• The Korean Journal of Pharmacology
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• v.24 no.1
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• pp.83-92
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• 1988

Although the release of lysosomal enzymes from activated PMN leukocyte can be regulated by intracellular cyclic nucleotide levels, other responses of PMN leukocyte according to the binding of neurotransmitters to either ${\beta}$-adrenergic or muscarinic receptors are still not clarified. In addition, the function of PMN leukocyte mediated by ${\alpha}$-adrenergic receptors is uncertain. Atropine, phentolamine and propranolol inhibited calcium uptake, superoxide generation, NADPH oxidase activity and phagocytic activity in activated PMN leukocyte, whereas carbachol and isoproterenol slightly further stimulated the responses of activated cells. Either carbachol or isoproterenol stimulated superoxide generation was inhibited by their antagonists, atropine and propranolol, respectively. The response of activated PMN leukocyte was inhibited by chlorpromazine, verapamil and dantrolene but slightly stimulated by lithium. On the other hand, chlorpromazine and dibucaine did not affect NADPH oxidase activity. Atropine, phentolamine and propranolol suppressed the calcium dependent phagocytic activity. Thus, the results suggest that atropine, phentolamine and propranolol may inhibit superoxide generation in activated PMN leukocyte by the inhibition of calcium influx and by their direct action on the NADPH oxidase system which is associated with autonomic receptors.

• The Korean Journal of Physiology and Pharmacology
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• v.18 no.1
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• pp.41-46
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• 2014

The possible roles of spinal histamine receptors in the regulation of the blood glucose level were studied in ICR mice. Mice were intrathecally (i.t.) treated with histamine 1 (H1) receptor agonist (2-pyridylethylamine) or antagonist (cetirizine), histamine 2 (H2) receptor agonist (dimaprit) or antagonist (ranitidine), histamine 3 (H3) receptor agonist (${\alpha}$-methylhistamine) or antagonist (carcinine) and histamine 4 (H4) receptor agonist (VUF 8430) or antagonist (JNJ 7777120), and the blood glucose level was measured at 30, 60 and 120 min after i.t. administration. The i.t. injection with ${\alpha}$-methylhistamine, but not carcinine slightly caused an elevation of the blood glucose level. In addition, histamine H1, H2, and H4 receptor agonists and antagonists did not affect the blood glucose level. In D-glucose-fed model, i.t. pretreatment with cetirizine enhanced the blood glucose level, whereas 2-pyridylethylamine did not affect. The i.t. pretreatment with dimaprit, but not ranitidine, enhanced the blood glucose level in D-glucose-fed model. In addition, ${\alpha}$-methylhistamine, but not carcinine, slightly but significantly enhanced the blood glucose level D-glucose-fed model. Finally, i.t. pretreatment with JNJ 7777120, but not VUF 8430, slightly but significantly increased the blood glucose level. Although histamine receptors themselves located at the spinal cord do not exert any effect on the regulation of the blood glucose level, our results suggest that the activation of spinal histamine H2 receptors and the blockade of spinal histamine H1 or H3 receptors may play modulatory roles for up-regulation and down-regulation, respectively, of the blood glucose level in D-glucose fed model.

• The Korean Journal of Pharmacology
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• v.19 no.2
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• pp.57-67
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• 1983

The influence of electrolyte concentrations on the action of morphine and naloxone was studied in the myenteric plexus-longitudinal muscle preparation of guinea-pig ileum to examine whether opiate receptor binding obseved in vitro with homogenates represents binding to the pharmacological receptor. The preparations were suspended in a modified Krebs-Henseleit bicarbonate buffer solution and electrically stimulated at 0.2 Hz. Morphine inhibited electrically evoked contractions; the concentration of morphine required for a 50-percent inhibition was 190 nM. This inhibitory action of morphine was potentiated in a medium containing lower concentrations of : $Na^+\;or\;K^+$, or by the addition of $Mn^{2+}$ to the medium, and weakened by increasing the concentration of $Ca^{2+}$ or decreasing the concentration of $Mg^{2+}$. Naloxone antagonized these actions of morphine: however, $pA_2values$ for naloxone (indices of affinity for antagonists, approximately 8.8) were unaffected by these electrolyte concentrations. Thus, changes in the inhibitory action of morphine caused by alterations in electrolyte concentrations are probably not the result of changes in the affinity of the receptor for opiates, but due to alterations in the events which precede or follow the receptor binding. Effects of electrolytes on the affinity of the functional opiate receptor for naloxone in guinea-pig ileum are apparently different from those reported with the specific binding sites for opiates in brain homogenate.

• Asian Journal of Turfgrass Science
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• v.26 no.1
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• pp.8-16
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• 2012

The objective of this study was to identify bacterial antagonists of R. solani AG2-2 (IV) on zoysiagrass and to evaluate their antifungal activity in vitro and in vivo to select an antagonistic isolate. Antagonistic isolates that inhibit large patch disease caused by R. solani AG2-2 (IV) in zoysiagrass were selected from several soils, and their antagonistic activities were investigated in vitro and in vivo. Of 216 bacterial isolates, 67 inhibited several plant pathogenic fungi. The isolates that inhibited stem-segment colonization by R. solani AG2-2 (IV) in zoysiagrass were tested in a growth chamber. Eleven isolates were active as plant growth promoting isolates. Among them, five plant growth promoting isolates and their concentration dependent efficiency on zoysiagrass following inoculation with R. solani AG2-2 (IV) was evaluated. Isolate H33 was one of the potential antagonistic isolates, and it was further tested against various plant pathogens. H33 not only suppressed the disease caused by R. solani AG2-2 (IV) on zoysiagrass but also promoted leaf weight and leaf height of zoysiagrass under growth chamber and greenhouse conditions. The H33 isolate, which belongs to Streptomyces arenae, was identified through physiological, biochemical, and 16S rDNA studies. Further studies will investigate the cultural characterization of S. arenae H33 and isolation and identification of antifungal substance produced by S. arenae H33.

• Journal of the korean academy of Pediatric Dentistry
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• v.38 no.3
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• pp.303-308
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• 2011

Tooth impaction refers to situations in which the eruption is inhibited by some physical barriers in eruptive path and the tooth remains unerupted beyond the normal time of eruption. The etiology of impacted tooth is controversial, but ankylosis has been suggested probably as a leading role. Impacted primary molars may cause several problems such as space loss, tipping of adjacent teeth, supra-eruption of the antagonists, dislocation of succeeding premolar, cystic change and infection. As one of conventional treatments of impacted primary molars, early tooth extraction or surgical extraction following space regaining when there is space loss has been suggested. However, when they are in normal formation and not ankylosed, orthodontic traction following surgical exposure can be the choice of treatment. In this case, a 3-year-old boy was referred to the department of pediatric dentistry for the unerupted mandibular right second primary molar. After surgical removal of gingiva on the occlusal surface, orthodontic traction was performed. After treatment, we could get normal alignment of primary teeth and the opportunity for normal development of permanent teeth.

• Biomedical Science Letters
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• v.23 no.3
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• pp.251-260
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• 2017

Platelet activation is essential at the sites of vascular injury, which leads to hemostasis through adhesion, aggregation, and secretion process. However, potent and continuous platelet activation may be an important reason of circulatory disorders. Therefore, proper regulation of platelet activation may be an effective treatment for vascular diseases. In this research, inhibitory effects of cordycepin (3'-deoxyadenosine) on platelet activation were determined. As the results, cordycepin increased cAMP and cGMP, which are intracellular $Ca^{2+}$-antagonists. In addition, cordycepin reduced collagen-elevated $[Ca^{2+}]_i$ mobilization, which was increased by a cAMP-dependent protein kinase (PKA) inhibitor (Rp-8-Br-cAMPS), but not a cGMP-protein kinase (PKG) inhibitor (Rp-8-Br-cGMPS). Furthermore, cordycepin increased $IP_3RI$ ($Ser^{1756}$) phosphorylation, indicating inhibition of $IP_3$-mediated $Ca^{2+}$ release from internal store via the $IP_3RI$, which was strongly inhibited by Rp-8-Br-cAMPS, but was not so much inhibited by Rp-8-Br-cGMPS. These results suggest that the reduction of $[Ca^{2+}]_i$ mobilization is caused by the cAMP/A-kinase-dependent $IP_3RI$ ($Ser^{1756}$) phosphorylation. In addition, cordycepin increased the phosphorylation of VASP ($Ser^{157}$) known as PKA substrate, but not VASP ($Ser^{239}$) known as PKG substrate. Cordycepin-induced VASP ($Ser^{157}$) phosphorylation was inhibited by Rp-8-Br-cAMPS, but was not inhibited by Rp-8-Br-cGMPS, and cordycepin inhibited collagen-induced fibrinogen binding to ${\alpha}IIb/{\beta}_3$, which was increased by Rp-8-Br-cAMPS, but was not inhibited by Rp-8-Br-cGMPS. These results suggest that the inhibition of ${\alpha}IIb/{\beta}_3$ activation is caused by the cAMP/A-kinase-dependent VASP ($Ser^{157}$) phosphorylation. In conclusion, these results demonstrate that inhibitory effects of cordycepin on platelet activation were due to inhibition of $[Ca^{2+}]_i$ mobilization through cAMP-dependent $IP_3RI$ ($Ser^{1756}$) phosphorylation and suppression of ${\alpha}IIb/{\beta}_3$ activation through cAMP-dependent VASP ($Ser^{157}$) phosphorylation. These results strongly indicated that cordycepin might have therapeutic or preventive potential for platelet activation-mediated disorders including thrombosis, atherosclerosis, myocardial infarction, or cardiovascular disease.

• Korean Journal Plant Pathology
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• v.3 no.3
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• pp.187-197
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• 1987

Bacteria and fungi antagonistic to Fusarium oxysporum f. sp. cucumerinum Owen were effectively isolated with each of modified Triple Layer Agar (TLA) technique from rhizosphere soil where cucumber had been grown healthily in plastic film house. Three predominant bacterial isolates selected were identified as Pseudomonas fluorescens, and P. putida, Serratia sp. and three fungal isolates were Gliocladium sp. Trichoderma harzianum, and T. viride. Antagonistic bacteria inhibited $26-45\%$ of germination and $41-56\%$ of germ tube elongation of microconidia of F. oxysporum f. sp. cucumerinum on Water Agar (WA). P. fluorescens was the strongest inhibitor. Several my co parasitisms were observed on dual culture of WA between antagonistic fungi and F. oxysporum f. sp. cucumerinum such as coiling, penetration, overgrowing, and lysis. Mycelial lysis of the pathogen was the most severe at pH 4.6, followed by 3.6, 5.6 and 6.6 of the medium in decreasing order. At pH 6.6, mycelia of the pathogen were not conspicuously damaged, however, the antagonistic fungi formed abundant chlamydospores especially Gliocladium sp. T. harzianum revealed the most excellent antagonism in vitro.

• Korean Journal of Clinical Pharmacy
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• v.10 no.3
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• pp.111-119
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• 2000

The objective of this study was to evaluate the efficacy and the pattern of regimens prescribed for the treatment of peptic ulcer disease in a regional community hospital. 226 patients were treated as an outpatient and followed for one year. 88 patients $(38.9\%)$ had gastric ulcer (GU) alone, 6 patients $(2.7\%)$ had duodenal ulcer (DV) alone, 5 patients $(2.2\%)$ had gastroesophageal reflux disease (GERD) alone, 25 patients $(11.1\%)$ had both GU and DU, 88 patients $(38.9\%)$ had both GU and GERD, and 14 patients $(6.2\%)$ had both DU and GERD. During this study period no one was treated for Zollinger-Ellison Syndrome. The disease showed higher occurrence in male population (139 patients, $61.5\%$) and among the ages of 30 and 40 $(62.4\%)$. The average age of these patients was 41.3 years and there was no difference between the genders. $81.4\%$ of these patients underwent CLO test to check for the existence of Helicobacter and $66.3\%$ of these Patients showed the positive response. $65.6\%$ of patients with GU and $80\%$ of patients with DU showed the positive response and there was no difference between the genders $(65.4\%\;vs.\;67.6\%)$. 184 patients $(81.4\%)$ were deemed to be cured based on the disappearance of their symptoms after completing the regimens. Compliance rate did not differ for gender or different diseases, while showing a difference in age. Patients between the ages of 20 to 30 years old showed the worst compliance rate. In addition, the compliance was lower among the patients who had previous occurrence of the disease, and this was more evident among female patients. Although 184 patients out of the total 226 patients were deemed to be cured, 36 patients $(20.65\%)$ of these returned to the hospital for relapsed diseases within one year. The factors that affected for patients to relapse were the diseases accompanied by ulcer and social environments, such as smoking, alcohol consumption, and previous history of the diseases (smoking P<0.001, alcohol consumption P<0.02, previous history of disease P<0.05). The regimen using $H_2$ receptor antagonists+tripotassium dicitrato bismuthate+clarithromycin showed the lower rate of relapse, and the regimens of omeprazole (OMP)+amoxicillin+tripotassium dicitrato bismuthate and OMP+amoxicillin+metronidazole showed better compliance rate. Patient education by pharmacists on the importance of compliance to regimens and the risk factors fer relapse can provide a better patient care. This would ultimately result in more cost-effective treatments by preventing additional cost for treating relapsed symptoms in approximately $20\%$ of patients.

• Biomedical Science Letters
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• v.13 no.3
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• pp.197-206
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• 2007

P2X receptors are membrane-bound ion channels that conduct $Na^+,\;K^+$, and $Ca^{2+}$ in response to ATP and its analogs. There are seven subunits identified so far ($P2X_1-P2X_7$). $P2X_2$ receptors are known to be expressed in a wide range of organs including brains and adrenal grands. PC12 cells are originated from adrenal grand and differentiated by nerve growth factor or pituitary adenylate cyclase activating poly peptide (PACAP). Previous studies indicate that $P2X_2$ receptor activation in PC12 cells couples to $Ca^{2+}-dependent$ release of catecholamine and ATP. It is known that acidic pH potentiates ATP currents at $P2X_2$ receptors. This leads to a hypothesis that $P2X_2$ receptors may play an important role in PC12 cell differentiation, one of the characteristics of which is neurite outgrowth, induced by the hormones under lower pH. In the present study, we isolated several clones which potentiate neurite outgrowth by PACAP in acidic pH (6.8), but not in alkaline pH (7.6). RT-PCR and electrophysiology data indicate that these clones express only functional $P2X_2$ receptors in the absence or presence of PACAP for 3 days. Potentiation of neurite outgrowth resulted from PACAP (100 nM) in acidic pH is inhibited by the two P2X receptor antagonists, suramin and PPADS ($100\;{\mu}M)$ each), and exogenous exprerssion of ATP-binding mutant $P2X_2$ receptor subunit ($P2X_2[K69A]$). However, acid sensing ion channels (ASICs) are not involved in PACAP-induced neurite outgrowth potentiation in lower pH since treatments of an inhibitor of ASICs, amyloride ($10\;{\mu}M$), did not give any effects to neurite extension. The vesicular proton pump ($H^+-ATPase$) inhibitor, bafilomycin (100 nM), reduced neurite extension indicating that ATP release resulted from $P2X_2$ receptor activation in PC12 cells is needed for neurite outgrowth. These were confirmed by activation of mitogen activated protein kinases, such as ERKs and p38. These results suggest roles of ATP and $P2X_2$ receptors in hormone-induced cell differentiation or neuronal synaptogenesis in local acidic environments.

• The Korean Journal of Physiology
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• v.18 no.2
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• pp.139-150
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• 1984

Vanadate is a potent inhibitor of Na-K-ATPase. Ouabain, the another specific inhibitor of Na-K-ATPase, induces the contraction in cardiac muscle and smooth muscle. But, some investigators observed the discrepancies between vanadate and ouabain-induced contraction in cardiac muscle. The difference of vanadate and ouabain-induced contraction was investigated in the cat ileal smooth muscle. The following results were obtained. 1) Ouabain-induced contraction was biphasic, but vanadate-induced contraction had one peak. 2) Atropine inhibited ouabain·induced contraction, but did not inhibit vanadate-induced contraction. 3) Changes in external $Ca^{++}$concentration or $Ca^{++}$ antagonists had a greater influence on the contraction induced hy vanadate than by ouabain. 4) Removal of $Na^+$ from incubation medium and high $K^+$ abolished ouabain-induced contraction, but had no effect on vanadate-induced contraction. 5) Vanadate-induced contraction was potentiated in the presence of ouabain. 6) After 3 hrs incubation with vanadate, there was no change in intracellular $Na^+$ concentrations in contrast with ouabain. These results suggest that vanadate contracts ileal smooth muscle through the mechanism different from ouabain, and this is independent of the inhibition of Na-K-ATPase activity.