg/day : FO), and sertraline(0.5mg/kg/day : SA) via an Alzet osmotic pump implanted for constant infusion. The [$^3H$]IMI binding $B_{max}$ and $K_d$ of the rabbit platelets were $6.4{\pm}1.2$pmol/mg protein and $10.9{\pm}2.1$nM and those in the [$^3H$]PAT binding were $8.6{\pm}1.1$pmol/mg protein and $1.6{\pm}0.3$nM, respectively. AP slightly increased $B_{max}$ of [$^3H$]IMI binding and both [$^3H$]IMI binding and [$^3H$]PAT binding $K_d$, and i contrast, it slightly decreased $B_{max}$ of [$^3H$]PAT binding. FO Slightly increased $K_d$ of both and [$^3H$]IMI and [$^3H$]PAT binding and slightly decreased $B_{max}$ of [$^3H$]IMI and [$^3H$]PAT binding. SA produced the significant increase of [$^3H$]PAT binding $B_{max}$ and the slight increase of both [$^3H$]IMI and [$^3H$]PAT binding $K_d$ and in contrast, it slightly decreased $B_{max}$ and of [$^3H$]IMI binding. And, the $V_{max}$ and $K_m$ of platelet [$^3H$]5-HT uptake were $24.2{\pm}2.4$pmol/$10^8$ platelets/min and $3.3{\pm}0.3$nM, respectively. The $V_{max}$ was little affected by AP, FO, or SA, but the [$^3H$]5-HT uptake $K_m$ value was moderately increased by FO. However, the platelet 5-HT content was moderately decreased by all of the 5-HT uptake inhibitors used in this study. These results seem to be consistent with the allosterical and competitive interaction of 5-HT uptake inhibiting antidepressants with each other as well as 5-HT in the 5-HT transporter binding, and provide no support for the view that the potencies of 5-HT uptake inhibitors to inhibit the [$^3H$]IMI or [$^3H$]PAT binding with 5-HT transporter complex correlate with their antidepressant potencies.

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Characterization of valacyclovir transport mechanism across the intestinal epithelium

  • Han, H.;Covitz, M.;Surendran, N.;Stewart, B.;Amidon, G.L.
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 1997년도 춘계학술대회
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    • pp.119-119
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    • 1997
  • Valacyclovir is a L-valyl ester prodrug of acyclovir which is a highly effective and selective antiviral agent in the treatment of herpes virus diseases. Valacyclovir is rapidly and almost completely converted to acyclovir and increases the oral bioavailability of acyclovir three to five fold. However, the intestinal absorption mechanism of valacyclovir is not clear. If the improved absorption mechanism of valacyclovir is fully understood, it will provide a rationale of designing the amino acid ester prodrugs of polar drugs containing hydroxyl group. The main objective of our present study is to characterize the membrane transport mechanism of valacyclovir. Methods : Intestinal absorption of valacyclovir was investigated by using in-situ rat perfusion study and its wall permeability was estimated by modified boundary layer model. The membrane transport mechanism was also investigated through the uptake study in Caco-2 cells and in CHO-hPepTl cells. Results : In the rat perfusion study, the wall permeability of valacyclovir was ten times higher than acyclovir and showed concentration dependency, Valacyclovir also demonstrated a D,L stereo-selectivity with L-isomer having an approximately five-fold higher permeability than D-isomer. Mixed dipeptides and cephalexin, which are transported by dipeptide carriers, strongly competed with valacyclovir for the intestinal absorption, while L-valine did not show any competition with valacyclovir. This indicated that the intestinal absorption of valacyclovir could be dipeptide carrier-mediated. In addition, the competitive uptake study in Caco-2 cells presented that dipeptides reduced the valacyclovir uptake but valine did not. Also, in IC$\sub$50/ study, valacyclovir showed strong inhibition on the $^3$H-gly-sar uptake in CHO-hPepTl cells over-expressing a human intestinal peptide transporter. Taken together, the result from our present study indicated that valacyclovir utilized the peptide transporter for the intestinal absorption.

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Growth and Chlorophyll Biosynthesis of Vigna angularis under Lead Stress

  • Suh-Young Koo;Sun
    • 한국환경과학회지
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    • 제1권2호
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    • pp.145-155
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    • 1992
  • The effect of various supplies of lead singly and in combination with aluminium on growth and chlorophyll biosynthesis was investigated in 7-day-old Vigna anguluris seedlings. Expose to 50 $\mu$N Pb or more drastically reduced root elongation rate. Significant depressions in root growth was observed within 1 day and no recovery of growth was seen over the duration of treatment period. Root elongation decreased depending on the Pb concentrations. Root growth inhibition was stronger than shoot growth inhibition. The initiation of lateral roots appeared to be more sensitive to Pb than the growth of main roots. Inhibition of root and shoot elongation by Pb was lessened by combined exposure of Pb and Al, suggesting that the presence of AA reverse the inhibitory effect of Pb alone. With the histochemical sodium rhodizonate method the rate of Pb uptake was dependent on the Pb concentration and exposure time of the roots to Pb salts. Pb was first deposited on the root surface and then translocated radially in the root cap cells. During a longer Pb administration (up to 72 h) Pb penetration was nonuniform, with accumulation within the cortex or endodermis. There was drastic reduction in chlorophyll content by Pb. The Pb inhibition of chlorophyll synthesis was concentration dependent. 5-Aminolevulinic acid dehydratase (ALAD) activity exhibited distinct inhibition from control. Reduction in chlorophyll content was accompanied by proportional changes in ALAD activity. Chlorophyll content and ALAD activity were less affected by combined exposure of Pb and Al, suggesting that Al has a protective effect against the inhibiting action of Pb on photosynthetic activity.

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Butachlor에 대한 벼 유묘의 생리적 반응 (Physiological Responses of Rice Seedlings to Butachlor)

  • 채문복
    • 한국잡초학회지
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    • 제15권4호
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    • pp.247-253
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    • 1995
  • The herbicide butachlor [N-(butoxymethyl)-2-chloro-N-(2,6-di-methylphenyl) acetamide] is widely used by farmers as a tool for weed management of transplanted rice(Oryza sativa L.) in Taiwan. The herbicide did not stop germination of rice and weed seeds, but strongly inhibited the subsequent growth of young shoots and roots. The inhibition was also strong on established seedlings. However, they could recover to normal growth after the herbicide effect disappeared. Butachlor greatly decreased the endogenous indole-3-acetic acid (IAA) but increased the endogenous abscisic acid (ABA) contents of rice seedlings. Addition of lAA into growth medium (Hoagland's solution) partly relieved growth inhibition. Pretreatment of both gibberellic acid ($GA_3$) and IAA 24 hours before butachlor treatment almost completely alleviated the butachlor-interfere with GA and/or IAA metabolism or their action resulting in the growth inhibition of rice. Butachlor was readily absorbed by rice roots. During 24 hours of uptake experiment, 32% of the applied herbicide was absorbed. Pretreatment of the herbicide for 2 days did ncx affect the absorption. Of the absorbed herbicide, 80% remained in roots, only 20% transported into shoots, and more than 50% was metabolized to water soluble substances. Thin-layer chromatographic (TLC) analysis indicated that the Rf value of the most abundant metabolite was butachlor-glutathione conjugate. Rice, barnyardgrass (Echinochloa crus-galli (L.) Beauv.), and monochoria (Monochoria vaginalis Presl) seedlings contained relatively high level of non-protein thiols, while the glutathione S-transferase (GST) activity was found highest in rice, barnyardgrass the next, monochoria the lowest. The difference in GST activity among these species might be related to their sensitivity to butachlor.

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수종의 불소방출 수복재의 탈회억제 효과 및 불소침투에 관한 연구 (IN VITRO STUDY OF DEMINERALIZATION INHIBITION EFFECT AND FLUORIDE UPTAKE INTO ADJACENT TEETH OF LIGHT-CURED FLUORIDE-RELEASING RESTORATIVES)

  • 김송이;최성철;김광철;최영철;박재홍
    • 대한소아치과학회지
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    • 제37권3호
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    • pp.288-297
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    • 2010
  • 자이오머(Giomer)는 레진강화형글라스아이오노머에 견줄 만큼 불소방출량이 많다고 하나, 우식예방 효과에 관한 연구들이 많지 않아 임상적용에 대한 근거가 부족한 실정이다. 본 연구는 자이오머(BF 군)를 포함하여 레진강화형글라스아이오노머(FF 군), 콤포머(DA 군)와 대조군인 콤포짓(FZ 군)의 우식억제 효과와 주변 치질로의 불소침투 양상을 비교하기 위하여, 공초점레이저주사현미경과 전자탐침미세분석기를 이용하여 각 수복재의 우식예방 효과를 비교하였으며, 다음과 같은 결과를 얻었다. 1. 수복물 주위 이차 인공우식에서 법랑질 외측병변의 깊이는 FZ 군에서 가장 깊었으며, BF 군이 가장 작게 나타났다(p<0.05). 2. 수복물과 법랑질 계면에 나타난 탈회억제층의 두께를 관찰한 결과 FZ 군이 가장 작게 나타났으며, FF, DA, BF 간에는 유의성 있는 차이를 보이지 않았다(p<0.05). 3. 법랑질에 침투된 불소농도는 BF, FF, DA의 순으로 높게 나타났다. 4. 상아질에 침투된 불소농도는 DA, BF, FF의 순으로 높게 나타났으며, 이는 상아질-수복물의 접착 계면에 영향 받는 것으로 보인다.

수도묘(水稻苗)의 Butachlor 흡수(吸收) 및 약해발생(藥害發生) 특성(特性)에 관한 생리적(生理的) 연구(硏究) (Uptake of Butachlor by Rice Seedlings and Its Phytotoxic Action to the Physiological Activities)

  • 정봉진;권용웅
    • 한국잡초학회지
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    • 제1권1호
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    • pp.57-68
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    • 1981
  • 수도묘(水稻苗)의 Butachlor(2-chloro-2',6'-diethyl-N-(carboxymethyl) acetanilide) 흡수특성(吸收特性)과 약해발생가구(藥害發生機構)를 밝히어 Butachlor의 안전사용(安全使用)에 도움을 주고자 시도(試圖)되었다. 수도품종(水稻品種) '만석(萬石)'(수원(水原)264호(號))을 사용(使用)하여 제(第)6, 7여기(葉期)까지 수경재배(水耕栽培)한 후 Butachlor를 0, 1.8, 3.6, 7.2, 10.8 또는 14.4ppm 되도록 처리(處理한) 수경액(水耕液)으로 1, 2, 4일간(日間) 생육(生育)시킨 경우와 Butachlor 처리(處理) 후(後) 정상수경액(正常水耕液)으로 교체(交替)하고 6일간(間生) 생장(生長)시킬 경우 약해(藥害)의 진전(進展) 또는 회복과정중(恢復過程中)에 일어나는 수도(水稻)의 Butachlor 흡수(吸收)에 따른 생장반응(生長反應), 수분흡수(水分吸收), 양분흡수(養分吸收), 기공(氣孔) 개폐(開閉), 질산환원효소(窒酸還元酵素)(Nitrate reductase)의 생합성(生合成) 및 분해작용(分解作用)의 변화(變化)를 검정(檢定)했고 Butachlor의 세포구성물질(細胞構成物質)들에 대한 흡착특성(吸着特性)을 비교(比較)하였으며 그 결과(結結)는 다음과 같이 요약(要約)된다. 1. 수도묘(水稻苗)의 Butachlor의 흡수(吸收)는 처리농도(處理濃度) 및 기간(期間)에 비례(比例)하여 거의 직선적(直線的)으로 증가(增加)하였다. 2. Butachlor는 지상부(地上部) 생육(生育)보다는 뿌리생육(生育)을, 지상부(地上部) 생체중(生體重) 및 출엽(出葉)보다는 초장(草長)의 생육(生育)을 더욱 저해(沮害)하였으며, 처리종료(處理終了) 후(後) 지상부(地上部) 생체중(生體重)과 출엽(出葉)은 조속(早速)히 회복(恢復)되었으나 초장(草長) 및 뿌리생체중(生體重) 생장(生長)은 4일(日) 이후(以後) 회복세(恢復勢)를 보였다. 3. Butachlor는 뿌리의 수분흡수(水分吸收)를 처리농도(處理濃度) 비례(比例)하여 곧 저해(沮害)하였고, 그 결과(結果) 엽면(葉面) 기공(氣孔)의 저항(低抗)을 증가(增加)시켰으며, 처리종료(處理終了) 후(後)에는 수분흡수력(水分吸收力)은 곧 회복(恢復)되었으나 기공(氣孔)의 개도(開度)는 서서히 회복(恢復)되었다. 4. Butachlor는 처리(處理) 전(前) 후(後) 수도묘(水稻苗)의 $NH_4^+$, $K^+$$Ca^{++}$ 같은 양(陽)이온의 흡수(吸收)에는 영향(影響)하지 않았으나 $NO_3^-$의 흡수(吸收)를 뚜렷이 저해(沮害)했고, 7.2 ppm의 고종도(高濃度)에서는 인산(燐酸)의 흡수(吸收)도 저해(沮害)했다.

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구강 편평세포암종 KB세포에서 아미노산 수송억제제 BCH에 의한 세포성장 억제 (Induction of Growth Inhibition by BCH in KB Human Oral Epidermoid Carcinoma Cells)

  • 윤정훈;김윤배;김도경
    • 한국식품영양과학회지
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    • 제32권5호
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    • pp.758-763
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    • 2003
  • 구강 편평 세포암종 KB 세포를 이용하여 아미노산 수송계 L억제제인 BCH의 세포 성장억제에 미치는 효과를 밝히기 위해, KB세포에서 uptake실험, MTT분석 및 DNA frag-mentation분석 등을 시행하여 다음과 같은 결과를 얻었다. KB 세포에서는 아미노산 수송계 L 중에서 LAT1과 그 보조인자 4F2hc를 통해 BCH및 중성 아미노산들이 수송되었다. BCH는 시간과 농도에 의존적으로 KB세포의 성장을 억제시켰다. BCH를 처리한 실험군에서 DNA fragmentation 현상은 볼 수 없었다. 본 연구의 결과로서 구강암 세포주인 구강 편평세포암종 KB 세포에서 LAT1과 그 보조인자 4F2hc를 통해 BCH및 중성 아미노산의 수송이 이루어지고 있다는 것을 확인할 수 있었으며 BCH는 이 LAT1을 차단하여 중성 아미노산들의 세포 내 고갈을 유도함으로서 KB 세포 성장의 억제를 유도하는 것으로 사료된다.

NaCl 스트레스가 토마토, 고추, 가지의 생육, 광합성 속도 및 무기양분 흡수에 미치는 영향 (Effect of NaCl Stress on the Growth, Photosynthetic Rate and Mineral Uptake of Tomato, Red Pepper and Egg Plant in Pot Culture)

  • 강경희;권기범;최영하;김회태;이한철
    • 생물환경조절학회지
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    • 제11권3호
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    • pp.133-138
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    • 2002
  • 본 실험은 가지과 작물의 염 스트레스에 대한 생장 특성 및 생리적 반응을 구명하기 위하여 수행되었다. 생육단계에 따라 NaCl을 농도별로 처리한 결과는 다음과 같았다. 초장, 생체중 등 생육은 유묘기 및 영양 생장기 모두 NaCl 농도가 높을수록 모든 작물에서 억제되었다 특히 토마토 및 가지에서는 NaCl 40mM 이상에서, 그리고 고추에서는 20mM 이상에서 작물의 생육이 크게 억제되었다. 수량은 토마토 및 가지에 서는 NaCl 20 mM 이상에서, 그리고 고추에서는 10 mM 이상에서 감소하였다. 이러한 수량감소는 낮은 농도에서는 착과수의 감소에, 그리고 농도가 높을수록 착과수의 감소와 더불어 평균과중의 감소의 영향이 컸다. 광합성 속도는 NaCl 농도가 높을수록 감소하는 경향이었으며. 고추가 가장 낮았고, 토마토, 가지 순으로 낮았다. 잎의 수분포텐셜과 기공 전도도도 광합성과 같은 경향을 나타냈다. 경엽의 무기 양분 함량에서는 질소, 인산, 칼슘, 마그네슘 및 칼륨 함량은 NaCl 농도가 증가할수록 감소하였으나 Na 및 Cl 함량은 증가하였다.

폐수 내 고농도 free ammonia(FA)가 미세조류의 성장 및 기질제거에 미치는 영향 평가 (Effect of high free ammonia concentration on microalgal growth and substrate uptake)

  • 김은지;조재형;노경호;남귀숙;황선진
    • 상하수도학회지
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    • 제30권6호
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    • pp.715-723
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    • 2016
  • This study investigated the effect of high concentration of free ammonia on microalgal growth and substrate removal by applying real wastewater nitrogen ratio. To test of this, the conditions of free ammonia 1, 3, 6, 9, 12, 15 mg-N/L are compared. After 3 days of incubation, algal growth of Chlorella vulgaris and carbon removal rate are respectively lower in the reactors of FA 12, 15 mg-N/L compared to the others. This indicates that the high concentration of free ammonia, in this case, above 12 mg-N/L, has negative effect on algal growth and metabolic activity. Also, high concentration of free ammonia causes the proton imbalance, ammonium accumulation in algae and has toxicity for these reasons. So, we have to consider free ammonia in applying the microalgae to wastewater treatment system by the way of diluting wastewater or controlling pH and temperature.

Relation between Chemical Structure of Yellow Disperse Dyes and Their Lightfastness

  • Kim, Sung-Dong;Park, Eun-Jin
    • Fibers and Polymers
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    • 제2권3호
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    • pp.159-163
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    • 2001
  • Five yellow disperse dyes were synthesized and their dyeing, fastness and photodegradation behaviors were investigated. It was found that dyes derived from phenylindole and N-alkylaminobenzene showed dye uptake directly proportional to the dye concentration, but the build-up of dyes derived from carbazole and pyridone were not good. The wavelength at maximum absorption. molar extinction coefficient. and the tendency to the photodegradation were strongly dependent on the electron donating ability of the coupling component. The dye, whose coupling component was phenylindole, possessed the excellent dyeing properties and the high degree of lightfastness. UVA had an effect on the inhibition of the photodegradation especially for the easily photodegradabte dyes.

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