• Title/Summary/Keyword: KR1

Search Result 802, Processing Time 0.025 seconds

Theoreitica1 analysis of plasma processes in discharge excited KrF laser (방전어기 KrF 레이저의 프라즈마 프로세서 해석)

  • Choi, Boo-Yeon;Lee, Choo-His
    • Proceedings of the KIEE Conference
    • /
    • 1989.11a
    • /
    • pp.505-508
    • /
    • 1989
  • A computer simulation code of UV preionized discharge KrF laser is developed, including time dependent circuit equations, boltzmann equations, and plasma kinetic equations for various atomic and molecular species. Rate constants for electron collision processes are calculated with a boltzmann equations as a function of E/N. In this study, we studied mainly the $KrF^*$ formation process, relaxation process, and the 248nm absorption process as a function of charging voltage.

  • PDF

A Study on preionization effect of discharge excited KrF excimer laser (방전여기 KrF 엑사이머 레이저의 에비전리 영향에 관한연구)

  • Kim, Sang-Ook;Choi, Boo-Yeon;Lee, Choo-Hie
    • Proceedings of the KIEE Conference
    • /
    • 1990.07a
    • /
    • pp.459-461
    • /
    • 1990
  • Me performed an experiment about preionization electron number density of charge transfer type KrF excimer laser. At the total pressure of 1.8 and 2.2 atm with helium (He) buffer gas, the experimental range of the electron number density is 8-9 ${\times}$ 10 cm The distance between electrode and preionization pin is 15 mJ at charging voltage of 27kV,gas pressure of 2.2 atm,gas mixture of F /Kr/He = 0.3/396.7(%).

  • PDF

Antiplatelet Activity of [5-(2-Methoxy-5-chlorophenyl)furan-2-ylcarbonyl]guanidine (KR-32570), a Novel Sodium/hydrogen Exchanger-1 and Its Mechanism of Action

  • Lee Kyung-Sup;Park Jung-Woo;Jin Yong-Ri;Jung In-Sang;Cho Mi-Ra;Yi Kyu-Yang;Yoo Sung-Eun;Chung Hun-Jong;Yun Yeo-Pyo;Park Tae-Kyu;Shin Hwa-Sup
    • Archives of Pharmacal Research
    • /
    • v.29 no.5
    • /
    • pp.375-383
    • /
    • 2006
  • The anti platelet effects of a novel guanidine derivative, KR-32570 ([5-(2-methoxy-5-chlorophenyl) furan-2-ylcarbonyl]guanidine), were investigated with an emphasis on the mechanisms underlying its inhibition of collagen-induced platelet aggregation. KR-32570 significantly inhibited the aggregation of washed rabbit platelets induced by collagen $(10{\mu}g/mL)$, thrombin (0.05 U/mL), arachidonic acid $(100{\mu}M)$, a thromboxane (TX) $A_2$ mimetic agent U46619 (9,11-dideoxy-9,11-methanoepoxy-prostaglandin $F_2,\;1{\mu}M$) and a $Ca^{2+}$ ATPase inhibitor thapsigargin $(0.5{\mu}M)$ ($IC_{50}$ values: $13.8{\pm}1.8,\;26.3{\pm}1.2,\;8.5{\pm}0.9,\;4.3{\pm}1.7\;and\;49.8{\pm}1.4{\mu}M$, respectively). KR-32570 inhibited the collagen-induced liberation of $[^3H]$arachidonic acid from the platelets in a concentration dependent manner with complete inhibition being observed at $50{\mu}M$. The $TXA_2$ synthase assay showed that KR-32570 also inhibited the conversion of the substrate $PGH_2$ to $TXB_2$ at all concentrations. Furthermore, KR-32570 significantly inhibited the $[Ca^{2+}]_i$ mobilization induced by collagen at $50{\mu}M$, which is the concentration that completely inhibits platelet aggregation. KR-32570 also decreased the level of collagen $(10{\mu}g/mL)$induced secretion of serotonin from the dense-granule contents of platelets, and inhibited the NHE-1-mediated rabbit platelet swelling induced by intracellular acidification. These results suggest that the antiplatelet activity of KR-32570 against collagen-induced platelet aggregation is mediated mainly by inhibiting the release of arachidonic acid, $TXA_2$ synthase, the mobilization of cytosolic $Ca^{2+}$ and NHE-1.

Pharmacological Effects of KR60886, A New β3 Adrenoceptor Agonist

  • Lee, Sang-Suk;Yang, Sung-Don;Ha, Jae-Du;Choi, Joong-Kwon;Cheon, Hyae-Gyeong
    • Biomolecules & Therapeutics
    • /
    • v.12 no.4
    • /
    • pp.215-220
    • /
    • 2004
  • In an attempt to develop new anti-diabetic agents, a series of aryloxypropanolamine derivatives was synthesized to serve as ${\beta}_3$ adrenoceptor agonists. Among these derivatives, 1-{1-methyl-3-[4-(2-methyl-2H-1,2,3,4-tetrazol-5-yl)phenyl]propylamino}-3-phenoxy-2-propanol (KR60886) possessed a high affinity for the ${\beta}_3$ adrenoceptor (Ki = 28 nM) and moderate affinities for ${\beta}_1$ and ${\beta}_2$ adrenoceptors (Ki = 95 nM and 100 nM, respectively). In addition, KR60886 stimulated cAMP production with an EC$_{50}$ of 0.4 ${\mu}M$, confirming its agonistic activity for the ${\beta}_3$ adrenoceptor. In vivo activities of KR60886 were examined by using a fat-fed/streptozotocin (STZ)-treated rat model and the ob/ob mouse model. Oral administration of KR60886 (10 mg/kg) for 3 days (b.i.d.) to fat-fed/STZ-treated rats significantly lowered plasma glucose levels and reduced plasma free fatty acid concentrations. Similarly, KR60886 treatment (10 mg/kg/day for 7 d) resulted in a reduction of plasma glucose concentrations in ob/ob mice. The present study suggests that KR60886 is a potent ${\beta}_3$ receptor agonist with in vivo anti-diabetic properties.

Motor Learning in Elderly: Effects of Decision Making Time for Self-Regulated Knowledge of Results During a Dynamic Balance Task

  • Jeon, Min-jae;Jeon, Hye-seon
    • Physical Therapy Korea
    • /
    • v.23 no.4
    • /
    • pp.16-26
    • /
    • 2016
  • Background: Deficiencies in the ability to maintain balance are common in elderly. Augmented feedback such as knowledge of results (KR) can accelerate learning and mastering a motor skill in older people. Objects: We designed this study to examine whether one session of Wii-Fit game with self-regulated KR is effective for elderly people, and to compare the effect of two different timings of self-regulated KR conditions. Methods: Thirty-nine community-dwelling elders, not living in hospice care or a nursing home, participated in this study. During acquisition, two groups of volunteers were trained in 10 blocks of a dynamic balancing task under the following 2 conditions, respectively: (a) a pre-trial self-regulated KR ($n_1=18$), or (b) a post-trial self-regulated KR ($n_2=21$). Immediate retention tests and delayed retention tests of balancing performance were administered in 15 minutes and 24 hours following acquisition period, respectively. Results: In both groups, significant improvements of balancing performances scores were observed during the acquisition period. Regardless of the group, mean of balancing performance scores on retention tests were well-maintained from the final session. There were no significant differences between groups in balancing performance scores during the acquisition period (p>.05); however, the post-trial self-regulated KR group exhibited significantly higher balancing performance scores in both the immediate retention test and delayed retention test than that of the pre-trial self-regulated KR group (p<.05). Conclusion: Therefore, subjects who regulated their feedback after a dynamic balancing task, during the acquisition period, experienced more efficient motor learning during the retention period than did subjects who regulated their feedback before a dynamic balancing task. Accordingly, in case of presenting the KR of motor learning in clinical settings to elders who reduced dynamic balance abilities, the requesting time of KR is imperative according to self-estimation processes as well as types of KR and practice.

Synovial Cell Migration is Associated with B Cell Activating Factor Expression Increased by TNFα or Decreased by KR33426

  • Lee, Jiyoung;Yoon, Sung Sik;Thuy, Pham Xuan;Moon, Eun-Yi
    • Biomolecules & Therapeutics
    • /
    • v.28 no.5
    • /
    • pp.405-413
    • /
    • 2020
  • Fibroblast-like synoviocytes (FLS) play a crucial role in initiating rheumatoid arthritis. B-cell activating factor (BAFF) plays a role in FLS survival as well as in B cell maturation and maintenance. Here, we investigated whether tumor necrosis factor (TNF)-α-induced BAFF expression controls FLS migration and whether BAFF expression in FLS could be regulated by KR33426 which is the inhibitor of BAFF binding to BAFF receptors (BAFF-R) by using MH7A synovial cells transfected with the SV40 T antigen. More TNF-α-treated cells migrated compared to the control. TNF-α increased BAFF expression in FLS, significantly. FLS migration was inhibited by the transfection with BAFF-siRNA. KR33426 also inhibited BAFF expression increased by TNF-α treatment in FLS as judged by western blotting, PCR, and transcriptional activity assay. Kinases including JNK, p38 and Erk were activated by TNF-α treatment. While JNK and p38 were inhibited by KR33426 treatment, no changes in Erk were observed. Transcription factors including p65, c-Fos, CREB and SP1 were enhanced by TNF-α treatment. Among them, c-Fos was inhibited by KR33426 treatment. Small interference(si)-RNA of c-fos decreased BAFF transcriptional activity. FLS migration induced by TNF-α was inhibited by the transfection with BAFF-siRNA. KR33426 increased Twist, Snail, Cadherin-11 and N-Cadherin. In contrast, KR33426 decreased E-cadherin and TNF-α-enhanced CCL2. Taken together, our results demonstrate that synovial cell migration via CCL2 expression could be regulated by BAFF expression which is decreased by KR33426 and c-Fos-siRNA. It suggests for the first time that the role of BAFF-siRNA on FLS migration might be matched in the effect of KR33426 on BAFF expression.

Metabolism of a New Neuroprotective Agent for Ischemia-Reperfusion Damage, KR-31543 in the Rats using Liquid Chromatography/Electrospray Mass Spectrometry

  • Kim, John;Ji, Hye-Young;Lee, Seung-Seok;Yoo, Sung-Eun;Kim, Sun-Ok;Lee, Dong-Ha;Lim, Hong;Lee, Hye-Suk
    • Archives of Pharmacal Research
    • /
    • v.25 no.5
    • /
    • pp.664-668
    • /
    • 2002
  • KR-31543,(2S,3R,4S)-6-amino-4-[N-(4-chlorophenyl)-N-(2-methyl-2H-tetrazol-5-ylmethyl)amino]-3,4-dihydro-2-dimethoxymethyl-3-hydroxy-2-methyl-2H-1-benzopyran is a new neuroprotetive agent for ischemia-reperfusion damage. The in vitro and in vivo metabolism of KR-31543 in rats has been studied by LC-electrospray mass spectrometry. Rat liver microsomal incubation of KR-31543 in the presence of NADPH resulted in the formation of a metabolite M1. M1 was identified as N-(4-chlorophenyl)-N-(2-methyl-2H-tetrazol-5-ylmethyl)amine on the basis of LC-MS/MS analysis with the synthesized authentic standard. Rat CYP3A1 and 3A2 are the major CYP isozymes involved in the formation of M1.

PHOSPHODIESTERASE 억제제 (PDE-1), SODIUM NITROPRUSSIDE, AMITRIPTYLINE, 및 CHLORPROMAZINE의 항-혈소판작용

  • 전보권;안상건;최상현;신경호;이민수;천연숙
    • Proceedings of the Korean Society of Applied Pharmacology
    • /
    • 1994.04a
    • /
    • pp.286-286
    • /
    • 1994
  • Thrombin (0.25 U/ml : TB), 소-피부 collagen (200 $\mu\textrm{g}$/ml : CG), adenosine 5'-diphesphate (4,0 $\times$ $10^{-5}$M : ADP), 및 epinephrine (4,0 $\times$ 10 $^{-5}$M : EPI)의 가토-혈소판 응집과 단백인산화작용에 미치는 PDE-I (3-isobutyl-1-methylxanthine : IBMX, 및 KR 30075), amitriptyline (AP), chlorpromazine (CP), 및 sodium nitrogrosside (SNP)의 염향을 비교-검토하였다. 그 결과, KR은 2,2 $\times$ $10^{-7}$M 이하의 $IC_{50}$/에서 EPI > ADP > CG > TB 순으로 각각을 억제하였으며, SNP 보다도 강하였고; KR-30075보다 약하나 IBMX, AP, 및 CP도 각 응집재의 작용을 억제하였으며 특히 EPI에 대하여 $10^{-8}$M 이하의 $IC_{50}$/에서 유의한 억제력을 보였다. 각 응집제들은 41 kD 인산화는 유의하게 증가시키며 47 kD와 20 kD 단백인산화는 감소시켰는데; 모든 항응집성 약물이 41 kD 인산화-증가는 유의하게 억제하였다, 아울러, AP와 CP는 47 kD 단백인산화-감소에 영향을 미치지 않았으나 20 kD 단백인산화-감소는 억제하였다. PDE-I (IBMX와 KR)와 SNP는 47 kD와 20 kD 단백인산화-감소를 다소 약화시켰으며, 43 kD와 22 kD 단백인산화를 KR > IBMX > SNP순으로 유의하게 증가시켰고, KR의 22 kD 단백인산화작용은 현저하였다.

  • PDF

Capsaicinoids-induced Neurotoxic Desensitization in Guinea Pig: Antinociception and Loss of Substance P-like Immunoreactivity from Peripheral Sensory Nerve Endings in Bronchi

  • Jung, Yi-Sook;Lee, Buyean;Shin, Hwa-Sup;Kong, Jae-Yang;Park, No-Sang;Cho, Tai-Soon
    • Biomolecules & Therapeutics
    • /
    • v.3 no.4
    • /
    • pp.256-259
    • /
    • 1995
  • Antinociceptive and desensitizing effects of systemically administered capsaicinoids (capsaicin and KR25018) were investigated in guinea pig. Nociceptive sensitivity to chemical stimulus was examined to test sensory function, and the content of substance P-like immunorractivity (SP-LI) in bronchi was determined as a peripheral marker of capsaicin-sensitive primary afferent neurons. Guinea pigs were pretreated s.c. with several doses of capsaicin (1,2.5,5, 10 mg/kg) or KR25018 (1, 2.5, 5, 10 mg/kg) one week prior to the experiments. Frequency of eye wiping was significantly decreased by capsaicin and KR25018 in a pretreatment dosedependent manner. In capsaicin- or KR25018-pretreated guinea pigs, there was a significant loss of SP-LI in bronchial tissue extracts. In summary, a newly synthesized capsaicin analogue H725018 exhibited antinociceptive effect against chemical stimulus in guinea pig, with comparable potency to capsaicin. This desensitizing activity of capsaicin or KR25018 might be related to the loss of SP-LI in peripheral afferent nerves.

  • PDF