• Title/Summary/Keyword: Carbamates

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Protective Effect of Physostigmine and Neostigmine against Acute Toxicity of Parathion in Rats

  • Jun, Jung-Won;Kim, Young-Chul
    • Archives of Pharmacal Research
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    • v.14 no.4
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    • pp.330-335
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    • 1991
  • The effects of physostigmine and neostigmine on the parathin induced toxicity were examined in adult female rats. Physostigmine $(100\;{\mu}g/kg,\;ip)$ or neostigmine $(200\;{\mu}g/kg,\;ip)$ inhibited acetylcholinesterase (AChE) and cholinesterase (ChE) activities in blood, brain and lung when the enzyme activity was measured 30 min after the treatment. At the doses of two carbamates equipotent on brain AChE, neostigmine showed greater inhibition on peripheral AChE/ChE. The enzyme activity returned to normal in 120 min following the carbamates except in the lung of rats treated with neostigmine. Carbamates administered 30 min prior to parathion (2 mg/kg) antagonized the inhibition of AChE/ChE by parathion when the enzyme activity was measured 2 hr following parathion. Neostigmine showed greater protective effect on peripheral AChE/ChE. The effect of either carbamate on AChE/ChE was not significant 2 hr beyond the parathion treatment. Carbamates decreased the mortality of rats challenged with a lethal dose of parathion (4 mg/kg, ip) either when treated alone or in combination with atropine (10 mg/kg, ip). Lethal action of paraoxon (1.5 mg/ks ip), the active metabolite of parathion was also decreased by the carbamate treatment indicating that the protection was not mediated by competitive inhibition of metabolic conversion of parathion to paraoxon. The results suggest that carbamylation of the active sites may not be the sole underlying mechanism of protection provided by the carbamates.

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Inhibition of Acetylcholinesterase Activity on the Organophosphorus and Carbamate Pesticides (유기인계 및 Carbamates 농약에 의한 Acetylcholinesterase 활성의 저해)

  • 김정호;김영호
    • Journal of Environmental Science International
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    • v.7 no.1
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    • pp.52-56
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    • 1998
  • The effects of organophosphorus and carbamate pesticides were examined inhibition of the acetylcholinesterase activity in the chicken brain with enzyme-inhibition methods. The acetylcholinesterase activity in chicken brain determined by the Ellman method was 167 mmol/min/g protein. The optimum pH of acetycholinesterase was 8.2. $pl_{50}$ of acetycholinesterase by some organophosphorus were 3.80M of phosphorodlthioate, 4.04M of phosphorothioate, 6.33M of phosphate, and 6.60M of phosphrothiolate. pluto of acetycholinesterase by some carbamates were 5.1 OM of XMC, 5. 90M of carbofuran, 6.16M of isoprocarb, 6.30M of carbaryl, 6.47M of BPMC, and 6.77M of propoxur. pluto of carbamates selected was similar to that of phosphorothioate and phosphate organophosphates.

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Retention of Configuration; Mechanism Studies on the Reaction of Chlorosulfonyl Isocyanate with Ethers

  • Kim, Ji-Duck;Jung, Young-Hoon
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.242.2-243
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    • 2003
  • We have developed the novel one-pot synthetic method for regioselective N-protected amines, carbamates as a protective group of amines, through the reaction of various ethers with chlorosulfonyl isocyanate (CSJ). This synthetic method provides a simple and convenient alternative for the formation of carbamates, such as -NHMoc, -NHPoc. -NHCbz, -NHPnz, -NHTroc and -NHAloc, by varying the alkyl moiety of ethers. (omitted)

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One-pot Synthesis of Cinnamylamines with Various Protecting Groups from Cinnamyl Ethers

  • Jung, Young-Hoon;Kim, Ji-Duck
    • Archives of Pharmacal Research
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    • v.24 no.5
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    • pp.371-376
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    • 2001
  • The reaction of various alkyl cinnamyl ethers with CSI afforded the corresponding cinnamylamines with various protecting groups, such as -NHMoc, -NHiPoc, -NHCbz, -NHPnz, -NHTroc and -NHAloc. In the case of cinnamyl t-butyl ether and cinnamyl p-methoxybenzyl ether, the corresponding cinnamyl carbamates were formed via a different reaction pathway from the above.

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Studies on Determination of Aliphatic Carbamates -Quantitative Analysis of Carisoprodol-

  • Kim, Jeoung-Sook;Kim, Bak-Kwang
    • Journal of Pharmaceutical Investigation
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    • v.15 no.3
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    • pp.151-159
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    • 1985
  • For the determination of aliphatic carbamates, the quantitative analysis of carisoprodol was investigated by gab chromatography (GC) and spectrophotometry. All the methods studied were found to be very quantitative. The minimum experimental amounts of GC method, spectrophotometric method I and II were approximately $10^{-9},\;10^{-5}$ and $10^{-8}$ mole, respectively. The obtained results showed that GC method I was much more sensitive and rapid than spectrophotometric method II.

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Efficient and Facile Synthesis of α-Chloroenones Bearing β-Carbonates or β-Carbamates

  • Magar, Krishna Bahadur Somai;Lee, Yong Rok
    • Bulletin of the Korean Chemical Society
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    • v.33 no.12
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    • pp.4150-4154
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    • 2012
  • Efficient synthesis of ${\alpha}$-chloroenones bearing ${\beta}$-carbonates or ${\beta}$-carbamates was achieved by rhodium(II)-catalyzed reaction of cyclic diazodicarbonyl compounds with a variety of chloroformates or carbamyl chlorides in good yields. These reactions provided a useful and rapid route to ${\beta}$-substituted ${\alpha}$-haloenones.

Determination of Bioconcentration Factor on Carbamates (Carbamate계 농약의 생체농축계수 측정)

  • 민경진
    • Journal of Environmental Health Sciences
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    • v.20 no.4
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    • pp.80-89
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    • 1994
  • It was reported that BCF's (Bioconcentration Factor) on Carbaryl and BPMC in concentration of 1, 2, 5 and 10 ppm, previously. Carassius auratus(goldfish) was chosen as test organism. Carbamates in fish and in test water were extracted with n-hexane and acetonitrile. GC-ECD was used to detecting and quantitating of Carbamates. Also, partition coefficients were determined with Stir flask method. To evaluate environmental toxicological profiles of tested compounds, experimental concentration were 0.05, 0.1 and 0.5 ppm in contrast to previous report. It was considered that higher BCFs of BPMC due to its higher partition coefficient compared to Carbaryl. The obtained results were as follows: 1. It was possible to determine short term BCF of Carbaryl and BPMC through relatively simple procedure in environmental concentrations. 2. BCF$_3$ of Carbaryl in concentration of 0.05, 0.1 and 0.5 ppm were 4.666 $\pm$ 0.002, 3.622 $\pm$ 0.004, 1.200 $\pm$ 0.002 and BCF$_5$ were 3.897 $\pm$ 0.005, 4.219 $\pm$ 0.017 and 1.186 $\pm$ 0.054, respectively. In the case of BPMC in same condition, BCF$_3$ were 4.077 $\pm$ 0.014, 4.900 $\pm$ 0.005, 4.750 $\pm$ 0.009 and BCF$_5$ were 3.465 $\pm$ 0.010, 4.612 $\pm$ 0.011 and 4.075 $\pm$ 0.012, respectively. 3. Carbaryl concentration in fish extract was increased as increasing test concentration, but BCF were decreased as prolonging test period, especially dropped at 0.5 ppm. 4. In the case of BPMC, BCF were decreased as increasing test concentration, but the concentration in fish extract of 3-day test group was slightly higher than that of 5-day test group. 5. Higher BPMC concentration in fish extract was due to its higher partition coefficient to compared with Carbaryl. 6. Determined logP of Carbaryl and BPMC were 2.200 and 3.180. But the calculated BCF using suggested equation was so different that predict BCF. It is suggested that BCF's of Carbamates have to be determined by experiment.

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Difference in Species of Test Fish on the Determination of Short-term Bioconcentration Factor (단기간 생물농축계수의 측정에 있어서 실험어류의 종에 따른 차이)

  • 민경진;차춘근;전봉식;김근배
    • Journal of Environmental Health Sciences
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    • v.24 no.1
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    • pp.24-31
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    • 1998
  • This study was performed to investigate the difference in species of test fish on the determination of short-term bioconcentration factor in zebrafish(Brachydanio rerio), red sword tail(Xiphophorus hellieri) and goldfish(Carassius auratus). Experimental concentrations of carbamates were 0.05 and 0.10 ppm and chlorothalonil were 0.005 and 0.01 ppm for 3 and 5 days, respectively. This paper reports the measured BCF value on pesticides in various species of test fish, under steady state, and examined correlation between the BCF value and depuration rate constant or LC$_{50}$ or lipid content. Carbamates and chlorothalonil concentration in fish extract and BCF of carbamate and chlorothalonil were increased as incresing test concentration. Carbamates concentration in fish extract and BCF of carbamate were decreased as incresing test period, but chlorothalonil concentration in fish extract and BCF of chlorothalonil were increased as prolonging test period. Determined pesticide concentration in fish extract and BCF were highest in red sword tail, and followed by goldfish, and zebrafish. Determined depuration rate constant were highest in zebrafish, and followed by goldfish, and red sword tail. 96hr-LC$_{50}$ were highest in red sword tail, and followed by zebrafish, and goldfish. Lipid compositions were highest in red sword tail, and followed by goldfish, and zebrafish. Therefore, it is suggested that the difference of BCF between each pesticide due to those of lipid composition of fish and deputation rate constant, while LC$_{50}$ have no effect on BCF.

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