• Title/Summary/Keyword: C doping

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Determination of Novel Synthetic 5HT2C Agonist KOPC20010 by Gas-Chromatography/Mass Spectrometry and its Bioavailability in Sprague-Dawley Rats

  • Im, Hye-Yeon;Pae, Ae-Nim;Yang, Ha-Yun;Park, Woo-Kyu;Seo, Ji-Eun;Haque, Md. Mamunul;Kwon, Oh-Seung
    • Journal of Pharmaceutical Investigation
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    • v.41 no.1
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    • pp.31-36
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    • 2011
  • $5HT_{2C}$ receptor among fourteen 5-HT subtypes plays important roles in several disorders such as depression, anxiety, epilepsy, schizophrenia and sleep disorders. The purpose of the study is to investigate pharmacokinetic parameters and bioavailability of a newly synthesized selective agonist of $5-HT_{2C}$ receptor, KOPC-20010 (KP10) in rats after intravenous and oral administration for the development of therapeutic anti-obesity agents. KP10 was administered orally (40 mg/kg) or intravenously (20 mg/kg), blood was collected via a catheter, and analyzed by GC/MSD. The calibration curve of KP10 in plasma and urine showed high linearity ($r^2$ >0.999). The retention times of KP10 in plasma and urine were 8.7 and 9.7 min, respectively. After oral administration of 40 mg/kg, pharmacokinetic parameters were calculated as follows; $C_{max}$ value was $1242.9{\pm}1195.5$ ng/mL at $1.1{\pm}0.6$ hr ($T_{max}$). $AUC_{0->24hr}$ and $AUC_{0>{\infty}}$ were $8034.2{\pm}960.7$ and $10464.1{\pm}681.5\;ng{\cdot}hr/mL$, respectively. The terminal half-life was $21.9{\pm}7.6$ hr. $AUC_{0->24hr}$ and $AUC_{0>{\infty}}$ were $4292.4{\pm}523.0$ and $6111.2{\pm}756.2\;ng{\cdot}hr/mL$, respectively, after 20 mg/kg of intravenous administration. The terminal half-life after intravenous administration was $25.1{\pm}9.4$ hr. Bioavailability of KP10 was determined to 86%. The excretion amount into the urine within 48 hr was approximately 4.7 to 6.7% of the dose administered. These data may be beneficial to the anti-obesity drug development of KP10.

Effects of Sr Contents on Structural Change and Electrical Conductivity in Cu-doped LSM ($La_{1-x}Sr_xMn_{0.8}Cu_{0.2}O_{3{\pm}{\delta}}$)

  • Ryu, Ji-Seung;No, Tae-Min;Kim, Jin-Seong;Jeong, Cheol-Won;Lee, Hui-Su
    • Proceedings of the Materials Research Society of Korea Conference
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    • 2011.10a
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    • pp.33.1-33.1
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    • 2011
  • Strontium doped lanthanum manganite (LSM) with perovskite structure for SOFC cathode material shows high electrical conductivity and good chemical stability, whereas the electrical conductivity at intermediate temperature below $800^{\circ}C$ is not sufficient due to low oxygen ion conductivity. The approach to improve electrical conductivity is to make more oxygen vacancies by substituting alkaline earths (such as Ca, Sr and Ba) for La and/or a transition metal (such as Fe, Co and Cu) for Mn. Among various cathode materials, $LaSrMnCuO_3$ has recently been suggested as the potential cathode materials for solid oxide fuel cells (SOFCs). As for the Cu doping at the B-site, it has been reported that the valence change of Mn ions is occurred by substituting Cu ions and it leads to formation of oxygen vacancies. The electrical conductivity is also affected by doping element at the A-site and the co-doping effect between A-site and B-site should be described. In this study, the $La_{1-x}Sr_xMn_{0.8}Cu_{0.2}O_{3{\pm}{\delta}}$ ($0{\leq}x{\leq}0.4$) systems were synthesized by a combined EDTA-citrate complexing process. The crystal structure, morphology, thermal expansion and electrical conductivity with different Sr contents were studied and their co-doping effects were also investigated.

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Chromosomal Aberration Assay of Taxol and 10-deacetyI baccatin III in Chinese Hamster Lung Cells In Vilro

  • Ryu, Jae-Chun;Kim, Kyung-Ran;Ryu, Eun-Kyung;Kim, Hyun-Joo;Kwon, Oh-Seung;Song, Choong-Eui;Mar, Woong-Chon;Chang, Il-Moo
    • Environmental Mutagens and Carcinogens
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    • v.16 no.1
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    • pp.6-12
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    • 1996
  • To investigate the clastogenicity of taxol and its precursor, 10-aleacetyl baccatin III, we performed chromosomal aberration assay with chinese hamster lung cells in vitro. The IC$_{50}$ values of taxol and 10-deacetyl baccatin III were determined as $1/16 \times 10^{-4}$ M (5.34 $\mu$g/ml) and $1 \times 10^{-2}$ M (560 $\mu$g/ml) in MTT assay, respectively. It means that the cytotoxicity of taxol revealed 100 times more cytotoxic than 10-deacetyl baccatin III in chinese hamster lung cell line. Nevertheless the strong positive genetic toxicity of taxol in the bone marrow micronucleus assay in vivo which was recently reported, we observed weak positive clastogenicity of taxoi only in the absence of metabolic activation system in the concentration ranges used in this experiment. Moreover, to clarify the involvement of metabolic fate of taxol because of its strong positive result in vivo, 10-deacetyl baccatin III which is a precursor in taxol synthesis, also subjected in chromosomal aberration assay in vitro. However, we observed no clastogenicity of 10-deacetyl baccatin III in this experiment. From above results, it was suggested that the esterification at C-13 appears to be relative for its genetic toxicity in chromosome aberration using chinese hamster lung cell in vitro.

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Thermal and Mechanical Properties of a N2 Doped Porous 3C-SiC Thin Film (질소가 도핑된 다공질 3C-SiC 박막의 열적, 기계적 특성)

  • Kim, Kang-San;Chung, Gwiy-Sang
    • Journal of the Korean Institute of Electrical and Electronic Material Engineers
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    • v.23 no.8
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    • pp.651-654
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    • 2010
  • This paper describes the thermal and mechanical properties of doped thin film 3C-SiC and porous 3C-SiC. In this work, the in-situ doped thin film 3C-SiC was deposited by using atmospheric pressure chemical vapor deposition (APCVD) method at $120^{\circ}C$ using single-precursor hexamethyildisilane: $Si_2(CH_3)_6$ (HMDS) as Si and C precursors. 0~40 sccm $N_2$ gas was used as doping source. After growing of doped thin film 3C-SiC, porous structure was achieved by anodization process with 380 nm UV-LED. Anodization time and current density were fixed at 60 sec and 7.1 mA/$cm^2$, respectively. The thermal and mechanical properties of the $N_2$ doped porous 3C-SiC was measured by temperature coefficient of resistance (TCR) and nano-indentation, respectively. In the case of 0 sccm, the variations of TCR of thin film and porous 3C-SiC are similar, but TCR conversely changed with increase of $N_2$ flow rate. Maximum young's modulus and hardness of porous 3C-SiC films were measured to be 276 GPa and 32 Gpa at 0 sccm $N_2$, respectively.

Preparation of Ce0.8Gd0.2O1.9 Powder Using CeO2 Powder and Gd Precipitation and Effect of CoO doping on Sintering

  • Sim, Soo-Man
    • Journal of the Korean Ceramic Society
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    • v.52 no.6
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    • pp.521-526
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    • 2015
  • $Ce_{0.8}Gd_{0.2}O_{1.9}$(GDC20) powder was prepared from a mixture of submicron-sized $CeO_2$ powder and Gd precipitates using ammonium carbonate $((NH_4)_2CO_3)$ as a precipitant. The mixture was calcined at $700^{\circ}C$ for 4 h followed by ball-milling that resulted in the GDC powder with an average particle size of $0.46{\mu}m$. The powder had a very uniform particle size distribution with particle sizes ranging from $0.3{\mu}m$ to $1{\mu}m$. Sintering of undoped GDC samples did not show a relative density of 99.2% until the temperature was increased to $1500^{\circ}C$, whereas GDC samples doped with 5 mol% CoO exhibited a significant densification at lower temperature reaching a relative density of 97.6% at $1100^{\circ}C$ and of 98.8% at $1200^{\circ}C$.