• Title/Summary/Keyword: PTZ test

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Synthesis and Anticonvulsant Evaluation of a Series of $N-Cbz-\alpha-aminoglutarimides$

  • Lee, Jaewon;Choi, Jongwon;Park, Minsoo
    • Archives of Pharmacal Research
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    • v.19 no.3
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    • pp.248-250
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    • 1996
  • In conclusion, a series of N-Cbz-.alpha.-amono-glutarimides (1a-f), combining common structures such as N-CO-C-N and cyclic imide in a single molecule, were prepared from the (R)- or (S)-N-Cbz-glutamic acid and evaluated for their anticonvulsant activities in MES and PTZ tests in order to develope new and broad spectrum anticonvulsant. In this study, N-Cbz-.alpha.-aminoglutarimides (1) except ac and af, showed significant anticonvulsant activity in both MES and PTZ tests enough to be recommended as promising new anticonvulsant drug candidates. Now we are continuing to investigate further anticonvulsant test (quantification)for these compounds and synthesize their analogues in order to develop more active anticonvulsant and define the structure activity relationship more precisely.

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Adansonia digitata L. Stem Bark Attenuates Epileptic Seizure, Depression, and Neurodegeneration by Mediating GABA and Glutamate in Pentylenetetrazol-Kindled Rats

  • Adamu Muhammad;Luteino Lorna Hamman;Samaila Musa Chiroma;Martha Orendu Oche Attah;Nathan Isaac Dibal
    • Journal of Pharmacopuncture
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    • v.26 no.4
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    • pp.327-337
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    • 2023
  • Objectives: Epilepsy is a neurological condition characterized by repeated seizures attributable to synchronous neuronal activity in the brain. The study evaluated the effect of acetone extract of Adansonia digitata stem bark (ASBE) on seizure score, cognition, depression, and neurodegeneration as well as the level of Gamma-Aminobutyrate acid (GABA) and glutamate in Pentylenetetrazol-kindled rats. Methods: Thirty-five rats were assigned into five groups (n = 7). Groups 1-2 received normal saline and 35 mg/kg PTZ every other day. Groups 3-4 received 125 mg/kg and 250 mg/kg ASBE orally while group 5 received 5 mg/kg diazepam daily for twenty-six days. Group 3-5 received PTZ every other day, 30 mins after ASBE and diazepam. Results: The results showed that Pentylenetetrazol (PTZ) induces seizure, reduces mobility time in force swim test and decreases the normal cell number in the brain. It also significantly decreases (p < 0.05) catalase, superoxide dismutase and reduced glutathione activities compared to the ASBE pre-treated rats. Pre-treatment with ASBE reportedly decreases seizure activities significantly (p < 0.05) and increases mobility time in the force swim test. ASBE also significantly elevate (p < 0.05) the normal cell number in the hippocampus, temporal lobe, and dentate gyrus. Conclusion: ASBE reduced seizure activity and prevented depression in PTZ-treated rats. It also prevented neurodegeneration by regulating glutamate and GABA levels in the brain as well as preventing lipid peroxidation.

The Effect of 6-Hydroxydopamine on the Anticonvulsant Activity of Clonazepam and Norepinephrine in Brain (뇌내(腦內) Norepinephrine함량변화(含量變化)와 Clonazepam의 항경련효과(抗痙攣效果)에 미치는 6-Hydroxydopamine의 영향(影響))

  • Yun, Jae-Soon;Kim, Young-Joo
    • YAKHAK HOEJI
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    • v.32 no.1
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    • pp.40-49
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    • 1988
  • There is evidence that brain norepinephrine may play a role in experimentally induced seizures in animals. Thus the present experiments were undertaken in an attempt to explore the role of brain norepinephrine in anticonvulsant activity of clonazepam. 6-Hydroxydopamine was given to newborn rats and PTZ-induced seizures were tested $70{\sim}90$ days after birth and the rats were killed for determination of brain norepinephrine 8 days after the seizure test. Depletion of norepinephrine in the rat brain significantly potentiated the PTZ-induced convulsions and antagonized the effect of clonazepam on clonic seizures, tonic seizures and the number of seizures, but the latency to the seizure and the mortality has not been altered. However the 6-hydroxydopamine-induced antagonism of anticonvulsant action was surmountable by increasing the dose of clonazepam. These results show that brain norepinephrine may play an important role in seizure susceptability as well as in the anticonvulsant activity of clonazepam in rats.

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Synthesis of N-acyl-α-aminosuccinimides and N-acyl-α-aminoglutarimides (N-아실-α-아미노숙신이미드와 N-아실-α-아미노글루탈이미드의 합성)

  • 정대일;김문주;송현애;김윤영;이용균;박유미;최순규;한정태;박민수
    • Journal of Life Science
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    • v.14 no.1
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    • pp.91-97
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    • 2004
  • As a part of our study on the improvement of anticonvulsant, here we report the synthesis of N-acyl-$\alpha$-aminosuc-cinimides 1 and N-acyl-$\alpha$-aminoglutarimides 2. (R)-Benzoic acid 4-benzyloxycarbonylamino-2-oxo-pyrrolidin-1-ylester 6a, (R)-4-nifro-benzoic acid 4-benzyloxycarbonylamino-2- oxo-pyrrolidin-1-yl ester 6b, (R) -4-nitro-benzoic acid 4-benzyloxycarbonylamino-2-oxo-pyrrolidin-1-yl ester 6c, and (R)-propionic acid 4-benzyloxycarbonylamino-2-oxo-pyrrolidin-1-yl ester 6d were synthesized from (R)-2-benzyloxy carbonylamino-succinic acid 3 as a starting meterial. (R)-(3- Benzyloxycarbonylamino-2,6-dioxo-piperidin-1-yloxy)-acetic acid methyl ester 10a, (R)-(3-benzyloxycarbonylamino-2,6-dioxo-piperidin-1-yloxy)-acetic acid ethy1 ester 10b, an d (R)-2-(3-benzyloxycarbonylamino-2,6- diox o-piperidin-1-yl oxy)-propionic acid methyl ester l0c were synthesized from (R)- 3-carbobenzyloxy-amino-glutarmic acid 7 as a starting meterial. The yield, mp, IR, $^1H-NMR,\; and^{13}C$- NMR spectra of the products 6a, 6b, 6c, 6d, 10a, l0b, l0c are summarized in footnote. The biological studies of these compounds are in progress and will be reported in future.

The Prophylactic and Therapeutic Effects of Saffron Extract and Crocin on Ethanol Withdrawal Syndrome in Mice

  • Shoja, Maryam;Mehri, Soghra;Amin, Bahareh;Askari, Vahid Reza;Hosseinzadeh, Hossein
    • Journal of Pharmacopuncture
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    • v.21 no.4
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    • pp.277-283
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    • 2018
  • Objectives: Ethanol withdrawal following its chronic use is a serious outcome and challenging to treatment. The chronic use of ethanol induces a progressive neuroplasticity in different reigns of brain. In this study we evaluated the effects of aqueous extract of Crocus sativus L. (saffron) and its active compound, crocin, on the withdrawal behavior induced after repeated administration of ethanol, in two regimens of prophylactic (administration of drugs concomitant with the induction of dependence) and treatment (administration of drugs during the period of ethanol withdrawal) in mice which received ethanol. Methods: Ethanol dependence was induced by oral administration of 10% v/v ethanol (2 g/kg) for 7 days. The aqueous extracts of saffron (40, 80 and 160) and crocin (10, 20 and 40 mg/kg) were administered to mice in two regimens of prophylactic (along with ethanol) and treatment (during withdrawal period). Diazepam (1 mg/kg) was used as a positive control. Six hours after discontinuation of the ethanol, seizure was evaluated by the sub-convulsive dose of pentyleneltetrazole (PTZ) (30 mg/kg). The open field test and Rota rod test were used for evaluation of locomotor activity and motor incoordination, respectively. Results: Both extracts and crocin increased the number of crossed lined in the open field test. PTZ kindling seizure was inhibited in animals received extract (80 and 160 mg/kg) in both regimens. Motor incoordination was only improved following administration of crocin. Conclusion: The aqueous extract of saffron and crocin can be considered as safe agents and reliable alternative to diazepam in management of ethanol withdrawal syndrome.

The Study on the Fire Monitoring Dystem for Full-scale Surveillance and Video Tracking (전방위 감시와 영상추적이 가능한 화재감시시스템에 관한 연구)

  • Baek, Dong-hyun
    • Fire Science and Engineering
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    • v.32 no.6
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    • pp.40-45
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    • 2018
  • The omnidirectional surveillance camera uses the object detection algorithm to level the object by unit so that broadband surveillance can be performed using a fisheye lens and then, it was a field experiment with a system composed of an omnidirectional surveillance camera and a tracking (PTZ) camera. The omnidirectional surveillance camera accurately detects the moving object, displays the squarely, and tracks it in close cooperation with the tracking camera. In the field test of flame detection and temperature of the sensing camera, when the flame is detected during the auto scan, the detection camera stops and the temperature is displayed by moving the corresponding spot part to the central part of the screen. It is also possible to measure the distance of the flame from the distance of 1.5 km, which exceeds the standard of calorific value of 1 km 2,340 kcal. In the performance test of detecting the flame along the distance, it is possible to be 1.5 km in width exceeding $56cm{\times}90cm$ at a distance of 1km, and so it is also adaptable to forest fire. The system is expected to be very useful for safety such as prevention of intrinsic or surrounding fire and intrusion monitoring if it is installed in a petroleum gas storage facility or a storing place for oil in the future.

Antioxdative Effect of the Essential Oil form the Rhizomes of Acorus gramineus (석창포 정유성분의 항산화활성)

  • 구병수;이동웅
    • Journal of Life Science
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    • v.11 no.6
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    • pp.503-508
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    • 2001
  • The essential oil of Acorus gramineus(Aracease), which has been used as an antioconvulsant in Korean folk medicine, was evaluated for its effects on antioxidative system in vitro and in vivo. This mixture of terpenes showed inhibitory effects on xanthine oxidase activity with 13.3% at 10 $\mu\textrm{g}$/ml and on aldehyde oxidase activity with 5.0% at 1$\mu\textrm{g}$/ml. Lipid perosidation was inhibited by 49.4% at 1.0 mg/ml of the essential oil in vitro and by 16.7% after 7 days inhablation of an oil as compared to PTZ-treated control group. DPPH radical scavenging activity of this essential oil was ralatively werak.

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Automatic FOD Detection Test Using EO/ IR Laser Light Camera (EO / IR Laser Light 카메라를 이용한 FOD 자동탐지 시험)

  • Shin, Hyun-Sung;Hong, Gyo-Young;Hong, Jae-Beom;Choi, Young-Soo;Kim, Yun-Seob
    • Journal of Advanced Navigation Technology
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    • v.21 no.6
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    • pp.638-642
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    • 2017
  • FOD is a generic term for substances with potential threats that can pose a fatal risk to aircraft. Therefore, FOD should be noted in all areas of the airport. Especially, the method of detecting and collecting FOD in runway and aircraft movements is very low efficiency and economical efficiency of airport operation, so it is essential to develop FOD automatic detection system suitable for domestic environment. As part of the aviation safety technology development project, the development of an automatic detection system for foreign matter in the moving area of the aircraft inside the airport is underway. In this paper, it is confirmed that EO / IR camera is used for detection of foreign objects at Taean Airfield of Hanseo University. EO camera is used during the day and IR camera is used at night.