• The Korean Journal of Pharmacology
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• v.30 no.1
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• pp.1-9
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• 1994

It has been shown that there are several subtypes of ${\kappa}$ opioid receptor. We examined ligand binding profiles and the effects of various opioid agonists on high potassium-stimulated release of $[^3H]$ histamine. We have evaluated the properties of $non-{\mu},\;non-{\delta},$ binding of $[^3H]\;DIP\;([^3H]\;diprenorphine),$ anonselective opioid antagonist, in rat cortex membranes. Binding $to\;{\mu}\;and\;{\delta}$ sites was inhibited by the use of an excess of competing selective agonists (DAMGO, DPDPE) for these sites. (-) Ethylketocyclazocine (EKC), DIP and bremazocine inhibited $[^3H]$ DIP binding. However, arylacetamides (U69593 and U50488H) gave little inhibition Replacement of sodium by NMDG and the addition of guanine nucleotide influenced the inhibitory potency of (-) EKC, an agonist for {\kappa}_1-and-{\kappa}_2-binding site, but not of bremazocine. This result suggests that bremazocine can be an antagonist at this binding site. Also, we have examined the opioid modulation of $K^+(30mM)-induced\;[^3H]\;histamine$ release in rat frontal cortex slices labeled with $1-[^3H]\;histidine$. The $[^3H]\; histamine$ release from cortex slices was inhibited by EKC in a concentration-dependent manner. However, the ${\delta}$ receptor selective agonists, DPDPE and deltorphine II, ${\mu}$ receptor agonists, DAMGO and TAPS, ${\kappa}_1-agonists$, U69593 and U50488H, and ${\varepsilon}-agonist,\;{\beta}-endorphin,$ did not. The concentration-response curve of EKC was shifted to right in the presence of naloxone, nor-binaltorphimine and bremazocine, respectively. These results suggest that ${\kappa}_2$ opioid receptor regulates histamine release in the fromtal cortex of the rat.

• Neonatal Medicine
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• v.17 no.2
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• pp.181-192
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• 2010

Purpose: Current studies have demonstrated the neuroprotective effects of dizocilpine (MK-801) in many animal models of brain injury, including hypoxic-ischemic (HI) encephlopathy, trauma and excitotoxicity, but limited data are available for those during the neonatal periods. Here we investigated whether dizocilpine can protect the developing rat brain from HI injury via anti-apoptosis. Methods: In an in vitro model, embryonic cortical neuronal cell culture of Sprague-Dawley (SD) rats at 18-day gestation was done. The cultured cells were divided into three groups: normoxia (N), hypoxia (H), and hypoxia treated with dizocilpine (HD). The N group was prepared in 5% $CO_2$ incubators and the other groups were placed in 1% $O_2$ incubators (94% N2, 5% $CO_2$) for 16 hours. In an in vivo model, left carotid artery ligation was done in 7-day-old SD rat pups. The animals were divided into six groups; hypoxia (N), hypoxia (H), hypoxia with sham-operation (HS), hypoxia with operation (HO), HO treated with vehicle (HV), and HO treated with dizocilpine (HD). Hypoxia was made by exposure to a 2 hour period of hypoxic incubator (92% N2, 8% $O_2$). Results: In the in vitvo and in vivo models, the expressions of Bcl-2 in the hypoxia groups were reduced compared to the normoxia group. whereas those in the dizocilpine-treated group were increased compared to the hypoxia group. However. the expressions of Bax and caspase-3 and the ratio of Bax/Bcl-2 were revealed reversely. Conclusion: Dizocilpine has neuroprotective property over perinatal HI brain injury via anti-apoptosis.

• The Korean Journal of Pharmacology
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• v.31 no.1 s.57
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• pp.1-9
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• 1995

The slow development of histopathological changes and long period required for stabilization of lesions have suggested that secondary injury processes exacerbate the effect of initial mechanical insult after traumatic spinal cord injury (SCI). The importance of glutamate receptors in the normal functions of spinal cord, in concert with the large body of evidence that points to their involvement in neurotoxicity due to both ischemic and traumatic insults to the CNS, suggested a probable role of glutamate receptors in secondary injury process after traumatic SCI. In order to investigate the involvement of excitatory amino acid in the secondary injury process after SCI, this study examined the effect of dextrorphan, a noncompetitive NMDA receptor antagonist, on the recovery of hindlimb function and the residual tissue at injury site following SCI. Locomotor function was assessed using open field test (21 point scale). At 8 weeks spinal cord tissue was examined using quantitative histopathologic technique. Prior to surgery female Long-Evans rats were adapted to the test environment. Rats received laminectomies (T9/T10), and spinal cord contusions (NYU impactor) were produced by a 10 gm weight dropped 25 mm. DXT (15 or 30 mg/kg, i.p.) or saline was injected 15 min before contusion. Behavioral testing resumed 2 days post-injury and continued twice a week for 8 weeks. No differences between DXT and saline groups were found for hindlimb function and sparing tissue at the lesion site. These results suggest that NMDA receptor might not be involved in secondary injury processes after traumatic SCI.

• The Korean Journal of Pharmacology
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• v.18 no.2
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• pp.103-117
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• 1982

In an effort to provide evidence as to the regulatory role of the central dopaminergic system on the renal function, the effects of centrally administered dopamine and its specific antagonist haloperidol were investigated. Haloperidol (HA) given intracerebroventricularly (i.c.v.) induced antidiuresis in doses of 15 and $50{\mu}g/kg$. With $15{\mu}g/kg$ sodium reabsorption in the tubules was increased, while with $50{\mu}g/kg$ free-water reabsorption was increased. However, a marked diuresis with increased sodium and potassium was observed with $150{\mu}g/kg$. Hemodynamic changes were not evident, indicating that the diuresis is of tubular origin. Dopamine (DA), on the other hand, produced antidiuresis when given i.c.v. in a dose-related fashion. With smaller doses of 5 and $15{\mu}g/kg$ the antidiuresis was related to increased reabsorption of sodium in the tubules, but higher doses of 50 and $150{\mu}g/kg$ the decreases in renal blood flow and glomerular filtration rate were evident in addition to the tubular action. After pretreatment with $150{\mu}g/kg$ HA, the effects of $15{\mu}g/kg$ DA was abolished, but the antidiuretic actions of 50 and $150{\mu}g/kg$ were not blocked, and the natriuretic diuretic action of HA was overcome and became inconspicuous. These observations indicate that the central dopaminergic system influences the renal function by producing antidiuresis, and HA elicits diuresis and natriuresis by competitively antagonizing DA specifically on the central dopaminegic receptors. The antidiuresis observed with smaller doses of HA can be best explained by the facts that there are more than two types of DA-receptors in the brain and that the presynaptic autoreceptors on the dopaminergic neurones which affect the dopamine release at the synapse are more sensitive than the postsynaptic receptors. Overall, these data provide an evidence indicating that the central dopaminergic system plays a role in the regulation of renal function in the rabbit.

• Research in Plant Disease
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• v.16 no.1
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• pp.27-34
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• 2010

This study was performed to develop a formulation using an antagonistic bacterium Bacillus amyloliquefaciens A-2 to control tomato leaf mold caused by Fulvia fulva. B. amyloliquefaciens A-2 was grown in a medium with rice oil and mixed with various carrier and additives. One of the formulations, A2-MP, showed the best disease control value among the tested formulations. The disease control value of A2-MP at 100-fold and 500-fold diluted treatment was not significantly different from that of chemical fungicide triflumizole in a growth chamber. Although disease control effect was decreased by serial diluted treatment of the prepared A2-MP, 1,000-fold diluted treatment of A2-MP still showed high disease control value of 72.0%. For the green house experiments, the disease control values of A2-MP was indicated as 79.4% which is similar to that of chemical fungicide, triflumizole showing 79.6%. When the disease control activity of the formulation A2-MP was compared in tomato production conditions, disease control values of 100-fold diluted A2-MP and 3,000 fold diluted triflumizole exhibited 60%, 81.6%, respectively. The disease control efficiency by A-2MP was 73% of the disease control value of chemical fungicide. The formulation A-2MP maintained the stable bacterial viability and disease control activity when stored at $4^{\circ}C$. This result suggested that A-2MP develped from B. amyloliquefaciens A-2 could be used to control tomato leaf mold.

• Korean Journal of Weed Science
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• v.16 no.4
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• pp.317-326
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• 1996

To know whether pyrazosulfuron-ethyl(PYR) and imazaquin(IMA), known as a acetolactate synthase(ALS) inhibitors, have a same herbicidal action pattern in rice(Oryza sativa) or barnyardgrass (Echinochloa crus-galli), an inhibition pattern and a response characteristics in combination with dymron or butachlor were investigated. In contrast to the phytotoxicity of rice treated with IMA, the one treated with PYR was completely tended to be recovered after 25 days after treatment. Safening effect of dymron against PYR was effectively developed to transplanted-rice, while such an effect was not shown in combination with IMA. In combination with PYR and butachlor, antagonistic effect was observed in both simultaneous or sequential treatment on bamyardgrass, however, additive effect was rather shown in combination with IMA and its activity was dominantly dependent on the first applied compound. $I_{50}$ of PYR and IMA on the ALS extracted from barnyardgrass was $4{\times}10^{-7}$M and $2.8{\times}10^{-6})$M, respectively. Butachlor did not affect their activities on ALS in vitro. These results suggest that PYR and IMA might have a different action each other in the pathway to a final herbicidal activity even though their primary action site is ALS.

• Korean Journal of Weed Science
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• v.18 no.3
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• pp.197-204
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• 1998

This study was conducted to determine the activity of ALS, content of endogenous free amino acids and fatty acids affected by herbicide mixture of cyhalofop-butyl, pyribenzoxim and pyrazosulfuron-ethyl. $I_{50}$ values (concentration required for 50% inhibition of ALS activity) of pyribenzoxim herbicide on the activity of ALS in Echinochloa crus-galli and Cyperus serotinus in vitro were recorded at 4${\times}$100 nM and 5${\times}$10 nM, respectively, while $I_{50}$ values of pyrazosulfuron against E crus-galli and C. serotinus were 4.5${\times}$10 nM and 4${\times}$10 nM, respectively, and the mixture of two herbicides showed additive effect on ALS activity at the low application rate, and independent effect at the high application rates of two herbicides. The inhibition rates of the three herbicides mixture treatment on the three branch-chain amino acids such as valine, leucine and isoleucine were 74.6%, 66.6% and 57.9% in C. serotinus and 36.6% 51.1% and 48.1% in E. crus-galli, respectively. A little bit higher inhibitory effect on the three branch-chain amino acids in C. serotinus and E. crus-galli seedlings was observed in two herbicide mixture of pyribenzoxim with pyrazosulfuron than three herbicide mixture of cyhalofop with pyribenzoxim and pyrazosulfuron. The interaction among three herbicides showed non-antagonism on the amounts of endogenous free amino acids.

• Korean Journal of Weed Science
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• v.3 no.2
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• pp.190-198
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• 1983

To examine the possibility of enhancing activity of foliar applied herbicides by spray methods and additives, field experiments were conducted to evaluate the effects of surfactant, spray volume, and additions of ammonium sulfate or potassium chloride to glyphosate on toxicity to Digitaria sanguinalis or Artemisia princeps. Glyphosate toxicity increased as spray volume was decreased from 120 1/10a to 40 and 80 1/10a. Additions of surfactant in the spray solution increased toxicity of glyphosate to D. sanguinalis and usually more pronounced effect was obtained at glyphosate 30.5g a.i./10a. Additions of 1 and 5% (w/v) ammonium sulfate to glyphosate increased toxicity to A. princeps at glyphosate 30.5 and 61.5g a.i./10a. 10% ammonium slufate, however, had no effect or were antagonistic. Additions of potassium chloride at 1,2 and 3% (w/v) were also very effective to increase herbicidal activity to A. princeps at glyphosate at 30.5 and 61.0g a.i/10a. These results suggest that the practices for enhancement of herbicidal activity by improvement of spray method and additions of ammonium sulfate or potassium chloride to glyphosate can be employed to use lower herbicide levels while giving the same degree of weed control in orchards and non-crop lands.

• Archives of Reconstructive Microsurgery
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• v.21 no.1
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• pp.61-67
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• 2012

Purpose: The purpose of this study was to investigate the role of mast cells and their product, histamine and leukotriene in ischemia-reperfusion injury. Methods: Forty Sprague-Dawley rats were divided into four groups. (Group I: Control group without ischemia, Group II: Normal saline with ischemia, Group III: Cimetidine with ischemia, Group IV: Zafirlukast with ischemia) Skin flap was elevated and ischemic insult was given by clamping the artery for 12 hours. Before reperfusion, the rats were treated with saline, cimetidine and zafirlukast. Flap survival was evaluated at 7 days. Neutrophil counts, mast cell counts were evaluated 24 hours after reperfusion. Results: Flap survival rate in the control group was 92.33%, whereas normal saline group had 37.34% survivals. Cimetidine and zafirlukast treated group showed significantly higher survival rates than normal saline group. The neutrophil and mast cell counts in cimetidine and zafirlukast treated group were significantly decreased than normal saline group. Cimetidine treated group showed higher survival rate and lower cell counts than zafirlukast treated group. Conclusion: The administration of cimetidine and zafirlukast can decrease neutrophils and mast cells caused by ischemia-reperfusion and increase flap survivals. It is suggests that antihistamine and leukotriene receptor antagonist have protective effect against ischemia-reperfusion injury to skin flap in rat.

• Korean Journal of Microbiology
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• v.49 no.3
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• pp.286-291
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• 2013

Soybean pastes with 8% (w/w) salinity were prepared instead of soybean paste with 14% (w/w) salinity to meet the growing demands of Korean's low sodium diet. After aging, white films had appeared on the surface of all low-salted soybean pastes [8% (w/w) salinity] unlike high-salted soybean pastes [14% (w/w) salinity]. All of eight microbes isolated from the surface film were identified as Pichia kudriavzevii. Eleven Bacillus strains with good characteristics of fermentation were isolated from traditionally fermented soybean pastes in order to preserve their unique flavors and aromas after aging, and as a result of analyzing the biochemical characteristics and 16S rRNA sequences, those were identified as B. subtilis, B. licheniformis, and B. methylotrophicus. All of the Bacillus isolates had antagonistic activities against 8 isolates of the film-forming yeasts and harbored the genes for synthesis of antimicrobial surfactants including lichenysin and/or surfactin.