• Title/Summary/Keyword: blocking effect

Search Result 904, Processing Time 0.027 seconds

Interaction of Antihistaminics with Muscarinic Receptor(II) -Action on the cerebral muscarinic $M_1$ Receptor- (항 Histamine제와 Muscarinic Receptor와의 상호작용(II) -대뇌 Muscarinic $M_1$ Receptor에 대한 작용-)

  • Lee, Shin-Woong;Park, Young-Joo;Park, In-Sook;Lee, Jeung-Soo
    • YAKHAK HOEJI
    • /
    • v.34 no.4
    • /
    • pp.224-237
    • /
    • 1990
  • A single uniform population of specific, saturable, high affinity binding site of $[^3H]QNB$ guinuclidinyl benzilate(QNB) was identified in the rat cerebral microsomes. The Kd value(37.2 pM) for $[^3H]QNB$ calculated from the kinetically derived rate constants was in agreement with the Kd value(48.9 pM) determined by analysis of saturation isotherms at various receptor concentrations. Dimenhydrinate(DMH), histamine $H_1-blocker$, increased Kd value for $[^3H]QNB$ QNB without affecting the binding site concentrations and this effect resulted from the ability of DMH to slow $[^3H]QNB-receptor$ association. Pirenzepine inhibition curve of $[^3H]QNB$ binding was shallow(nH = 0.52) indicating the presence of two receptor subtypes with high ($M_1-site$) and low($M_2-site$) affinity for pirenzepine. Analysis of these inhibition curves yielded that 68% of the total receptor populations were of the $M_1-subtype$ and the remaining 32% of the $M_2-subtype$. Ki values for the $M_1-$ and $M_2-subtypes$ were 2.42 nM and 629.3 nM, respectively. Ki values for $H_1-blockers$ that inhibited $[^3H]QNB$ binding varied with a wide range ($0.02-2.5\;{\mu}M$). The Pseudo-Hill coefficients for inhibition of $[^3H]QNB$ binding by most of $H_1-blockers$ examined except for oxomemazine inhibition of $[^3H]QNB$ binding were close to one. The inhibition curve for oxomemazine in competition with $[^3H]QNB$ was shallow(nH = 0.74) indicating the presence of two receptor populations with different affinities for this drug. The proportion of high and low affinity was 33:67. The Ki values for oxomemazine were $0.045{\pm}0.016\;{\mu}M$ for high affinity and $1.145{\pm}0.232\;{\mu}M$ for low affinity sites. These data indicate that muscarinic receptor blocking potency of $H_1-blockers$ varies widely between different drugs and that most of $H_1-blockers$ examined are nonselective antagonist for the muscarinic receptor subtypes, whereas oxomemazine might be capable of distinguishing between subclasses of muscarinic receptor.

  • PDF

Impacts of Elevated $CO_2$ on Algal Growth, $CH_4$ Oxidation and $N_2O$ Production in Northern Peatland (이탄습지에서 이산화탄소의 농도가 조류의 증식, 메탄 산화 및 아산화질소 생성에 미치는 영향)

  • Freeman, Chris;Kang, Ho-Jeong
    • Korean Journal of Ecology and Environment
    • /
    • v.34 no.4 s.96
    • /
    • pp.261-266
    • /
    • 2001
  • Effects of elevated carbon dioxide ($CO_2$) on soil microbial processes were studied in a northern peatland. Intact peat cores with surface vegetation were collected from a northern Welsh fen, and incubated either under elevated carbon dioxide (700 ppm) or ambient carbon dioxide (350 ppm) conditions for 4 months. Higher algal biomass was found under the elevated $CO_2$ condition, suggesting $CO_2$ fertilization effect on primary production, At the end of the incubation, trace gas production and consumption were analyzed using chemical inhibitors. For methane ($CH_4$ ), methyl fluoride ($CH_3F$) was applied to determine methane oxidation rates, while acetylene ($C_2H_2$) blocking method were applied to determine nitrification and denitrification rates. First, we have adopted those methods to optimize the reaction conditions for the wetland samples. Secondly, the methods were applied to the samples incubated under two levels of $CO_2$. The results exhibited that elevated carbon dioxide increased both methane production (210 vs. $100\;ng\;CH_4 g^{-1}\;hr^{-1}$) and oxidation (128 vs. $15\;ng\;CH_4 g^{-1}\;hr^{-1}$), resulting in no net increase in methane flux. For nitrous oxide ($N_2O$) , elevated carbon dioxide enhanced nitrous oxide emission probably from activation of nitrification process rather than denitrification rates. All of these changes seemed to be substantially influenced by higher oxygen diffusion from enhanced algal productivity under elevated $CO_2$.

  • PDF

Effect of Heparin-binding Epidermal Growth Factor (HB-EGF) on Integrin $\alpha_{\nu}-\betaFe_3$ Expression in Preimplantation Mouse Embryos

  • Lim, Jung-Jin;Shin, Hyun-Sang;Lee, Ji-Won;Kang, Sue-Man;Lee, Sung-Eun;Kang, Han-Seung;Kim, Moon-Kyoo
    • Proceedings of the Korean Society of Embryo Transfer Conference
    • /
    • 2002.11a
    • /
    • pp.102-102
    • /
    • 2002
  • Heparin-bindin epidermal growth factor (HB-EGF) is one of the EGF family to be expressed at the time of implantation in the mouse uterus. Although HB-EGF has been shown to stimulate the development of embryo and uterus in the mouse, its correlation between cell adhesion molecules remains undefined. Integrin $\alpha$$_{ν}$$\beta$$_3$, one of the cell adhesion molecules, is an important mediator of cell-substratum and cell-cell adhesion in implantation. In the present studies, we investigated the effects of HB-EGF on the embryonic development, initiation of implantation and expression of integrin $\alpha$$_{ν}$$\beta$$_3$ in in vitro culture, blocking of HB-EGF, RT-PCR and immunofluores cence analysis. The results showed that HB-EGF significantly improved the developmental rate of hatched embryos (24.1%, p<0.01) and outgrowth embryos (42.5%, p<0.01). On the other hand, this growth factor showed no offset before the hatching embryonic stage. Analysis of RT-PCR showed that HB-EGF upregulated the expression level of integrina $\alpha$$_{ν}$$\beta$$_3$ subunit genes on the preimplantation embryo and outgrowth of blastocyst (120hr and 144hr after hCG injection). Immunofluorescence analysis showed that the integrin $\alpha$$_{ν}$$\beta$$_3$ subunits localized at the pericellular borders and cell-cell contact areas. Increase in fluorescence intensity was observed in the HB-EGF treated embryos. Intrauterine injection of an anti-HB-EGF antiserum at day 3 significantly decreased the number of implantation sites (14.4, p<0.01) and significantly increased the number of recovered embryos(6.4, p<0.05) at day 5. From these results, it imply that HB-EGF improve the embryo development and accelerated the expression of integrin $\alpha$$_{ν}$$\beta$$_3$ in the preimplantation mouse embryos.

  • PDF

The Effect of Computer-Assisted Instruction Using Molecular-Level Animation in Middle School Science Class (중학교 과학수업에서 입자수준의 애니메이션을 이용한 컴퓨터 보조수업의 효과)

  • Noh, Tae-Hee;Cha, Jeong-Ho;Kim, Chang-Min;Choi, Yong-Nam
    • Journal of The Korean Association For Science Education
    • /
    • v.18 no.2
    • /
    • pp.161-171
    • /
    • 1998
  • The effects of computer-assisted instruction (CAl) using molecular-level animation upon students' conceptions, attitudes toward science instruction, and learning motivation were investigated. Treatment and control groups (2 classes) were selected from a girls middle school in Seoul, and taught about the motion of molecule for 5 class hours. Before instruction, the short-version Group Assessment of Logical Thinking (GALT) and the Patterns of Adaptive Survey were administered, and the grade for the previous science course was obtained. The GALT score was used as a blocking variable, and the others as covariates. After the instructions, the researcher-made conceptions test, the test of attitudes toward science instruction, and the motivation questionnaire were administered. The perception questionnaire of CAl was also administered to the treatment group. Although more students in the CAl group had sound understanding about the motion of molecule, the scores of the conceptions test for the two groups were not significantly different at .05 level of significance. The students in the CAl group, however, were found to have more positive attitudes toward science instruction and learning motivation. In the perception questionnaire of CAl, most students in the treatment group exhibited positive attitudes toward the CAl. However, some students mentioned that they were disturbed by noisy environments, and that they could not understand some content presented. Educational implications are discussed.

  • PDF

Neuroprotective Effects of Cheongnoemyeongsin-hwan against Hydrogen Peroxide-induced DNA Damage and Apoptosis in Human Neuronal-Derived SH-SY5Y Cells (인체 신경세포에서 청뇌명신환(淸腦明神丸)의 산화적 스트레스에 대한 세포보호 효과)

  • Pi, Guk Hyun;Hwang, Won Deuk
    • Herbal Formula Science
    • /
    • v.25 no.1
    • /
    • pp.51-68
    • /
    • 2017
  • Objectives : Oxidative stress due to excessive accumulation of reactive oxygen species (ROS) is one of the risk factors for the development of several chronic diseases, including neurodegenerative diseases. Methods : In the present study, we investigated the protective effects of cheongnoemyeongsin-hwan (CNMSH) against oxidative stress‑induced cellular damage and elucidated the underlying mechanisms in neuronal-derived SH-SY5Y cells. Results : Our results revealed that treatment with CNMSH prior to hydrogen peroxide (H2O2) exposure significantly increased the SH-SY5Y cell viability, indicating that the exposure of the SH-SY5Y cells to CNMSH conferred a protective effect against oxidative stress. CNMSH also effectively attenuated H2O2‑induced comet tail formation, and decreased the phosphorylation levels of the histone ${\gamma}H2AX$, as well as the number of apoptotic bodies and Annexin V‑positive cells. In addition, CNMSH exhibited scavenging activity against intracellular ROS generation and restored the mitochondria membrane potential (MMP) loss that were induced by H2O2, suggesting that CNMSH prevents H2O2‑induced DNA damage and cell apoptosis. Moreover, H2O2 enhanced the cleavage of caspase-3 and degradation of poly (ADP-ribose)-polymerase, a typical substrate protein of activated caspase-3, as well as DNA fragmentation; however, these events were almost totally reversed by pretreatment with CNMSH. Furthermore, CNMSH increased the levels of heme oxygenase-1 (HO-1), which is a potent antioxidant enzyme, associated with the induction of nuclear factor-erythroid 2-related factor 2 (Nrf2). According to our data, CNMSH is able to protect SH-SY5Y cells from H2O2-induced apoptosis throughout blocking cellular damage related to oxidative stress through a mechanism that would affect ROS elimination and activating Nrf2/HO-1 signaling pathway. Conclusions : Therefore, we believed that CNMSH may potentially serve as an agent for the treatment and prevention of neurodegenerative diseases caused by oxidative stress.

Quality Improvement of Interpolated Image Using Weight-Granting Method Based on Median Values Of Local Area (국부 영역 중앙값 기반의 가중치 부여 방법을 이용한 보간 영상의 화질 개선)

  • Kwak, Nae-Joung;Ryu, Sung-Pil;Ahn, Jae-Hyeong;Kwon, Dong-Jin
    • The Journal of the Korea Contents Association
    • /
    • v.7 no.12
    • /
    • pp.346-354
    • /
    • 2007
  • Interpolation methods to get the magnified image from an image with low resolution use known pixels to make an interpolated pixel. This interpolation process usually generates blurred edges and blocking effect in the result image. To improve these defects, conventional methods multiply proper weights reflecting neighborhood pixels and add the values during interpolating process. The proposed method changes input pixels in consideration of information of neighborhood pixels, gets interpolated pixels by using these values and improves the quality of interpolated image. Firstly, we compute difference values of the diagonal directions of a pixel and classify flat regions and complex regions according to these values. If the regions is complex ones, the proposed method changes an original pixel into a new value using a input pixel and a median value of it's neighbor pixels. Therefore, the proposed method applies bilinear method to the original pixels in flat regions and the changed ones in complex regions and produces the interpolated images. We evaluate the performance of the proposed method with existing methods by using PSNR and the quality of enlarged image. The results show that the proposed method improves PSNR in comparing with conventional methods and that is superior to the existing methods in terms of the quality of the interpolated image.

Histogram compression equalization method that has been deformed for the distribution of brightness and balanced improvement of the image contrast (영상의 명암대비 향상 및 균형적인 밝기 분포를 위한 변형된 히스토그램 압축 평활화 기법)

  • Kim, Jong-in;Lee, Jae-won;Hong, Sung-hoon
    • Proceedings of the Korean Institute of Information and Commucation Sciences Conference
    • /
    • 2013.05a
    • /
    • pp.820-823
    • /
    • 2013
  • Recently, the need for improving image quality of the image is increasing in various fields smartphones, cameras, and portable devices. How a significant impact on improving image quality of the image is a contrast enhancement, as a representative method to improve the contrast, the process of histogram equalization, various studies have been made. However, the method of histogram equalization general, by readjusting the only brightness, when the image histogram is biased to one side, due to changes in the excess brightness, distortions such as blocking phenomenon occurs. In this paper, we provide a contrast enhancement techniques through the compression and re-distribution of a well-balanced average brightness of the histogram distribution. By be differential compression histogram based on the histogram frequency in order to suppress the supersaturation phenomenon due to the increase in contrast ratio excessive repositioning well-balanced histogram lopsided, the proposed method, the balance of the brightness of the image I want to to take. The experimental results, the image brightness is balanced manner compared to conventional methods, the proposed method showed a good effect to improve the contrast without supersaturation phenomenon as compared with the conventional methods.

  • PDF

A Study on the $Na^+/Ca^{2+}$ Exchange Mechanism in the Smooth Muscle of Guinea-pig Stomach

  • Kim, Eui-Yong;Han, Jin;Kim, Ki-Whan
    • The Korean Journal of Physiology
    • /
    • v.26 no.1
    • /
    • pp.55-68
    • /
    • 1992
  • The effects of changes in extracellular $Na^+\;and\;Ca^+$ concentration on the membrane potential and contractility were studied in the antral circular muscle of guinea pig stomach in order to elucidate the existence and the nature of $Na^+/Ca^{2+}$ exchange mechanism. All experiments were performed in tris buffered Tyrode solution which was aerated with 100% $O_2$ and kept at $35^{\circ}C.$ The treatment of $10^{-5}$ ouabain was performed to induce intracellular $Na^+$ loading prior to the start of experiment. The results were as follows: 1. $Na^+$-free Tyrode or high $Ca^{2+}$-Tyrode solution hyperpolarized the membrane potential and induced contracture. The time course of contracture was similar to that of change in membrane potential. 2. The degree of hyperpolarization and the amplitude of contracture decreased in accordance with the increase of extracellular $Na^+$ concentration. 3. $Na^+$-free contracture was developed even after blocking the influence of intrinsic nerves by the pretreatment with atropine, guanethidine and TTX. 4. $Ca^{2+}$-channel blockers(D-600 or $Mn^{2+}$) and the blocker of intracellular $Ca^{2+}$ release from sarcoplasmic reticulum(ryanodine) did not suppress the development of $Na^+$-free contracture. And also, dinitrophenol had no effect on $Na^+$-free contracture. 5. Dose-response relationship between extracellular $Na^+$ concentrations and the magnitude of contractures showed a sigmoid pattern. The slope of straight line from Hill plot was 2.7. 6. In parallel with the increase of extracellular $Ca^{2+}$ concentration, the amplitude of contracture increased dose dependently and was maximum at 8 mM $Ca^{2+}$-Tyrode solution. 7. The relationship between extracellular $Ca^{2+}$ concentrations and the magnitude of contractures showed hyperbolic pattern. The slope of straight line from Hill plot was 1.1. From the above results, it is suggested that $Na^+/Ca^{2+}$ exchange mechanism exists in the antral circular muscle of guinea pig stomach and this mechanism affects the membrane potential electrogenically.

  • PDF

Evaluation of Ascorbic Acid Treatment in Clinical and Subclinical Mastitis of Indian Dairy Cows

  • Naresh, Ram;Dwivedi, S.K.;Swarup, D.;Patra, R.C.
    • Asian-Australasian Journal of Animal Sciences
    • /
    • v.15 no.6
    • /
    • pp.905-911
    • /
    • 2002
  • A study was carried out to assess the therapeutic effect of ascorbic acid in mastitis of dairy cows. The herd with a population of 250-275 lactating cows was screened for clinical and subclinical mastitis for a period of 5 months. Based on inclusion and exclusion criteria, eighteen animals each with clinical and subclinical mastitis in one quarter only were selected as study population. Twelve cows (group A) with normal udder and health were also selected as a healthy control. Clinical mastitis cows were grouped as B (n=12) and C (n=6). Cows of group B were treated with ascorbic acid at 25 mg/kg, subcutaneously for 5 consecutive days and intramammary infusion (Ampicillin sodium 75 mg and Cloxacillin sodium 200 mg/infusion) based on antibiotic sensitivity test, till complete recovery. Group C cows received only intramammary infusion till the complete recovery. Eighteen subclinical mastitis cows were divided in group D (n=12) and E (n=6). Cows of group D were treated with ascorbic acid at 25 mg/kg subcutaneously for 5 consecutive days while group E did not receive any treatment. California mastitis test (CMT), somatic cell count (SCC), physical changes of udder and milk were used to diagnose and classify the mastitis. Evaluation of the therapy was based on CMT score and physical changes of udder and milk. Sample size calculation was also performed but was not followed for control groups due to scarcity of cases. Adequate blinding was done when and where required to avoid the biases. Confounding variables like herd, age of the cow, stage of the lactation, season and geographical region were duly considered and adequate blocking was followed. Ascorbic acid was administered in clinical and subclinical cases even after cure considering its immunostimulatory and healing inducing effects. The recovery rate was faster in cases of clinical mastitis treated with ascorbic acid along with an intramammary infusion (group B) than the quarters of group C cows. Quarter wise the average duration/number (3.16${\pm}$0.11 days) of antimicrobial intramammary infusion was significantly (p<0.01) less in group B than that of average duration/number (5.33${\pm}$0.20 days) of group C. Subclinical mastitis cows treated with ascorbic acid showed 83.33% recovery while 16.77% did not respond to treatment till last day of study. Cows of group E (untreated) did not recovered from the mastitis. Subjective parameters viz. swelling, pain reflex of udder and physical changes in milk from quarter of ascorbic acid treated cows (group B) disappeared earlier than that of group C cows. It is concluded from this study that the ascorbic acid might be useful as an adjunct in case of clinical mastitis to get quick recovery with less number of intramammary infusions. High recovery rate in subclinical mastitis quarters of group D cows is appreciable and opens a new avenue to conduct further trials in a larger population in various field conditions. However, the pharmacology of ascorbic acid with particular reference to health of mammary gland needs to be investigated.

Inhibitory Effect on RANKL-Induced Osteoclast Differentiation by Water Extract of Zizyphus Jujuba Mill (대추 물 추출물이 RANKL에 의해 유도되는 파골세포 분화에 미치는 영향)

  • Yoon, Kang Hugh;Baek, Jong Min;Kim, Ju Young;Kwak, Seong Cheoul;Cheon, Yoon Hee;Jeon, Byung Hoon;Lee, Chang Hoon;Choi, Min Kyu;Oh, Jaemin;Lee, Myeung Su;Kim, Jeong Joong
    • Journal of Physiology & Pathology in Korean Medicine
    • /
    • v.28 no.1
    • /
    • pp.29-34
    • /
    • 2014
  • Bone homeostasis is maintained by balance between bone resorbing-osteoclasts and bone forming-osteoblasts. Excessive osteoclastic bone resorption plays a critical role in bone destruction in pathological bone diseases such as osteoporosis, rheumatoid arthritis, and periodontal disease. Many compounds derived from natural products have pharmacological applications and have therapeutic value for treating or preventing several bone diseases characterized by excessive bone resorption. To discover new compounds that can act as anti-resorptive agents, we screened for natural compounds that regulate osteclast differentiation, and found that water extract of Ziziphus Jujuba Mill (WEZJ) has inhibitory effects on osteoclast differentiation. In this study, WEZJ clearly inhibits the osteoclast differentiation in the presence of receptor activator of nuclear factor kB (RANKL), macrophage colony-stimulating factor (M-CSF) without cytoxicity by blocking activation of nuclear factor of activated T cells (NFAT)c1, and c-Fos. In signaling pathway, the phosphorylation of Akt, p38, c-Jun N-terminal kinases (JNK), extracellular signal-regulated kinases (ERK) and the expression of osteoclast-associated receptor (OSCAR), tartrate-resistant acid phosphates (TRAP), Integrin av, Integrin b3, Cathepsin K are suppressed, too. These result suggest that WEZJ may have therapeutic value for treating or preventing several bone diseases characterized by excessive bone destruction.