• The Korean Journal of Physiology and Pharmacology
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• v.21 no.2
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• pp.169-177
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• 2017

Lamotrigine is an antiepileptic drug widely used to treat epileptic seizures. Using whole-cell voltage clamp recordings in combination with a fast drug application approach, we investigated the effects of lamotrigine on 5-hydroxytryptamine $(5-HT)_3$ receptors in NCB-20 neuroblastoma cells. Co-application of lamotrigine ($1{\sim}300{\mu}M$) resulted in a concentration-dependent reduction in peak amplitude of currents induced by $3{\mu}m$ of 5-HT for an $IC_{50}$ value of $28.2{\pm}3.6{\mu}M$ with a Hill coefficient of $1.2{\pm}0.1$. These peak amplitude decreases were accompanied by the rise slope reduction. In addition, $5-HT_3$-mediated currents evoked by 1 mM dopamine, a partial $5-HT_3$ receptor agonist, were inhibited by lamotrigine co-application. The $EC_{50}$ of 5-HT for $5-HT_3$ receptor currents were shifted to the right by co-application of lamotrigine without a significant change of maximal effect. Currents activated by 5-HT and lamotrigine co-application in the presence of 1 min pretreatment of lamotrigine were similar to those activated by 5-HT and lamotrigine co-application alone. Moreover, subsequent application of lamotrigine in the presence of 5-HT and 5-hydroxyindole, known to attenuate $5-HT_3$ receptor desensitization, inhibited $5-HT_3$ receptor currents in a concentration-dependent manner. The deactivation of $5-HT_3$ receptor was delayed by washing with an external solution containing lamotrigine. Lamotrigine accelerated the desensitization process of $5-HT_3$ receptors. There was no voltage-dependency in the inhibitory effects of lamotrigine on the $5-HT_3$ receptor currents. These results indicate that lamotrigine inhibits $5-HT_3$-activated currents in a competitive manner by binding to the open state of the channels and blocking channel activation or accelerating receptor desensitization.

• Journal of Periodontal and Implant Science
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• v.26 no.3
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• pp.669-679
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• 1996

Gingival overgrowth is a well known side effect of several drugs, including nifedipine, phenytoin, cyclosporin, dilitiazem, verapamil. A number of studies have been performed to investigate the mechanism by which nifedipine(a calcium channel blocking agent) affects the gingival tissue. The aim of the present work was to investigate the effect of nifedipine on healthy gingival fibroblasts with special emphasis on determining the changes in cellular proliferation and protein and collagen synthesis. Gingival fibroblasts were obtained from the explants of healthy gingiva of extracted 3rd molars or premolar teeth extracted from the patients for orthodontic treatment. To evaluate the effect of nifedipine on cell proliferation, the cells were seeded at a cell density of $1{\times}10^4$cells/well in 24-well culture plates and treated with 100 and 200ng/ml of nifedipine for 10days. After trypsinization, the cells were counted with a haemocytometer on 1st, 3rd, 5th, 7th and 10th days. Then, MTT assay was carried out. For total protein and percent collagen synthesis, $3{\mu}Ci/ml$ $^3H-proline$ was added to each well for the final 4 hours of the incubation period. The results indicate that nifedipine does not influence cell proliferation in healthy gingival fibroblast in vitro and has a specific effect in reducing total protein and percent collagen synthesis. On the above the findings, exogenous nifedipine does not influence on healthy human gingival fibroblast proliferation and protein and collagen synthesis.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1996.04a
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• pp.175-175
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• 1996

The spinal dorsal horn is the area where primary afferent fibers terminate and cutaneous sensory information is Processed. A number of putative neurotransmitter substances, including excitatory and inhibitory amino acids and peptides, are present in this region and sites and cellular mechanisms of their actions have been a target of numerous studies. In this study, single neurons were acutely isolated and the properties of whole cell current and responses to excitatory and inhibitory neurotransmitters were studied by the patch clamp method. Young rats (7-14 days) were anesthetized with diethyl-ether, and the lumbar spinal cord was excised and cut transversely at a thickness of 30$\mu\textrm{m}$ by Vibroslicer. The treatment of spinal slices with low concentration of proteases (pronase and thermolysin 0.75 mg/$m\ell$) and mechanical dissociation yielded isolated neurons with near intact morphology. Multipolar, ellipsoidal and bipolar, and pyramidal cells were shown. By applying step voltage pulses to neurons held at -70 mV, two types of inward currents and one outward currents observed. The fast activating and inactivating inward current was the Na$\^$+/ current because of its fast kinetics and blocking by 0.5${\mu}$M TTX, a specific blocker of Na$\^$+/ channel. The second type of inward currents were sustained. Based on their kinetics and current-voltage relations, it was likely that the second type of inward current was the voltage-dependent Ca$\^$2+/ current. In the presence of TTX, the steady-state currents mainly represented outward K$\^$+/ current which looked like the delayed rectifier K$\^$+/ current. In addition, the membrane currents produced by agonist of excitatory amino acid (EAA) receptor and the endogenous transmitter candidate L-glutamate were recorded in isolated whole-cell voltage clamped neurons as well as responses to inhibitory amino acids (${\gamma}$-amino butyric acid, glycine). Drugs were applied by a method that allows complete exchange of the solution within 1 sec; an infinite number of solutions can be applied to a single cell.

• Journal of Pharmaceutical Investigation
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• v.27 no.1
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• pp.57-64
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• 1997

$Amino-{\beta}-lactam$ antibiotics are absorbed by the dipeptide transporter in the small intestine. These uptakes are coupled to a proton influx. The inward proton gradient is partly induced by the $Na^+/H^+$ exchanger and calcium ion is involved in control of this antiport. Interaction between ampicillin which is one of the $Amino-{\beta}-lactam$ antibiotics and nifedipine which is one of calcium channel blocking agents was studied in rats in vivo and with rabbit jejunum mounted on the Sweetana/Grass diffusion cells in vitro. Bioavailability of ampicillin was increased significantly when nifedipine was co-administered orally in rats. There were no differences in the distribution phase and the elimination phase when ampicillin was given either alone or with nifedipine intravenously. Conditions for in vitro experiments were determined. The lift rate of $O_2/CO_2$ gas was controlled to 3 bubbles/sec and ampicillin was stable in the Kreb's buffer at pH 6.0. Absorption of ampicillin was the greatest when the completely-stripped serosal membrane was used. Transport of ampicillin from mucosal to serosal side in the rabbit jejunum was enhanced by 32% in the presence of nifedipine (p=0.059). Above results suggest that nifedipine might increase the plasma level of ampicillin via the improved absorption in the intestine rather than the reduction in the elimination or/and alteration in the distribution.

• The Korean Journal of Physiology and Pharmacology
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• v.16 no.5
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• pp.343-348
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• 2012

Blocking or regulating $K^+$ channels is important for investigating neuronal functions in mammalian brains, because voltage-dependent $K^+$ channels (Kv channels) play roles to regulate membrane excitabilities for synaptic and somatic processings in neurons. Although a number of toxins and chemicals are useful to change gating properties of Kv channels, specific effects of each toxin on a particular Kv subunit have not been sufficiently demonstrated in neurons yet. In this study, we tested electro-physiologically if heteropodatoxin2 ($HpTX_2$), known as one of Kv4-specific toxins, might be effective on various $K^+$ outward currents in CA1 neurons of organotypic hippocampal slices of rats. Using a nucleated-patch technique and a pre-pulse protocol in voltage-clamp mode, total $K^+$ outward currents recorded in the soma of CA1 neurons were separated into two components, transient and sustained currents. The extracellular application of $HpTX_2$ weakly but significantly reduced transient currents. However, when $HpTX_2$ was added to internal solution, the significant reduction of amplitudes were observed in sustained currents but not in transient currents. This indicates the non-specificity of $HpTX_2$ effects on Kv4 family. Compared with the effect of cytosolic 4-AP to block transient currents, it is possible that cytosolic $HpTX_2$ is pharmacologically specific to sustained currents in CA1 neurons. These results suggest that distinctive actions of $HpTX_2$ inside and outside of neurons are very efficient to selectively reduce specific $K^+$ outward currents.

• The Korean Journal of Physiology and Pharmacology
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• v.17 no.1
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• pp.37-42
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• 2013

Taxifolin glycoside is a new drug candidate for the treatment of atopic dermatitis (AD). Many drugs cause side effects such as long QT syndrome by blocking the human ether-a-go-go related gene (hERG) $K^+$ channels. To determine whether taxifolin glycoside would block hERG $K^+$ channels, we recorded hERG $K^+$ currents using a whole-cell patch clamp technique. We found that taxifolin glycoside directly blocked hERG $K^+$ current in a concentration-dependent manner ($EC_{50}=9.6{\pm}0.7{\mu}M$). The activation curve of hERG $K^+$ channels was negatively shifted by taxifolin glycoside. In addition, taxifolin glycoside accelerated the activation time constant and reduced the onset of the inactivation time constant. These results suggest that taxifolin glycoside blocks hERG $K^+$ channels that function by facilitating activation and inactivation process.

• Journal of Satellite, Information and Communications
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• v.7 no.3
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• pp.1-7
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• 2012

In this paper, we was performed the interference analysis to determine an optimal coexisting criteria for the european digital video broadcasting service (DVB-T2) and the IMT-advanced LTE based TV Band Device (TVBD). The TVBD was equipped with the spectrum cognition method. To this end, we set the various transmission parameters, that includes the emission and blocking mask, antenna height and gain, transmission power and bandwidth, channel model etc. Based on this parameters, we were calculated the allowable transmit power, the number of TVBD and the change in probability of interference for the TVBD user operating in the adjacent channels of the DVB-T2 user. Also this paper presents how many TVBD users can sharing with DVB-T2 for spectral cognition performance.

• The Journal of Korean Obstetrics and Gynecology
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• v.20 no.2
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• pp.83-96
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• 2007

Purpose: Ligustri Lucidi Fructus and Ecliptae Herba has long been used for clinical therapy associated especially with menopausal symptoms in Korea. To provide a scientific rationale for such use, we have investigated the antioxidant and vasorelaxant effects of Ligustri Lucidi Fructus, Ecliptae Herba and its mixture. Methods: The antioxidant activity of the extracts from Ligustri Lucidi Fructus, Ecliptae Herba and its mixture were evaluated and compared with that of BHA (butylated hydroxyanisole), BHT (butylated hydroxytoluene), vitamin C and vitamin E, using the ${\alpha}$,${\alpha}-diphenyl-{\beta}-picrylhydrazyl$ (DPPH) radical scavenging method. Results: Antioxidant activity of all extracts using the DPPH radical scavenging method decreased in the order vitamin C>BHA>vitamin E>Ligustri Lucidi Fructus>Ligustri Lucidi Fructus:Ecliptae Herba(1:1)>Ecliptae Herba>BHT. The vasorelaxant effects of extracts were investigated on the vasomotor tone of the rat thoracic aorta in an organ bath. All of the extracts elicited along-term relaxing response in the endothelium-intact as well as endothelium-denuded rat aorta contracted with norepinephrine. This relaxant effect was abolished by Precontraction with 72 mM KCI. Thus, it is suggested that the mechanism of vasorelaxant effect of extracts not involve voltage-operated $Ca^{2+}$ channel blocking but receptor-mediated route. Conclusion: These antioxidant and vasorelaxant effecs of the extracts may contribute to the beneficial effects in postmenopausal women.

• Journal of the Institute of Electronics Engineers of Korea TC
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• v.37 no.2
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• pp.17-23
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• 2000

Wireless link has high bit error rate compared with wired link and many users share this limited bandwidth. So it needs more powerful error control code and efficient media access control(MAC) to provide multimedia service reliably. In this paper we proposed efficient MAC frame format based on TDMA using mini-slot for request access. The number of mini-slots is variable based on the result of collision in the previous frame. This dynamic allocation of request mini-slots helps resolve the contention situation quickly and avoids the waste of bandwidth that may occur when there are several unneeded request mini-slots. The simulation results are also presented in terms of channel utilization, call blocking probability and cell transmission delay for mixed traffic environment.

• Journal of the Institute of Electronics Engineers of Korea TC
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• v.40 no.12
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• pp.46-58
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• 2003

The recent Internet is changing from its best-effort service and needs the network structure and traffic engineering, which can support various applications requiring differentiated traffic processing and high quality of service. The extension of the Internet from wired to wireless system generating location-dependent and burst errors make more difficult to support a good service with the existing packet scheduling algorithm. In this paper, we propose a wireless diffserv packet scheduling (WDSPS) algorithm that can provide reliable service in the differentiated wireless internet service network. The proposed scheduling algorithm solves the HOL(head of line) blocking problems of class queue occurred in wireless network, supports the differentiated service for each class which is defined in differentiated service networks and makes possible the gradual and efficient service compensation not only among classes but also among flows to prevent the monopoly of one class or one flow. Through simulations, we show that our proposed WDSPS scheduling algorithm can provide the required QoS differentiation between classes and enhance the service throughput in various wireless network conditions.