• Title/Summary/Keyword: Ion Channel

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Influence of the Central Benzodiazepinergic System on Peripheral Cardiovascular Regulation

  • Koh, Jeong-Tae;Ju, Jeong-Min;Shin, Dong-Ho;Cho, Han-Ho;Choi, Bong-Kyu;Kim, Jae-Ha
    • The Korean Journal of Physiology and Pharmacology
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    • v.2 no.3
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    • pp.287-295
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    • 1998
  • Diazepam is known to have cardiovascular depressive effects through a combined action on benzodiazepinergic receptor and the GABA receptor-chloride ion channel complex. Moreover, it is known that barbiturates also have some cardiovascular regulatory effects mediated by the central GABAergic system. Therefore, this study was undertaken to delineate the regulatory actions and interactions of these systems by measuring the responses of the cardiovascular system and renal nerve activity to muscimol, diazepam and pentobarbital, administered intracerebroventricularly in rabbits. When muscimol $(0.03{\sim}0.3\;{\mu}\;g/kg)$, diazepam $(10{\sim}100\;{\mu}\;g/kg)$ and pentobarbital $(1{\sim}10\;{\mu}\;g/kg)$ were injected into the lateral ventricle of the rabbit brain, there were similar dose-dependent decreases in blood pressure (BP) and renal nerve activity (RNA). The relative potency of the three drugs in decreasing BP and RNA was muscimol > pentobarbital > diazepam. Muscimol and pentobarbital also decreased the heart rate in a dose-dependent manner; however, diazepam produced a trivial, dose-independent decrease in heart rate. Diazepam $(30\;{\mu}g/kg)$ augmented the effect of muscimol $(0.1\;{\mu}g/kg)$ in decreasing blood pressure and renal nerve activity, but pentobarbital $(3\;{\mu}g/kg)$ did not. Bicuculline $(0.5\;{\mu}g/kg)$, a GABAergic receptor blocker, significantly attenuated the effect of muscimol in decreasing BP and RNA, either alone or with diazepam, and that of pentobarbital in decreasing BP and RNA, either alone or with muscimol. We inferred that the central benzodiazepinergic and barbiturate systems help regulate peripheral cardiovascular function by modulating the GABAergic system, which adjusts the output of the vasomotor center and hence controls peripheral sympathetic tone. Benzodiazepines more readily modulate the GABAergic system than barbiturates.

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Extracellular ATP Stimulates $Na^+\;and\;Cl^-$ Transport through the Activation of Multiple Purinergic Receptors on the Apical and Basolateral Membranes in M-1 Mouse Cortical Collecting Duct Cells

  • Jung, Jin-Sup;Hwang, Sook-Mi;Lee, Ryang-Hwa;Kang, Soo-Kyung;Woo, Jae-Suk;Kim, Yong-Keun
    • The Korean Journal of Physiology and Pharmacology
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    • v.5 no.3
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    • pp.231-241
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    • 2001
  • The mammalian cortical collecting duct (CCD) plays a major role in regulating renal NaCl reabsorption, which is important in $Na^+$ and $Cl^-$ homeostasis. The M-1 cell line, derived from the mouse cortical collecting duct, has been used as a mammalian model of the study on the electrolytes transport in CCD. M-1 cells were grown on collagen-coated permeable support and short circuit current $(I_{sc})$ was measured. M-1 cells developed amiloride-sensitive current $5{\sim}7$ days after seeding. Apical and basolateral addition of ATP induced increase in $I_{sc}$ in M-1 cells, which was partly retained in $Na^+-free$ or $Cl^--free$ solution, indicating that ATP increased $Na^+$ absorption and $Cl^-$ secretion in M-1 cells. $Cl^-$ secretion was mediated by the activation of apical cystic fibrosis transmembrane regulator (CFTR) chloride channels and $Ca^{2+}-activated$ chloride channels, but $Na^+$ absorption was not mediated by activation of epithelal sodium channel (ENaC). ATP increased cAMP content in M-1 cells. The RT-PCR analysis demonstrated that M-1 cells express $P2Y_2,\;P2X_3\;and\;P2Y_4$ receptors. These results showed that ATP regulates $Na^+$ and $Cl^-$ transports via multiple P2 purinoceptors on the apical and basolateral membranes in M-1 cells.

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Glycine- and GABA-mimetic Actions of Shilajit on the Substantia Gelatinosa Neurons of the Trigeminal Subnucleus Caudalis in Mice

  • Yin, Hua;Yang, Eun-Ju;Park, Soo-Joung;Han, Seong-Kyu
    • The Korean Journal of Physiology and Pharmacology
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    • v.15 no.5
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    • pp.285-289
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    • 2011
  • Shilajit, a medicine herb commonly used in Ayurveda, has been reported to contain at least 85 minerals in ionic form that act on a variety of chemical, biological, and physical stressors. The substantia gelatinosa (SG) neurons of the trigeminal subnucleus caudalis (Vc) are involved in orofacial nociceptive processing. Shilajit has been reported to be an injury and muscular pain reliever but there have been few functional studies of the effect of Shilajit on the SG neurons of the Vc. Therefore, whole cell and gramicidin-perfotrated patch clamp studies were performed to examine the action mechanism of Shilajit on the SG neurons of Vc from mouse brainstem slices. In the whole cell patch clamp mode, Shilajit induced short-lived and repeatable inward currents under the condition of a high chloride pipette solution on all the SG neurons tested. The Shilajit-induced inward currents were concentration dependent and maintained in the presence of tetrodotoxin (TTX), a voltage gated $Na^+$ channel blocker, CNQX, a non-NMDA glutamate receptor antagonist, and AP5, an NMDA receptor antagonist. The Shilajit-induced responses were partially suppressed by picrotoxin, a $GABA_A$ receptor antagonist, and totally blocked in the presence of strychnine, a glycine receptor antagonist, however not affected by mecamylamine hydrochloride (MCH), a nicotinic acetylcholine receptor antagonist. Under the potassium gluconate pipette solution at holding potential 0 mV, Shilajit induced repeatable outward current. These results show that Shilajit has inhibitory effects on the SG neurons of Vc through chloride ion channels by activation of the glycine receptor and $GABA_A$ receptor, indicating that Shilajit contains sedating ingredients for the central nervous system. These results also suggest that Shilajit may be a potential target for modulating orofacial pain processing.

Quercetin-induced Growth Inhibition in Human Bladder Cancer Cells Is Associated with an Increase in $Ca^{2+}$-activated $K^+$ Channels

  • Kim, Yang-Mi;Kim, Wun-Jae;Cha, Eun-Jong
    • The Korean Journal of Physiology and Pharmacology
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    • v.15 no.5
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    • pp.279-283
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    • 2011
  • Quercetin (3,3',4',5,7-pentahydroxyflavone) is an attractive therapeutic flavonoid for cancer treatment because of its beneficial properties including apoptotic, antioxidant, and antiproliferative effects on cancer cells. However, the exact mechanism of action of quercetin on ion channel modulation is poorly understood in bladder cancer 253J cells. In this study, we demonstrated that large conductance $Ca^{2+}$-activated $K^+$ ($BK_{Ca}$) or MaxiK channels were functionally expressed in 253J cells, and quercetin increased $BK_{Ca}$ current in a concentration dependent and reversible manner using a whole cell patch configuration. The half maximal activation concentration ($IC_{50}$) of quercetin was $45.5{\pm}7.2{\mu}m$. The quercetin-evoked $BK_{Ca}$ current was inhibited by tetraethylammonium (TEA; 5 mM) a non-specific $BK_{Ca}$ blocker and iberiotoxin (IBX; 100 nM) a $BK_{Ca}$-specific blocker. Quercetin-induced membrane hyperpolarization was measured by fluorescence-activated cell sorting (FACS) with voltage sensitive dye, bis (1,3-dibutylbarbituric acid) trimethine oxonol ($DiBAC_4$2(3); 100 nM). Quercetin-evoked hyperpolarization was prevented by TEA. Quercetin produced an antiproliferative effect ($30.3{\pm}13.5%$) which was recovered to $53.3{\pm}10.5%$ and $72.9{\pm}3.7%$ by TEA and IBX, respectively. Taken together our results indicate that activation of $BK_{Ca}$ channels may be considered an important target related to the action of quercetin on human bladder cancer cells.

Porosity Control in LSM Electrode Formation in Layered Plannar SOFC Module (적층 평판형 SOFC에서 LSM 전극의 기공 제어)

  • Lee, Won-Jun;Yeo, Dong-Hun;Shin, Hyo-Soon;Jeong, Dea-Yong
    • Journal of the Korean Institute of Electrical and Electronic Material Engineers
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    • v.27 no.12
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    • pp.866-870
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    • 2014
  • In solid oxide fuel cell system, yttria-stabilized zirconia is generally adopted as the electrolyte, which has high strength and superior oxygen ion conductivity, and the air electrode and the fuel electrode are attached to this. Recently, new structure of 'layered planar SOFC module' was suggested to solve the reliability problem due to the high temperature stability of a sealing agent and a binding material. In this study to materialize the air electrode in a layered planar SOFC module, the LSM ink was coated to form homogeneous electrode in the channel after the ink preparation. As the porosity control agent, PMMA or active carbon powder was adopted with use of a commercial dispersant in ethanol. The optimal amounts of both the porosity control agents and the dispersant were determined. Four (4) vol% of the dispersant for the LSM-PMMA case and 15 vol% for LSM-carbon powder showed the lowest viscosities respectively to indicate the best dispersed states of the slurries. With PMMA and carbon powder, sintered LSM ink shows the relatively homogeneous distributions of pores and with increases of the agents, the porosities increased in both cases. From this, it can be thought that the amount of the PMMA or carbon powder could be used to control the porosity of the LSM ink.

Thermal and Chemical Quenching Phenomena in a Microscale Combustor (II)- Effects of Physical and Chemical Properties of SiOx(x≤2) Plates on flame Quenching - (마이크로 연소기에서 발생하는 열 소염과 화학 소염 현상 (II)- SiOx(x≤2) 플레이트의 물리, 화학적 성질이 소염에 미치는 영향 -)

  • Kim Kyu-Tae;Lee Dae-Hoon;Kwon Se-Jin
    • Transactions of the Korean Society of Mechanical Engineers B
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    • v.30 no.5 s.248
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    • pp.405-412
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    • 2006
  • In order to realize a stably propagating flame in a narrow channel, flame instabilities resulting from flame-wall interaction should be avoided. In particular flame quenching is a significant issue in micro combustion devices; quenching is caused either by excessive heat loss or by active radical adsorptions at the wall. In this paper, the relative significance of thermal and chemical effects on flame quenching is examined by means of quenching distance measurement. Emphasis is placed on the effects of surface defect density on flame quenching. To investigate chemical quenching phenomenon, thermally grown silicon oxide plates with well-defined defect distribution were prepared. ion implantation technique was used to control defect density, i.e. the number of oxygen vacancies. It has been found that when the surface temperature is under $300^{\circ}C$, the quenching distance is decreased on account of reduced heat loss; as the surface temperature is increased over $300^{\circ}C$, however, quenching distance is increased despite reduced heat loss effect. Such abberant behavior is caused by heterogeneous surface reactions between active radicals and surface defects. The higher defect density, the larger quenching distance. This result means that chemical quenching is governed by radical adsorption that can be parameterized by oxygen vacancy density on the surface.

Design and Fabrication of Flexible OTFTs by using Nanocantact Printing Process (미세접촉프린팅 공정을 이용한 유연성 유기박막소자(OTFT)설계 및 제작)

  • Jo Jeong-Dai;Kim Kwang-Young;Lee Eung-Sug;Choi Byung-Oh;Esashi Masayoshi
    • Proceedings of the Korean Society of Precision Engineering Conference
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    • 2005.10a
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    • pp.506-508
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    • 2005
  • In general, organic TFTs are comprised of four components: gate electrode, gate dielectric, organic active semiconductor layer, and source and drain contacts. The TFT current, in turn, is typically determined by channel length and width, carrier field effect mobility, gate dielectric thickness and permittivity, contact resistance, and biasing conditions. More recently, a number of techniques and processes have been introduced to the fabrication of OTFT circuits and displays that aim specifically at reduced fabrication cost. These include microcontact printing for the patterning of metals and dielectrics, the use of photochemically patterned insulating and conducting films, and inkjet printing for the selective deposition of contacts and interconnect pattern. In the fabrication of organic TFTs, microcontact printing has been used to pattern gate electrodes, gate dielectrics, and source and drain contacts with sufficient yield to allow the fabrication of transistors. We were fabricated a pentacene OTFTs on flexible PEN film. Au/Cr was used for the gate electrode, parylene-c was deposited as the gate dielectric, and Au/Cr was chosen for the source and drain contacts; were all deposited by ion-beam sputtering and patterned by microcontact printing and lift-off process. Prior to the deposition of the organic active layer, the gate dielectric surface was treated with octadecyltrichlorosilane(OTS) from the vapor phase. To complete the device, pentacene was deposited by thermal evaporation and patterned using a parylene-c layer. The device was shown that the carrier field effect mobility, the threshold voltage, the subthreshold slope, and the on/off current ratio were improved.

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Regulation of Transient Receptor Potential Melastatin 7 (TRPM7) Currents by Mitochondria

  • Kim, Byung Joo;Jeon, Ju-Hong;Kim, Seon Jeong;So, Insuk;Kim, Ki Whan
    • Molecules and Cells
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    • v.23 no.3
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    • pp.363-369
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    • 2007
  • Mitochondria play a central role in energy-generating processes and may be involved in the regulation of channels and receptors. Here we investigated TRPM7, an ion channel and functional kinase, and its regulation by mitochondria. Proton ionophores such as CCCP elicited a rapid decrease in outward TRPM7 whole-cell currents but a slight increase in inward currents with pipette solutions containing no MgATP. With pipette solutions containing 3 mM MgATP, however, CCCP increased both outward and inward TRPM7 currents. This effect was reproducible and fully reversible, and repeated application of CCCP yielded similar decreases in current amplitude. Oligomycin, an inhibitor of $F_1/F_O$-ATP synthase, inhibited outward whole-cell currents but did not affect inward currents. The respiratory chain complex I inhibitor, rotenone, and complex III inhibitor, antimycin A, were without effect as were kaempferol, an activator of the mitochondrial $Ca^{2+}$ uniporter, and ruthenium red, an inhibitor of the mitochondrial $Ca^{2+}$ uniporter. These results suggest that the inner membrane potential (as regulated by proton ionophores) and the $F_1/F_O$-ATP synthase of mitochondria are important in regulating TRPM7 channels.

Spray coating of electrochemically exfoliated graphene/conducting polymer hybrid electrode for organic field effect transistor

  • Kim, Youn;Kwon, Yeon Ju;Hong, Jin-Yong;Park, Minwoo;Lee, Cheol Jin;Lee, Jea Uk
    • Journal of Industrial and Engineering Chemistry
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    • v.68
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    • pp.399-405
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    • 2018
  • We report the fabrication of organic field-effect transistors (OFETs) via spray coating of electrochemically exfoliated graphene (EEG) and conducting polymer hybrid as electrodes. To reduce the roughness and sheet resistance of the EEG electrodes, subsequent coating of conducting polymer (poly(3,4-ethylenedioxythiophene)-poly(styrenesulfonate) (PEDOT:PSS)) and acid treatment was performed. After that, active channel layer was developed by spin coating of semiconducting poly(3-hexylthiophene) on the hybrid electrodes to define the bottom gate bottom contact configuration. The OFET devices with the EEG/PEDOT:PSS hybrid electrodes showed a reasonable electrical performances (field effect mobility = $0.15cm^2V^{-1}\;s^{-1}$, on/off current ratio = $10^2$, and threshold voltage = -1.57V). Furthermore, the flexible OFET devices based on the Polydimethlsiloxane (PDMS) substrate and ion gel dielectric layer exhibited higher electrical performances (field effect mobility = $6.32cm^2V^{-1}\;s^{-1}$, on/off current ratio = $10^3$, and threshold voltage = -1.06V) and excellent electrical stability until 1000 cycles of bending test, which means that the hybrid electrode is applicable to various organic electronic devices, such as flexible OFETs, supercapacitors, organic sensors, and actuators.

Influences of Hinge Region of a Systhetic Antimicrobial Peptide, Cecropin A(1-13)-Melittin(1-13) Hybrid on Antibiotic Activity

  • 신송엽;강주현;이동건;장소윤;서무열;김길룡;함경수
    • Bulletin of the Korean Chemical Society
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    • v.20 no.9
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    • pp.1078-1084
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    • 1999
  • A synthetic cecropin A(1-13)-melittin(1-13) [CA-ME] hybrid peptide was known to be an antimicrobial peptide having strong antibacterial, antifungal and antitumor activity with minimal cytotoxic effect against human erythrocyte. Analogues were synthesized to investigate the influences of the flexible hinge region of CA-ME on the antibiotic activity. Antibiotic activity of the peptides was measured by the growth inhibition against bac-terial, fungal and tumor cells and vesicle-aggregating or disrupting activity. The deletion of Gln-Gly-Ile (P1) or Gly-Gln-Gly-Ile-Gly (P3) from CA-ME brought about a significant decrease on the antibiotic activities. In contrast, Gly-Ile-Gly deletion (P2) from CA-ME or Pro insertion (P5) instead of Gly-Gln-Gly-Ile-Gly of CA-ME retained antibiotic activity. This result indicated that the flexible hinge or β-bend structure provided by Gly-Gln-Gly-Ile-Gly, Gln-Gly, or Pro in the central region of the peptides is requisite for its effective antibiotic activity and may facilitate easily the hydrophobic C-terminal region of the peptide to penetrate the lipid bilayers of the target cell membrane. In contrast, P4 and P6 with Gly-Gln-Gly-Pro-Gly or Gly-Gln-Pro in the central region of the peptide caused a drastic reduction on the antibiotic activities. This result suggested that the con-secutive β-bend structure provided by Gly-Gln-Gly-Pro-Gly or Gly-Gln-Pro in the central hinge region of the peptide seems to interrupt the ion channel/pore formation on the target cell membranes.