• Title/Summary/Keyword: time reversible

Search Result 220, Processing Time 0.025 seconds

Blockade of Kv1.5 by paroxetine, an antidepressant drug

  • Lee, Hyang Mi;Hahn, Sang June;Choi, Bok Hee
    • The Korean Journal of Physiology and Pharmacology
    • /
    • v.20 no.1
    • /
    • pp.75-82
    • /
    • 2016
  • Paroxetine, a selective serotonin reuptake inhibitor (SSRI), has been reported to have an effect on several ion channels including human ether-a-go-go-related gene in a SSRI-independent manner. These results suggest that paroxetine may cause side effects on cardiac system. In this study, we investigated the effect of paroxetine on Kv1.5, which is one of cardiac ion channels. The action of paroxetine on the cloned neuronal rat Kv1.5 channels stably expressed in Chinese hamster ovary cells was investigated using the whole-cell patch-clamp technique. Paroxetine reduced Kv1.5 whole-cell currents in a reversible concentration-dependent manner, with an $IC_{50}$ value and a Hill coefficient of $4.11{\mu}M$ and 0.98, respectively. Paroxetine accelerated the decay rate of inactivation of Kv1.5 currents without modifying the kinetics of current activation. The inhibition increased steeply between -30 and 0 mV, which corresponded with the voltage range for channel opening. In the voltage range positive to 0 mV, inhibition displayed a weak voltage dependence, consistent with an electrical distance ${\delta}$ of 0.32. The binding ($k_{+1}$) and unbinding ($k_{-1}$) rate constants for paroxetine-induced block of Kv1.5 were $4.9{\mu}M^{-1}s^{-1}$ and $16.1s^{-1}$, respectively. The theoretical $K_D$ value derived by $k_{-1}/k_{+1}$ yielded $3.3{\mu}M$. Paroxetine slowed the deactivation time course, resulting in a tail crossover phenomenon when the tail currents, recorded in the presence and absence of paroxetine, were superimposed. Inhibition of Kv1.5 by paroxetine was use-dependent. The present results suggest that paroxetine acts on Kv1.5 currents as an open-channel blocker.

Studies on the Mechanism of Action of the Gastric $H^{+}$+$K^{+}$ ATPase Inhibitor KH 3218

  • Cheon, Hyae-Cyeong;Kim, Hyo-Jung;Yum, Eul-Kgun;Cho, Sung-Yun;Kim, Do-Yeob;Yang, Sung-Il
    • Biomolecules & Therapeutics
    • /
    • v.3 no.3
    • /
    • pp.205-209
    • /
    • 1995
  • The novel compound KH 3218 was synthesized and evaluated for its ability to inhibit the gastric H$^{+}$$K^{+}$ ATPase activity in vitro as well as to lessen gastric acid secretion in vivo. KH 3218 inhibited rabbit gastric H$^{+}$$K^{+}$ ATPase in a concentration and time dependent manner. $IC_{50}$/ value was estimated to be about 15 $\mu$M. The inhibition of the H$^{+}$$K^{+}$ ATPase by KH 3218 was blocked by sulfhydryl reducing agents, dithiothreitol or $\beta$-mercaptoethanol. The inhibition of the enzyme was not reversible by 50 fold dilution of the incubation mixtures, suggesting the irreversible nature of the inactivation. In the pylorus-ligated rift, KH 3218 reduced the total acid output as compared with the control. In addition, KH 3218 was capable of inhibiting H. pylori urease activity. These data suggest that KH 3218 is a potent inhibitor for H$^{+}$$K^{+}$ ATPase activity as well as for gastric acid secretion, and has a potential to be developed as a novel antiulcer agent.

  • PDF

Numerical Simulation considering Latent Heat Effect for Laser Cladding Process (잠열을 고려한 레이저 클래딩 공정의 수치해석)

  • Zhao, Guiping;Si, Ho-Mun;Jo, Jong-Du;Kim, Jae-Do
    • Journal of the Korean Society for Precision Engineering
    • /
    • v.18 no.10
    • /
    • pp.134-147
    • /
    • 2001
  • Laser cladding process accompanies phase transformations from melting (on heating) through solidifying (on cooling) at the same time within a small material volume and to final solid phase. The phase transformations are not reversible, but an irreversible thermodynamic process; they accompany either absorption or release of thermal energy (referred to latent heat) during transformation. Yet, most analyses on materials processed by laser as a heat source have been performed on models of neglecting the latent heat in the process and those did not Justify the simplification. With literatures on the laser material process, we have not place an answer to how little the assumption affects on analyses. This led us to our current study: the effects of latent heat on thermo-mechanical analysis. To this end, we developed a fairly accurate program accommodating an algorithm for enforcing the latent heat whenever necessary and ran it combining with ABAQUS$^{TM}$. The simulation techniques we used in this study were verified by directly comparing our prediction with experimental publications elsewhere; our numerical results agreed accurately with the experiments. On the effects of the latent heat, we performed two alternatives about considering the latent heat in analysis, and compared each other. As a result, we found that more accurate conclusions might come out when considering the latent heat in process analyses.s.

  • PDF

The Effect of Light on Germination of the Major Weed Seeds in Upland Fields (주요(主要) 밭잡초종자(雜草種子)의 발아(發芽)에 미치는 광(光)의 영향(影響))

  • Woo, I.S.;Choi, K.S.;Pyon, J.Y.
    • Korean Journal of Weed Science
    • /
    • v.10 no.4
    • /
    • pp.305-311
    • /
    • 1990
  • Effects of light on germination of major weeds in upland fields were examined. Most weeds showed light positive response to germination at above 25$^{\circ}C$, but germination percentage was very low at lower temperatures. Red light promoted germination of Amaranthus lividus, Portulaca oleracea, and A. retroflexus, but far-red light inhibited germination. Germination resposnse of A. retroflexus, A. lividus, and P. oleracea showed reversible reaction to red/far-red light, and thus it seemed that phytochrome was involoved in seed germination, Echinochloa crusgali and Eleusine indica showed higher germination percentage under the conditions of continuous illumination of red, white, and bule lights, and thus it was estimated that blue light pigment (HIR, high irradiation reaction) related to long time illumination was involved in germination in addition to phytochrome.

  • PDF

A Comparative Study of the Prolonged Effect with Neurectomy & Botox Injection Method on the Gastrocnemius Muscle Hypertrophy (비복근비대의 치료 방법인 신경절단술과 보톡스 주사법의 지속효과 비교에 대한 실험적 연구)

  • Kwan, Sung Tak;Joo, Chun Seung
    • Archives of Plastic Surgery
    • /
    • v.35 no.1
    • /
    • pp.56-61
    • /
    • 2008
  • Purpose: There was no controlled study on botox injection and neurectomy for treatments of muscle hypertrophy. Although many studies have shown the clinical effects of each treatment, it was not able to evaluate and compare the effects of each treatment because there was no comparison of the two treatments under the same experimental condition. Hence, the aim of this study is to com Methods: The study was carried out on 21 rabbits. 9 rabbits received botox injection(botox injection group), and neurectomy was performed to another 9 rabbits (neurectomy group). 3 rabbits did not receive any treatment(control group). To compare and analyze the effects of muscular atrophy, muscle was stained with NADH-TR, and the changes in size of the muscle fiber were examined. And the electromyography was examined. In each group, muscle fiber was stained and electromyography was performed 2, 3, and 6 months after injection or operation. Results: In histological test and electromyography, in the neurectomy group, the size of muscular fiber and amplitude of electromyography decreased until 2 months after neurectomy. And decreased results were maintained with the passage of time. It showed irreversible aspect. On the other hand, in the botox injection group, the decrease in the size of muscular fiber and amplitude of electromyography was observed until 2 months after injection. In 3 months after the injection, it was slowly getting back to original size and had almost recovered by 6 months after the injection. It showed reversible aspect. Conclusion: This study shows researches about clinical effect of botox injection and neurectomy coincide with the results of experiment under the same experimental condition.

Effect of coagaulation on ceramic microfiltration membrane fouling (응집공정이 세라믹 정밀여과막 파울링에 미치는 영향)

  • Hwang, Young Jin;Lim, Jae Lim;Choi, Young Jong;Wang, Chang Gun
    • Journal of Korean Society of Water and Wastewater
    • /
    • v.23 no.4
    • /
    • pp.459-469
    • /
    • 2009
  • It is well known that coagulation pretreatment can reduce foulants prior to membrane filtration. The purpose of this research was to investigate the effects of coagulation on fouling of ceramic microfiltration membrane($0.1 {\mu}m$) using pilot plant of $150m^3/day/train$ capacity. Train A membrane system has pretreatment process of ozonation and coagulation while train B has only coagulation. Two types of coagulation operation were investigated: back mixer(rapid mixing with or without slow mixing) which is a conventional mechanically stirred mixer and an inline static mixer. Ozone dose rate for train A was 1 mg/L and ozone contact time was 12 min. The coagulation dose(PACl 10% as $Al_2O_3$) rate was changed 20~40 mg/L according to experimental schedule. In this experimental conditions, the coagulation of back mixer type with rapid mixing(GT=72,000) and slow mixing(GT=45,000) was the best effective in reduction of ceramic membrane fouling regardless preozonation. Especially, the effect of inline static mixer was sensitive to change in water quality. Ozonation mainly affected irreversible fouling rather than reversible fouling in accordance with less adsorption of NOM on the membrane surface. Thus, the increase rate of the nomalized TMP(trans membrane pressure) at $25^{\circ}C$ for train A was relatively lower than that of train B under same coagulation process with same coagulant dosage. The best performance of ceramic membrane appeared in case of combined process with ozonation, therefore this integrated process is able to archive less coagulant dosing and secure a stability of ceramic membrane system.

Electrochromic Properties on $\textrm{MoO}_3$ Thin Films with Heat Treatment ($\textrm{MoO}_3$ 박막의 열처리 효과에 따른 일렉트로크로믹 특성)

  • Jo, Bong-Hui;Kim, Yeong-Ho
    • Korean Journal of Materials Research
    • /
    • v.9 no.11
    • /
    • pp.1144-1147
    • /
    • 1999
  • The effect of the heat treatment on electrochromic properties of $\textrm{MoO}_3$ thin films is investigated by studing optical modulation, optical density, response time, and cyclic voltammetry. From the results of XRD analysis, heat-treated at $450^{\circ}C$ in air for 1 hour Moo3 thin films are found to be crystalline while as-deposited and heat- treated at low temperature ($\leq\;300^{\circ}C$) film are amorphous. The electrochromic devices using as-deposited $\textrm{MoO}_3$ films exhibit good electrochromic properties compared to those using the heat treated $\textrm{MoO}_3$ films. It has shown that the heat-treatment affected the reversible color change and the electrochromic properties of $\textrm{MoO}_3$ films.

  • PDF

Studies on Determination of Titanium from Ilmenite by Polarographic Method (Polarography 에 依한 Titanium 의 定量에 關한 硏究)

  • Kim, Hwang-Am;Kim, Chan-Kuk
    • Journal of the Korean Chemical Society
    • /
    • v.6 no.1
    • /
    • pp.10-13
    • /
    • 1962
  • Titanium in solution of EDTA (Ethylenediaminetetraacetic acid) yield well-defined, reversible polarographic waves. In this report, a polarographic method for rapid determination of titanium in the Korean ilmenite was proposed, This polarographic method is based on the measurement of polarogram in the supporting electrolyte of EDTA. As the pH is increased the wave become more irreversible the diffusion current are diminished, and the half wave potential become more negative. In spite of the complication arising from numerous titanium species, in 0.2 M of EDTA, pH 6.3, the titanium waves are reproducible and analytically useful. In this medium titanium ion give well-defined reduction wave, and the half wave potential were -0.61V vs S.C.E. at pH 6.3. At the same time, the wave had a linear relationship between the concentration of titanium ion and the wave height. The Korean ilmenites were analyzed by this method and satisfactory results were obtained.

  • PDF

A HISTOLOGIC STUDY OF PULPAL REACTION AFTER EXPERIMENTAL TOOTH MOVEMENT IN RATS (백서구치의 실험적 치아이동후 치수조직 변화에 관한 조직학적 연구)

  • Jin, Keun Ho;Hong, Sung Joon
    • The korean journal of orthodontics
    • /
    • v.21 no.3
    • /
    • pp.635-656
    • /
    • 1991
  • It was the aim of this investigation to evaluate some histologic aspect of rat pulp tissue after it had been compromised by an experimental orthodontic force. Experimental animals of thirty five Spraque-Dawley rats were employed. The first upper molars had been successively mesial moved (initial load 100 gr.) with a closed coil spring during 21 days. The experimental periods were set on immediate, 1 day, 1 week, 2 weeks, 3 weeks, 4 weeks following retention time. On each experimental period, the rats were killed and prepared for the light microscopy. After prepared with H/E stain and Gomori's one-step trichrome stain, the specimens were analyzed with evaluation criteria which were adopted in this study. The result may be summarized as follows; 1. The main pulp changes due to experimental orthodontic force included vacuolization of odontoblastic layer, circulation disturbance, root resorption, reduced pulp collagenous fiber density and mean cell count of pulp fibroblast in the immediate group. 2. The pulp tissue changes were revealed reversible because the relieved pulp tissues from experimental orthodontic force were recovered rapidly in each evaluation criteria during retention periods. 3. Compared with normal control group, pulp collagenous fiber density were decreased in immediated group (p < 0.01), but increased in each retention groups. These seem to suggest that the pulp tissues were aged after experimental orthodontic force conditions. 4. Compared with normal control group, mean cell counts of pulp fibroblasts were decreased in immediate group (p < 0.05), but increased continuous in each retention groups. These seem to indicate that the pulp tissues were highly regenerative after experimental orthodontic force conditions. 5. Compared with normal control group, root resorptions occurred in all immediate specimens (p < 0.01) and they were healed in each retention periods, but often observed in 4 weeks retention group. These seem to indicate that root resorptions were recovered slowly after experimental orthodontic force conditions.

  • PDF

High Performance Liquid Chromatographic Analysis of a New Proton Pump Inhibitor KR60436 and Its Active Metabolite O-Demethyl-KR60436 in Rat Plasma Samples Using Column-Switching

  • Lee, Hyun-Mee;Lee, Hee-Yong;Choi, Joong-Kwon;Lee, Hye-Suk
    • Archives of Pharmacal Research
    • /
    • v.24 no.3
    • /
    • pp.207-210
    • /
    • 2001
  • A fully automated high performance liquid chromatography with column-switching was developed for the simultaneous determination of KR60436, a new reversible proton pump inhibitor, and its active metabolite O-Demethyl-KR60436 from rat plasma samples. Plasma sample (50$\mu$l) was directly introduced onto a Capcell Pak MF Ph-1 column ($10{\times}4$ mm I.D.) where primary separation was occurred to remove proteins and concentrate target Substances Using acetonitrile-Potassium Phosphate (PH 7, 0.1 M) (2 : 8, v/v). The drug molecules eluted from MF Ph-1 column were focused in an intermediate column ($10{\times}2$ I.D.) by the valve switching step. The substances enriched in intermediate column were eluted and separated on a Vydac 218MR53 column ($250{\times}3.2$ I.D.) using acetonitrilepotassium phosphate (pH 7, 0.02 M) (47:53, v/v) at a flow rate of 0.5 ml/min when the valve status was switched back to A position. The method showed excellent sensitivity (detection limit of 2 ng/ml) with small volume of samples ($50{\mu}$l), good precision and accuracy, and speed (total analysis time 24 min) without any loss in chromatographic efficiency. The response was linear ($r^2{\geq}0.797$) over the concentration range of 5-500 ng/ml.

  • PDF