• 제목/요약/키워드: blocking effect

검색결과 904건 처리시간 0.031초

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

  • 이신웅;박영주;박인숙;이정수
    • 약학회지
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    • 제34권4호
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    • pp.224-237
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    • 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.

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

  • ;강호정
    • 생태와환경
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    • 제34권4호통권96호
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    • pp.261-266
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    • 2001
  • 이산화탄소 농도가 증가할 때에 북구 이탄 습지에서 나타나는 생지화학적 변화과정을 살펴보았다. 표면 식생을 포함한 온전한 코어를 북웨일스의 이탄습지로부터 채취하여, 높은 이산화탄소농도(700ppm)와 자연상태 (350ppm)환경에서 4개월간 배양하였다. 배양 후, 화학적인 저해제를 이용하여 습지 토양에서 미량기체의 생성과 소비를 측정하였다. 메탄의 경우, 불화메탄($CH_3F$)를 이용하여 메탄 산화율을 결정하였고, 질산화와 탈질작용을 측정하기위해 아세틸렌($C_2H_2$)저해 방법을 적용하였다. 이를 위해, 먼저 각 측정 방법을 습지 시료에 적합하도록 최적화 시켰고, 둘째로 두 수준의 이산화탄소에서 배양한 시료에 이 방법들을 적용하였다. 높은 이산화탄소 농도는 메탄의 생성량을 증가 시켰으나(210대 $100\;ng\;CH_4 g^{-1}\;hr^{-1}$), 메탄 산화의 양도 증가시켜서 (128대 $15\;ng\;CH_4 g^{-1}\;hr^{-1}$) 결국에는 순메탄 방출량에는 변화가 없었다. 아산화질소의 경우에는 증가된 발생량이 탈질 보다는 질산화 과정에서 생성된 것으로 사료된다. 이러한 변화들은 높은 이산화탄소 하에서 조류의 성장이 증가되어 야기된 것으로 추측된다.

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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
    • 한국수정란이식학회:학술대회논문집
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    • 한국수정란이식학회 2002년도 국제심포지엄
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    • pp.102-102
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    • 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.

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

  • 노태희;차정호;김창민;최용남
    • 한국과학교육학회지
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    • 제18권2호
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    • pp.161-171
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    • 1998
  • 본 연구에서는 입자수준의 애니메이션을 이용한 컴퓨터 보조수업 프로그램을 개발 적용하여 학습자의 개념 이해도, 과학 수업에 대한 태도, 학습동기에 미치는 효과를 분석하였다. 본 연구는 서울 시내 여자 중학교 2학년 2개 학급을 대상으로 '분자와 운동' 단원에 대하여 5차시 동안 실시되었다. 수업 처치 전에 GALT와 사전 학습동기 검사를 실시하고, 중간고사 과학 과목 성적을 조사하였다. GALT 점수는 구획변인으로 사용하였으며, 사전 학습동기 검사와 중간고사 과학 과목 성적을 공변인으로 사용하였다. 수업 처치 후, 개념 검사, 과학수업에 대한 태도 검사, 사후 학습동기 검사를 실시하였고, 처치 집단에 대하여 컴퓨터 보조수업에 대한 인식을 조사하였다. 연구 결과, 컴퓨터 보조수업 집단 학생들이 전통적 학습 집단에 비하여 분자의 운동성에 대한 오개념이 적었으나, 개념 이해도 측면에서 두 집단간에 유의미한 차이는 없었다. 그러나, 컴퓨터 보조수업이 과학 수업에 대한 태도와 학습동기에는 효과적이었다(p<.01). 학생들은 컴퓨터 보조수업에 대하여 전반적으로 긍정적으로 인식하였으나, 몇몇 학생들은 어수선한 수업 분위기를 지적하였으며, 화면에 제시된 일부 내용은 어려웠다고 답하였다.

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

  • 피국현;황원덕
    • 대한한의학방제학회지
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    • 제25권1호
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    • pp.51-68
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    • 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.

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

  • 곽내정;유성필;안재형;권동진
    • 한국콘텐츠학회논문지
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    • 제7권12호
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    • pp.346-354
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    • 2007
  • 저해상도 영상에서 고해상도 영상으로 영상을 확대할 경우 적용하는 보간법은 알고 있는 값을 기준으로 해서 보간 값을 추론한다. 이 과정에서 블러링과 블록화 현상 등이 발생한다. 기존의 보간법은 처리과정에서 주변의 값들에 적절한 가중치를 곱하여 더함으로 이러한 단점들을 보완하고자 한다. 제안방법은 원화소의 값을 주변의 정보를 고려하여 변형하고 이 화소값을 이용하여 보간 화소를 생성함으로 보간 영상의 화질을 개선한다. 먼저 대각 방향의 차이값을 이용하여 복잡영역과 평탄 영역으로 구분하고 복잡영역일 경우 주변 영역의 메디안 값과 원화소의 값을 이용하여 변형된 화소의 값을 구한다. 즉, 평탄 영역일 경우는 원화소의 값을, 복잡영역은 변형된 화소의 값을 이용하여 양선형 보간법을 적용하여 보간 값을 구한다. 제안 방법의 성능을 평가하기 위해 기존의 보간 방법과의 PSNR과 확대 영상의 화질을 비교하였다. 실험결과 제안 방법은 기존의 방법에 비해 PSNR을 개선하였고 화질도 우수함을 보여준다.

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

  • 김종인;이재원;홍성훈
    • 한국정보통신학회:학술대회논문집
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    • 한국정보통신학회 2013년도 춘계학술대회
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    • pp.820-823
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    • 2013
  • 최근 스마트폰, 카메라, 휴대용 기기 등의 확산으로 다양한 분야에서 영상의 화질 향상의 필요성이 증가하고 있다. 영상의 화질 향상에 큰 영향을 주는 방법이 명암대비 향상이며 명암대비를 향상시키는 대표적인 방법으로는 히스토그램 평활화 방법이 있으며 다양한 연구가 이루어지고 있다. 그러나 일반적인 히스토그램 평활화 방법은 밝기만을 재조정하는 방법으로써 히스토그램이 한 쪽으로 치우친 영상의 경우 과도한 밝기 변화로 인하여 블록현상과 같은 왜곡이 발생한다. 본 논문에서는 히스토그램 분포의 평균 밝기를 균형 있게 재 분포 및 압축을 통해서 명암대비 향상 기법을 제안한다. 제안한 방법은 과도한 명암대비 증가로 인한 과포화 현상을 억제하기 위하여 히스토그램 빈도수에 따라 히스토그램을 차등 압축 시키며, 한 쪽으로 치우친 히스토그램을 균형 있게 재배열함으로써 영상의 밝기를 균형 있게 한다. 실험결과 제안방법은 기존 방법에 비해 영상의 밝기가 균형적이며 기존 방법에 비해 과포화 현상 없이 좋은 명암대비 향상 효과를 보였다.

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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
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    • 제26권1호
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    • pp.55-68
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    • 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.

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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
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    • 제15권6호
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    • pp.905-911
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    • 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.

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

  • 윤강휴;백종민;김주영;곽성철;천윤희;전병훈;이창훈;최민규;오재민;이명수;김정중
    • 동의생리병리학회지
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    • 제28권1호
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    • pp.29-34
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    • 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.