• 대한화학회지
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• 제64권1호
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• pp.7-18
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• 2020

An efficient and facile procedure has been developed for the synthesis of novel bichalcone derivatives (4a, 4b). The key step contains the solvent-free aldol synthesis of bichalcones based on quinones. Bichalcones (4a, 4b) were used as precursors for the synthesis of some interesting heterocyclic compounds like, diazepines (5a, 5b), pyrazolo-pyrimidines (7a, 7b), and pyrazoline derivatives (8a, 8b). Moreover, new thioxopyrimidine derivatives (9a, 9b) were furnished and used as a functionalizing agent to produce the triazole-pyrimidines (11, 12) and the carbonitrile derivative (14). All the synthesized compounds were fully characterized using physical and spectral data like, FT-IR, ¹H NMR, ¹³C NMR, and MS. Bichalcones (4a, 4b) and diazepines (5a, 5b) were screened for their anticonvulsant activity, where compounds (4a, 5a, and 5b) revealed potent anticonvulsant activity compared to diazepam. On the other hand, some of the prepared compounds were screened for their antiproliferative activity and they showed significant cytotoxic effects on most of the cancer cell lines with regard to broad spectrum antitumor activity.

• Natural Product Sciences
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• 제22권4호
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• pp.263-269
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• 2016

Rhynchophylline (RP) is a major tetracyclic oxindole alkaloid of Uncariae Ramulus et Uncus which has been used to treat hypertension, seizures, pain and anxiety in the oriental countries. A recent report revealed that RP attenuated ischemia-induced neuronal damage and kainite-induced convulsions in animals. This study was performed to investigate whether RP enhances pentobarbital-induced sleep behaviors and modulates sleep architecture in mice. Locomotor activity was significantly inhibited by RP at 0.25 and 0.5 mg/kg, similar to 2 mg/kg diazepam (a benzodiazepine agonist) in mice. RP shortened sleep latency and increased total sleep time in a dose-dependent manner when administrated with pentobarbital (42 mg/kg, i.p.). RP also increased the number of sleeping mice and total sleep time by concomitant administration with the sub-hypnotic dosage of pentobarbital (28 mg/kg, i.p.). On the other hand, RP (0.25 mg/kg, p.o.) itself significantly inhibited sleep-wake cycles, prolonged total sleep time, and rapid eye movement in rats. In addition, RP also increased chloride influx in the primary cultured hypothalamic neuronal cells. In addition, we found that glutamic acid decarboxylase ($GAD_{65/67}$) was activated by RP. In conclusion, RP augments pentobarbital-induced sleeping behaviors, and can be a candidate for treating insomnia.

• 대한의용생체공학회:학술대회논문집
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• 대한의용생체공학회 1995년도 추계학술대회
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• pp.147-150
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• 1995

최근의 마취과학에 관한 연구에 있어서의 주된 경향은 마취심도 및 의식수준의 결정을 신경생리학적인 관점에서 분석하고자 하는 것이다. 즉, 마취와 의식에 관한 인간의 뇌가 가지고 있는 기능이나 약리학적인 반응을 대표할 수 있는 생체신호를 검출, 분석하여 정량화하고 이들을 이용하면 마취심도 및 의식수준과의 큰 상관관계를 얻을 수 있을 것이라 가정하는 것이다. 본 연구에서는 청각유발전위 (LAEP, Long latency Auditory Evoked Potential)를 검출하여 추출된 변수들과 마취제 투여량간의 변화에 따른 상관성을 분석하고자 하였다. 수술환자(17명)를 대상으로 실험을 실시하였으며 마취제로서는 Midazolam과 Diazepam을 인체로 투여하고 1 KHz와 2 KHz의 청각자극을 제시하였을 때 피검자로부터 발생되는 LAEP를 검출하였다. 검출된 LAEP로부터 추출된 N100과 P300의 진폭은 마취량의 증가에 따라서 간소함을 알 수 있었으며, 이러한 유의한 상관성을 보이는 진폭의 변화는 마취제의 투여에 따른 의식수준의 변화를 나타내는 지수(index)의 설정 및 알고리듬의 수립에 이용될 수 있을 것이다.

• 약학회지
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• 제53권5호
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• pp.241-249
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• 2009

Various neurotransmitters are involved in regulating stress systems. In this study, we investigated the combination relieving effect of green tea extract(GTE) and L-theanine on the stress induced by electric foot shock. Four week oral administration of GTE (24 mg/kg), L-theanine (4 mg/kg) or their combination reduced the levels of dopamine, noradrenaline and corticosterone in blood, brain cortex, hippocampus, and striatum, wherease increased serotonin level. The combination of GTE and L-theanine showed much greater effects than single treatment of each component, and the effects are comparable to diazepam (2 mg/kg). Therefore, this study suggests that the combination of GTE and L-theanine may act effective and be useful for stress relieving treatment.

• Clinical and Experimental Pediatrics
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• 제57권9호
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• pp.384-395
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• 2014

Febrile seizure (FS) is the most common seizure disorder of childhood, and occurs in an age-related manner. FS are classified into simple and complex. FS has a multifactorial inheritance, suggesting that both genetic and environmental factors are causative. Various animal models have elucidated the pathophysiological mechanisms of FS. Risk factors for a first FS are a family history of the disorder and a developmental delay. Risk factors for recurrent FS are a family history, age below 18 months at seizure onset, maximum temperature, and duration of fever. Risk factors for subsequent development of epilepsy are neurodevelopmental abnormality and complex FS. Clinicians evaluating children after a simple FS should concentrate on identifying the cause of the child's fever. Meningitis should be considered in the differential diagnosis for any febrile child. A simple FS does not usually require further evaluation such as ordering electroencephalography, neuroimaging, or other studies. Treatment is acute rescue therapy for prolonged FS. Antipyretics are not proven to reduce the recurrence risk for FS. Some evidence shows that both intermittent therapy with oral/rectal diazepam and continuous prophylaxis with oral phenobarbital or valproate are effective in reducing the risk of recurrence, but there is no evidence that these medications reduce the risk of subsequent epilepsy. Vaccine-induced FS is a rare event that does not lead to deleterious outcomes, but could affect patient and physician attitudes toward the safety of vaccination.

• Natural Product Sciences
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• 제18권2호
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• pp.67-75
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• 2012

Zizyphi Spinosi Semen (ZSS) have been widely used for the treatment of insomnia in Asia. This experiment was performed to investigate whether methanol extract of ZSS (MEZSS) has hypnotic effects through the ${\gamma}$-amino butyric acid (GABA)ergic systems. MEZSS inhibited the locomotor activity. MEZSS enhanced pentobarbital-induced sleep behaviors. However, MEZSS itself did not induce sleep at higher dose, similar to muscimol. On the other hand, both pentobarbital and MEZSS increased the non rapid eye move (NREM) sleep, especially reducing the -wave electroencephalogram (EEG) activity in REM sleep. MEZSS showed similar effects with muscimol on potentiating chloride influx induced by pentobarbital. MEZSS significantly increased GABAA receptors ${\gamma}$-subunit expression and slightly decreased ${\beta}$-subunit expression in hypothalamus and thalamus, showing that subunit-expression was similar to diazepam. In addition, MEZSS enhanced the expression of glutamic acid decarboxylase (GAD). In conclusion, it is suggested that MEZSS might augment pentobarbital-induced sleep behaviors through the modification of GABAergic systems.

• 약학회지
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• 제43권3호
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• pp.300-305
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• 1999

A sensitive and efficient assay method was applied to determine the level of glutamic acid (GA) and ${\gamma}-aminobutyric$ acid (GABA) in frontal cortex and hippocampus of rat administrated with ethanol and drugs. The compounds were derivatized with ο-phthalaldehyde (OPA) and 2-mercaptoethanof for precolunm analysis. The condition for the simultaneous determination of GA, GABA and $\beta-aminobutyric$ acid (BABA) by high performance liquid chromatography with electrochemical detection was reverse phase $C_{18}$ column as stationary phase, 0.1 M phosphate buffer containing 0.1 mM $Na_4EDTA$ : methanol = 55:45 (v+v) pH 3.8 as mobile phase and 0.7V electrode voltage. The stability of reaction product of GA, GABA and BABA with OPA could be increased by adding the same volume of polyethylene glycol 400 to reaction mixture. The GABA level in frotal cortex of rat was significantly decreased by the administration of picrotoxin and diazepam, but it was significantly increased by the administration of red ginseng total saponin, N-methyl-D-glucamine and (-)-deprenyl.

• 약학회지
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• 제54권3호
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• pp.205-214
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• 2010

This study aimed to evaluate the patterns of inappropriate medication use and inappropriate dosage in elderly patients in Korea. A retrospective study was performed for the elderly 65 years or older admitted from January 2007 to December 2007 in a medical center, Seoul, Korea. Potentially inappropriate medication (PIM) use in the elderly was evaluated using Beers criteria. Eighteen drugs out of Beers criteria were included in the formulary of the institute. Inappropriate dosage was set using Beers criteria, CMS (the Centers for Medicare& Medicaid Services) guideline, Geriatric Dosage Handbook. As results, the patients with PIM were 2,172 during the study period. The commonly used inappropriate medications were drugs for the nervous system (n=1237, 44.78%), the alimentary System (n=663, 24.54%) and the cardiovascular system (n=494, 18.28%). The elderly patients with prescription of inappropriate dosage were 10% out of patients with PIMs. The commonly inappropriate dosage drugs were digoxin (n=75, 27.27%), diazepam (n=70, 22.55%) and ferrous sulfate (n=66, 24.00%). Logistic regression analysis showed the number of PIM, days of hospital stay as predictors related to inappropriate dosage use. In conclusion, CNS drugs were frequently prescribed as PIM and inappropriate dosages were identified. It is needed to develop a means of decreasing adverse drug events in elderly.

• 한국임상수의학회지
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• 제37권5호
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• pp.273-277
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• 2020

A 12-year-old, female Maltese was referred with uncontrolled hyperadrenocorticism (HAC). Despite well management of HAC through treatment with trilostane and serial monitoring with ACTH stimulation tests for over three years, stiffness of the neck and limbs progressively worsened over time. Neurological test was performed, which showed no abnormalities of cranial nerves. Proprioception was delayed but the cause appeared to be due to stiffness of limb muscles. Muscle tone had increased over time and stiffness had worsened to the extent where it made walking difficult. MRI scans showed no orthopedic or spinal diseases, and pituitary microadenoma was confirmed with pituitary gland measurement of 6 × 6.4 × 4.5 mm (H × W × L). Electromyography presented random discharges with fluctuating amplitude and frequency, which were consistent with myotonic discharges. There were no improvements of myotonic signs despite treatment for HAC with trilostane. Supplementation of L-carnitine and coenzyme Q-10 to mitigate muscle stiffness, following diazepam and methocarbamol to help with muscle rigidity, failed to show any positive effect and the dog died a sudden death, 1,182 days after the initial visit.

• Fisheries and Aquatic Sciences
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• 제17권1호
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• pp.13-18
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• 2014

Sleep is vital to maintain health and well-being; however, insomnia is currently a widespread health complaint worldwide. In particular, caffeine, a psychoactive component of coffee, tea, and caffeine beverages may lead to sleep disorders such as insomnia. In this study, our primary objective was to investigate the inhibitory effect of high-purity phlorotannin preparation (HP-PRT) on caffeine-induced wakefulness. The sleep test of pentobarbital-induced mice was used as an in vivo animal model. Caffeine (50 and 100 mg/kg) showed significant arousal effects (an increase in sleep latency and a decrease in sleep duration). Co-administration of caffeine (50 mg/kg) and the sedative-hypnotic diazepam (DZP, 1 mg/kg) did not result in similar arousal activity. HP-PRT (500 mg/kg) also inhibited caffeine-induced wakefulness. Our results suggest that HP-PRT would be a useful additive for developing coffee products without the arousal effect.