• The Korean Journal of Physiology
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• v.6 no.1
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• pp.27-31
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• 1972

The activity of Mg and Na-K activated ATPase of homogenate from rat brain cortex was measured in vitro under the variety of conditions. The effects of various hypnotic and tranquilizer such as phenobarbital, amobarbital, diazepam, promazine and chlorpromazine on the activities of both ATPase was investigated and the results was summarized as follows. 1. Na-K ATPase was slightly inhibited by phenobarbital and amobarbital while Mg ATPase was moderately activated by these drugs. 2. Both Mg and Na-K ATPase activities were markedly inhibited by diazepam. 3. Promazine and chlorpromazine markedly inhibited both Mg and Na-K ATPase activities. These findings indicate that remarkable correlation between hypnotic or tranquilizing potency and ATPase inhibition could be observed.

• 대한임상약리학회:학술대회논문집
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• 1993.12a
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• pp.42-42
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• 1993

• The Korean Journal of Pharmacology
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• v.11 no.1 s.17
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• pp.55-60
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• 1975

An animal which is placed in a new environment displays a complex behavioral pattern consisting of locomotion, grooming and rearing. This behavioral pattern is influenced by endogenous and exogenous stimuli, such as hormonal secretion, level of neurohumoral transmitters, drugs and light. It is widely known that the most tranquilizers depressed spontaneous motor activity although their mechanisms of action were different, while antidepressants stimulated except imipramine which showed various action. Until the present time, the hole-board apparatus, which gives rather subjective data, has been used extensively to study the effects of drugs on general activity and exploratory behavior in mice. Recently a new apparatus for mobility measurements, called a 'Selective Activity Meter' has been introduced. This instrument supposedly produces more objective data on activity and behavior. The purpose of the present experiment was to study the influence of psychotropics on motor activity using the Selective Activity Meter. In the experiment, various psychotropic agents such as major tranquilizers(chlorpromazine, haloperidol); minor tranquilizers(meprobamate, diazepam); and antidepressants(amphetamine, imipramine) were used. In each experiment, the drug was administered to five mice and their activity was recorded. Each experiment was run five or more times and the results are based on the mean of each trial. The results are summarized as follows: 1. The group of mice treated with chlorpromazine showed markedly inhibited motor activity in comparison with controls and the inhibitory action of chlorpromazine was shown to be more intense than any of the other drugs used in the test. Haloperidol administration yielded similar results until 60 minutes, but mice showed less inhibition of motor activity than with chlorpromazine after 90 minutes. 2. In the group treated with diazepam, there was strong inhibition of motor activity until 30 minutes, but after 60 minutes the mice showed less inhibition than with chlorpromazine. In the meprobamate group, motor activity was inhibited in a manner similar to that of other tranquilizers, but the inhibition was less than that of diazepam. 3. In the group treated with imipramine, the inhibition developed gradually after ten minutes. 4. The effects of amphetamine did not appear until 30 minutes after administration, but then there was a significant increase in the motor activity.

• International Journal of Oral Biology
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• v.31 no.2
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• pp.33-43
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• 2006

Dysplasia-associated seizure disorders are markedly resistant to pharmacological intervention. Relatively little research has been conducted studying the effects of antiepileptic drugs(AEDs)on seizure activity in a rat model of dysplasia. We have used rats exposed to methylazoxymethanol acetate(MAM) in utero, an animal model featuring nodular heterotopia, to investigate the effects of AEDs in the dysplastic brain. Pilocarpine was used to induce acute seizure in MAM-exposed and age-matched vehicle-injected control animals. Field potential recordings were used to monitor amplitude and numbers of population spikes, and paired pulse inhibition in response to stimulation of commissural pathway. Two commonly used AEDs were tested: diazepam 5, 2.5 mg/kg; phenytoin 40, 60 mg/kg. Diazepam(DZP) and phenytoin(PHT) reduced the amplitude of population spike in control and MAM-exposed rats. However, the amplitude of population spike was nearly eliminated in control rats as compared to the MAM-exposed rats. Pharmaco-resistance was tested by measuring seizure latencies in awake rats after pilocarpine administration(320 mg/kg, i.p.) with and without pretreatment with AEDs. Pre-treatment with PHT 60 mg prolonged seizure latency in control rats, but not in MAM-exposed animals. The main findings of this study are that acute seizures initiated in MAM-exposed rats are relatively resistant to standard AEDs assessed in vivo. These data suggest that animal model with cortical dysplasia can be used to screen the effects of potential AEDs.

• Biomolecules & Therapeutics
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• v.4 no.2
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• pp.167-173
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• 1996

This study was undertaken to evaluate a behavior-electroencephalogram (EEG) pattern relationship in pilocarpine- and kainic acid-induced convulsions of rats. Also we intended to examine the effect of a noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist, MK-801, and diazepam on the pilocarpine-induced behavioral and electrical seizures in rats. The electrical activities at frontal and hippocampal areas and behavior activities were measured in freely moving rats. At the beginning of the experiments, the rats displayed an exploratory behavior. This awake and moving phase with a low amplitude, irregular, 4-10 Hz wave was followed by a still phase. Pilocarpine (400 mg/kg, i.p.) and kainic acid (0.5 mg/kg, i.c.v.) induced tonic and clonic seizures. The pilocarpine-induced change in electrical activities exhibited a weak correlation with behavioral convulsion at all stages. The amplitude and duration of the electrical response were not linear with the degree of behavioral score. An application of MK-801 (dizocilpine, 7.5 mg/kg) did not affect the amplitudes of the convulsant-induced electrical activities, though the same dose of this drug caused the deformation of the electrical pattern. There was no effect of MK-801 on the behavioral and electrical activities as expected. Diazepam (1 mg/kg) did not affect the amplitude of the electrical activities induced by pilocarpine but changed the pattern of these activities. Our study shows that there is no linear relationship between degree of behavior and amplitude of electrical activities of convulsants. This may indicate that the NMDA receptor stimulation can be processed by the neocortical or hippocampal network in a different way between behavioral and electrical activities.

• CELLMED
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• v.9 no.1
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• pp.1.1-1.13
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• 2019

Background: Contents of bioactive substances extractable from different parts of terrestrial plants vary enormously. Aim: To ascertain that parts of Withania somnifera other than its roots can also be used for prevention and cure of unavoidable stress triggered central hypersensitivity to pain. Material and Methods: Groups of male or female mice treated either with Withania somnifera extracts or with metformin, aspirin, imipramine, diazepam and niacin for 11 consecutive days were subjected to "foot-shock stress-induced hyperthermia" and "hot plate" tests on the 1st, 5th, 7th, and 10th days of the experiments. On the 11th day, they were subjected to tail suspension test and on 12th day pentobarbital hypnosis test. Results: Except for diazepam and imipramine, protective effects of all other tested drugs as well as of the Withania somnifera extracts against stress-induced central hypersensitivity to pain were accompanied by their preventive effects against foot-shock stress-induced body weight losses. All observed stress response suppressing effects of all test agents increased with increasing numbers of treatment days. However, mean duration of pentobarbital-induced sleep was shorter in the extracts treated groups and longer in the diazepam treated ones only. Conclusions: Reported observations reveal that pharmacological activity profile of Withania somnifera extracts in male and female mice are almost identical, and are not like those of several drugs currently often prescribed for the treatment of diabetes-associated comorbidities. Withanolides are not the only extractable bioactive constituents of Withania somnifera. The described bioassay system is well suited for pharmacological standardization of diverse types of Withania somnifera extracts.

• Journal of Physiology & Pathology in Korean Medicine
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• v.35 no.1
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• pp.8-14
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• 2021

Shihogayonggolmoryo-tang (ST) is a Korean medical herb cocktail which has been used to treat anxiety induced insomnia. In this study, we will examine sleep-promoting and anti-anxiety effects of ST, and investigate its mechanism. ICR mice were divided into three groups for the first examination : control group (n=11), ST50 group (50 mg/kg, po, n=11), ST200 group (200 mg/kg, po, n=11). Sleep-promoting effect was confirmed by measuring the sleeping duration time and sleeping onset time after thiopental sodium treatment (50 mg/kg, ip). ICR mice were divided into five groups for the second examination : control group (n=11), ST200 group (200 mg/kg, po, n=11), ST200+Flumazenil group (ST 200 mg/kg, po, flumazenil 0.3 mg/kg, ip, n=11), diazepam group (1 mg/kg, ip, n=11), diazepam+flumazenil group (diazepam 1 mg/kg, ip, Flumazenil 0.3 mg/kg, ip, n=11). Anxiety behavior and sleep-promoting effect was confirmed by open field test and measuring the sleeping duration time and sleeping onset time. Expression levels of c-fos in tuberomammillary nucleus (TMN) and ventrolateral preoptic nucleus (VLPO) were analyzed by immunohistochemistry. ST treated group showed significantly decreased anxiety behavior and enhanced sleeping duration time and sleeping onset time concentration dependently. The expression of c-fos was significantly upregulated in VLPO as sleep-inducing center and TMN as downregulated in arousal center by ST treatment. In addition, all effects of ST were reversed by flumazenil. Our results suggest that ST has sleep-promoting and anti-anxiety effects through regulating arousal center (TMN) and sleep-inducing center (VLPO).

• Proceedings of the Korea Environmental Mutagen Society Conference
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• 2004.05a
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• pp.74-75
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• 2004

• Journal of The Korean Dental Society of Anesthesiology
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• v.3 no.2 s.5
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• pp.87-91
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• 2003

Background: The purpose of this study was to compare the availability of propofol and fentanyl (P + F) with diazepam and morphine (D + M) for intravenous conscious sedation during third molar surgery. Methods: Forty patients without systemic disease were operated under IV conscious sedation administered by either of the two techniques. Monitoring consisted of continuous observation of pulse rate, blood pressure, oxygen saturation, and the respiratory rate and were recorded every 15 minutes. Cooperation score was measured 5 and 15 minutes after induction of IV sedation. Following the operation, the surgeon and patients completed questionnaires including pain visual analog scale, amnesia, and side effects. Results: The P + F group was significantly more cooperative than the D + M group. The side effects of D + M group included pain on injection, nausea/vomiting and abdominal pain. The side effects of P + F group included talkativeness, nausea/vomiting, temporary apnea, pain on injection and vertigo. Conclusions: In this study, there were following benefits in the P + F group; more cooperative status and less pain perception. But respiratory depression developed in some patients.

• Biomolecules & Therapeutics
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• v.16 no.3
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• pp.261-269
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• 2008

This experiment was performed to investigate the anxiolytic-like effects of cyclopeptide fraction alkaloids of Zizyphi Spinosi Semen (CFAZ), by using the experimental paradigms of anxiety, and compared with those of a known anxiolytic, diazepam. CFAZ (8.0 mg/kg, p.o.) increased the percentage of time spent on the open arms and the number of open arms entries in the elevated plus-maze test, increased the number of head dips in the hole-board test, and increased the percentage of center zone ambulatory time in the open-field box. However, CFAZ has no effect on the locomotor activity, while diazepam (2.0 mg/kg, p.o.) significantly reduced locomotor activity. CFAZ did not influence the grip force in the grip strength meter test, either. From the molecular experiments, CFAZ increased chloride influx in cultured cerebellar granule cells. In addition, $GABA_A$ receptors $\gamma$-subunit were over-expressed by CFAZ in cultured cerebellar granule cells. It is concluded that CFAZ may have anxiolytic-like effects, and these effects may be mediated by $GABA_A$ receptors.