• Title/Summary/Keyword: 1,5-Benzodiazepine

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Anxiolytic-like Effects of the Methanol Extract of Sophorae Fructus (괴각(Sophorae Fructus) 메탄올 추출물의 항불안 효과)

  • Oh, Han Saem;Lee, Gil Yong;Jung, Ji Wook
    • Food Science and Preservation
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    • v.19 no.5
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    • pp.767-773
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    • 2012
  • The purpose of this study was to investigate the anxiolytic-like effect of the methanol extract of Sophorae fructus (MESF) using elevated plus-maze (EPM), open field test, and horizontal wire test in mice. MESF was orally administered at doses of 50, 100, 200, or 400 mg/kg to ICR mice 1 h before behavioral evaluation. The control group was given an equal volume of 10% Tween 80, and the positive control group was given diazepam (1 mg/kg, i.p.). The administration of MESF significantly increased the percentage of time spent in open arms and the entries into the open arms of the EPM compared with the 10% Tween 80-treated control group (p < 0.05). In addition, the anxiolytic-like activities of MESF were antagonized by flumazenil (a GABAA antagonist, 10 mg/kg) but not by WAY-100635 (a 5-HT1A antagonist, 0.3 mg/kg). Futhermore, there were no changes in the locomotor activity and myorelaxant effects of the experimental group, as opposed to the 10% Tween 80-treated control group. Therefore, these findings suggest that MESF promotes the anxiolytic-like activity mediated by the GABAergic nervous system in mice.

Clinical Characteristics of Acute Drug Intoxication in Emergency Department

  • Kim In Byung;Chun Sung Pil;Kim Seung Whan
    • Biomedical Science Letters
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    • v.10 no.3
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    • pp.299-303
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    • 2004
  • The number of acute drug intoxication who visiting to emergency department which is located near urban and rural area concomitantly is inclined to increase slightly, The purpose of this study was the investigation of methods and strategies of management of acute drug intoxication in emergency department Clinical trials were done on 92 cases of acute drug intoxication visiting to Emergency Department of Chungnam National University Hospital during 4 months from April to July 2003. 1. The total number of acute drug intoxication during this period was 92 patients, which presented 0.95% of all the emergency department visiting patients during the study. The intentional ingestions were observed in 84 cases (91.3%). 2. The maximal point of age distribution was 4th decade. The number of that was 21 cases (22.8%). 3. The number of patients who had ingested benzodiazepines and doxylamine succinates was 26 cases (28.2%), organophosphorus was 20 (21.7%), paraquat was 10 (10.8%), others were 36 (39.3%). 4. Five kinds of po1ydrug ingestion was observed in 3 cases, four kinds was observed in 3, three kinds was observed in 5 and co-ingestion of alcohol was observed in 28 cases (30.4%). 5. The mortality was occurred in 4 cases, 2 of them were caused by paraquat, 1 of them was caused by organophosphorus (OP), 1 of them was caused by acetic acid. 6. The gastric larvage as a mean of treatment modality was done in 57 cases (61.9%). The use of activated charcoal was done in 8 (8.69%). The maintenance of tracheal intubation was done in 6 (6.52%). 7. The mean observational period in emergency department was 8 hours 42 minutes in benzodiazepine and doxylamine succinate group, 21 hours 46 minutes in OP, 20 hours 39 minutes in other germicidal except OP, 23 hours 9 minutes in paraquat group. Without a drug information and intoxication center in Korea, We should minimize the exhaustion of medical resources by establishment of determinant criteria which can be seen in relatively less-complicated cases of acute drug intoxication. Thus, we should consider the introduction of simple toxicology treatment protocol and toxicologic observation unit in emergency department as possible means to reduce economical and social burdens.

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Antagonistic Effects of Doxapram and Yohimbine on Tiletamine-Zolazepam Anesthesia in Dogs (개에서 Tiletamine-Zolazepam 마취에 대한 Doxapram과 Yohimbine의 길항효과)

  • Park Myeong-ho;Kim Myung-cheol
    • Journal of Veterinary Clinics
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    • v.12 no.1
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    • pp.799-818
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    • 1995
  • This study was performed to examine the general anesthetic efficacy of tiletamine-zolazepam, a mixture of phencyclidine-derived tiletamine and benzodiazepine-related zolazepam. The antagonistic activities of doxapram and yohimbine to the anesthetic effects of tiletamine-zolazepam were also studied. Thirty healthy mongrel dogs were divided into three groups (each of 10) twenty minutes after being anesthetized with tiletamine-zolazepam : T-Z-S group(tiletamine-zolazepam-saline), T-Z-D group (tiletamine -zolazepam-doxapram), T-Z-Y group (tiletamine-zolaz.pam-yohim bine). Various parameters wert evaluated in terms of the onset and recovery time of analgesia, respiration rates, hear rates, body temperature, electrocardiogram, blood chemistry, and lymphocyte blastogenesis. The results obtained through these experiment could be summarized as follows: 1. he anesthetic efficacy of tiletamine-zolazepam was considered desirable, with the onset time of anesthesia being as short as 0.23-0.24 minutes. 2. Both of the antagonistic effects of yohimbine and doxapram on the anesthesia induced by liletamine-zolazepan were evaluated statistically significant(p<0.05) as the recovery time was shortened from 39.3$\pm$4.9 min(T-Z-S group) to 25.3$\pm$2.9 nin(T-Z-Y group) and 29.9$\pm$8.8min(T-Z-D group), respectively. 3. Respiration rates were not changed by the treatments of both doxapram and yohimbine, with the only transient increase in the T-Z-D group. The changes in the respiration rate were not observed during the whole time course of the experiment. 4. Yohimbine(T-Z-Y group) increased the heart rate significantly from 30 minutes after the adminstration compared to the T-Z-S group and T-Z-D group (p<0.05). 5. The decreases in th, body temporature were observed from 30 minutes in the T-Z-S group(p<0.05) and 40 minutes in th, T-Z-D group(p<0.05), after the adminstration. On the other hand, there was no hypothermia in the T-Z-Y group. 6. In the all experimental groups of the T-Z-S, T-Z-D and T-Z-Y, there were no specific findings on the electrocardiograph incept slight shift to the tachycardia in all cases. 1. We could not find any differences in the blood chemistry between all experimental groups (T-Z-S, T-Z-D and T-Z-Y). 8. the inhibition of the lymphocyte blastogenesis shown in the T-Z-S with 3 hours decreasing and thereafter restoring to the normal values up to the point 5 hours were not occurred in the T-Z-D and T-Z-Y groups. With the above results, we could conclude that both doxapram and yohimbine can be clinically used as recovery agents towards anesthesia by tiletamine- zolazepam fi:on the efficacy point of view, but yohimbine is more recommendable in this case if considering the recovery time and lymphocyte blastogenesis.

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Convulsions with Noroviral Gastroenteritis in Children at a Single Center in Korea (단일 센터에서 경험한 소아에서의 노로바이러스 위장관염과 연관된 양성 경련)

  • Kang, SooYeon;Lee, Hyun Ju;Kim, Shin Hye
    • Journal of the Korean Child Neurology Society
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    • v.26 no.4
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    • pp.233-239
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    • 2018
  • Purpose: Viral gastroenteritis is a common disease in infants and children. Seizures can be associated with viral gastroenteritis as benign convulsions with mild gastroenteritis (CwG). After the development of the rotavirus vaccination, norovirus has become inreasingly significant in children. We retrospectively analyzed the clinical features in a pediatric population presenting with seizures and confirmed enteral viral infections, especially norovirus infections. Methods: We retrospectively reviewed the medical records of pediatric patients aged <15 years admitted due to convulsions and gastroenteritis to the Department of Pediatrics of Myongji Hospital between July 2014 and June 2016. Results: A total of 46 patients (24 male and 22 female) were included. Norovirus was detected in 21 (45.7%) patients, adenovirus in three (6.5%), rotavirus in two (4.3%), astrovirus in one (2.2%), and none of agents were detected in 19 (41.3%) patients. Patients in the norovirus gastroenteritis (NGE) group had a higher incidence of diarrhea than that among in the non-norovirus gastroenteritis (NNGE) group (61.9% vs 28.0%; P<0.05). Twelve patients experienced status epilepticus, including five (23.8%) in the NGE group and seven (33.0%) in the NNGE group (P=0.837). Seizures were effectively terminated by intravenous benzodiazepines in 8 (66.7%) of 12 patients. Additional long-acting antiepileptic drugs such as fosphenytoin or levetiracetam were required in three (25%) of 12 patients. Conclusion: Patients with CwG with and without noroviurs infection did not differ in terms of clinical features. However, status epilepticus was not uncommon among patients with CwG by definition.

Effect of GABA on the Contractility of Isolated Canine Trachealis Muscle (개의 기관근 수축성에 미치는 GABA의 효과)

  • Koo, Cheol-Hoe;Kwon, Oh-Chul;Choi, Eun-Mee;Lee, Kwang-Youn;Kim, Won-Joon
    • Journal of Yeungnam Medical Science
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    • v.11 no.2
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    • pp.314-322
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    • 1994
  • This study aimed to investigate the existence of GABA receptor and the mechanisms of action of GABA and diazepam on the trachealis muscle isolated from dog. Horizontal muscle strips of $2mm{\times}15mm$ were prepared from canine trachea, and isometric myography in isolated muscle chamber bubbled with 95/5%-$O_2/CO_2$at $36^{\circ}C$, at the pH of 7.4 was performed. Muscle strips contracted responding to the electrical field stimulation (ESP) by 2~20 Hz, 20 msec, monophasic square wave of 60 VDC GABA and diazepam suppressed the EFS-induced contractions to the similar extent, significantly. (p<0.05) Bicuculline, a $GABA_A$ receptor antagonist blocked both GABA- and diazepam- inhibitions; but DAVA, a $GABA_B$ receptor antagonist did not affect either of them. These results suggest that in the canine trachealis muscle, there may be only $GABA_A$ receptor, and GABA and diazepam inhibit the contractility via $GABA_A$A receptor.

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A Convenient Radiolabeling of [$^{11}$C](R)-PK11195 Using Loop Method in Automatic Synthesis Module ($^{11}$C 표지 자동합성장치에서 루프법을 이용한 ($^{11}$C)(R)-PK11195의 간편한 합성법)

  • Lee, Hak-Jeong;Jeong, Jae-Min;Lee, Yun-Sang;Kim, Hyung-Woo;Choi, Jae-Yeon;Lee, Dong-Soo;Chung, June-Key;Lee, Myung-Chul
    • Nuclear Medicine and Molecular Imaging
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    • v.43 no.4
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    • pp.337-343
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    • 2009
  • Purpose: ((R)-1-(2-chlorophenyl)-N-1-[$^{11}$C]methyl-N(1-propyl)-3-isoquinoline carboxamide ((R)-PK11195) is a specific ligand for the peripheral type benzodiazepine receptor and a marker of activated microglia, used to measure inflammation in neurologic disorders. We report here that a direct and simple radiosynthesis of [$^{11}$C](R)-PK11195 in mild condition using NaH suspension in DMF and one-step loop method. Materials and Methods: (R)-N-Desmethyl-PK11195 (1 mg) in DMSO (0.1 mL) and NaH suspension in DMF (0.1 mL) were injected into a semi-prep HPLC loop. [$^{11}$C]methyl iodide was passed through HPLC loop at room temperature. Purification was performed using semi-preparative HPLC. Aliquots eluted at 11.3 min were collected and analyzed by analytical HPLC and mass spectrometer. Results: The labeling efficiency of [$^{11}$C](R)-PK11195 was 71.8$\pm$8.5%. The specific activity was 11.8:$\pm$6.4 GBq/$\mu$mol and radiochemical purity was higher than 99.2%. The mass spectrum of the product eluted at 11.3 min showed m/z peaks at 353.1 (M+1), indicating the mass and structure of (R)-PK11195. Conclusion: By the one-step loop method with the [$^{11}$C]CH3l automated synthesis module, [$^{11}C$](R)-PK11195 could be easily prepared in high radiochemical yield using NaH suspension in DMF.

Clinical Trial of Nasal Flumazenil Administration (플루마제닐의 경비 투여)

  • Hong, Soo-Jin;Kim, Hyun-Jung;Yum, Kwang-Won
    • Journal of the korean academy of Pediatric Dentistry
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    • v.28 no.3
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    • pp.441-446
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    • 2001
  • Flumazenil is a competitive antagonist of benzodiazepines. It is usually administered intravenously. However, if the intravenous route is not available then other routes of drug administration should be considered. This study was designed to evaluate the reversal effects of flumazenil after nasal administration. Twenty-five young, healthy adult volunteers participated in this clinical trial. The dosage of 0.08mg/kg midazolam was administered intravenously to induce deep sedation. Ten minutes after midazolam administration, 0.5mg of flumazenil was dropped nasally, over a period of one minute. Blood samples were taken to measure the concentration of midazolam and flumazenil at 0, 5, 10, and 20min after nasal administration of flumazenil, using High Performance Liquid Chromatography. The degree of sedation was evaluated with sedation score and bispectral index (BIS), Statistical analysis was performed by multivariate ANOVA and correlation analysis (P<0.05). Peak serum flumazenil concentration was reached in 10min. Sedation score decreased after midazolam administration and showed a significant increase after flumazenil administration. However, BIS decreased during the first 10min after midazolam administration and then no significant changes after flumazenil administration. There were two instances representing rapid and complete reversal of midazolam after intranasal administration of flumazenil. In conclusion, intranasal flumazenil administration may be effective in some patients when intravenous route is not available in condition of benzodiazepine overdose.

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Effect of Cooking Methods and Reheating on Texture of Sausage (시판소시지의 조리방법 및 재가열이 조직특성에 미치는 영향)

  • 김성희;이숙미;조정순
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.26 no.1
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    • pp.37-44
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    • 1997
  • The Purpose of this study was to evaluate the effect of cooking methods and reheating on texture characteristics of sausage. Sausage samples were cooked(microwaving, gas-broiling and frying), reheated on day 3 and 6 after refrigeration and put to evaluation of sensory and texture characteristics. The results of sensory evaluation showed that hardness, salty taste, rancid flavor and after-taste were increased but wetness and chewiness were decreased by reheating after refrigeration. Overall acceptability was the highest when the samples were gas broiled and reheated on day 3 after refrigeration. As for the estimation of texture changes by rheometer, hardness, cohesiveness, elasticity, gum-miness and chewiness tended to increase by reheating after refrigeration. Hardness, cohesiveness, gumminess and chewiness were the highest when the samples were gas-broiled and reheated on day 3 after refrigeration.

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Neuropeptides in Clinical Psychiatric Research : Endorphins and Cholecystokinins (정신질환에 있어서의 신경펩타이드 연구 - Endorphin과 cholecystokinin을 중심으로 -)

  • Kim, Young Hoon;Shim, Joo Chul
    • Korean Journal of Biological Psychiatry
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    • v.5 no.1
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    • pp.34-45
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    • 1998
  • We provide the reader with a brief introduction to the neurobiology of neuropeptides. Several comprehensive reviews of the distribution and neurochemical, neurophysiological, neuropharmacological and behavioral effects of the major neuropeptides have recently appeared. In reviews of the large number of neuropeptides in brain and their occurance in brain regions thought to be involved in the pathogenesis of major psychiatric disorders, investigators have sought to determine whether alternations in neuropeptide systems are associated with schizophrenia, mood disorders, anxiety disorders, alcoholism and neurodegenerative disease. There is no longer any doubt that neuropeptide-containing neurons are altered in several neuropsychiatric disorders. One of the factors that has hindered neuropeptide research to a considerable extent is the lack of pharmacological agents that specifically alter the synaptic availability of neuropeptides. With the exception of naloxone and naltrexone, the opiate-receptor antagonists, there are few available neuropeptide- receptor antagonists. Two independent classes of neuropeptide-receptor antagonists has been expected to be clinically useful. Naltrexone, a potent ${\mu}$-receptor antagonist, has been used successfully to reduce the need for alcohol consumption. And cholecycstokinin antagonists are now in development as a new class of anxiolytics, which would be expected to be free from tolerance and physical dependence and lack of sedation. In this review, we deal with these two kinds of neuropeptide system, the opioid system and cholesystokinins in the brain. The role of opioid systems in the reinforcement after alcohol consumtion and that of cholesystokinins in the pathogenesis of anxiety will be discussed briefly. As we know, the future for neuropeptides in psychiatry remains bright indeed.

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