• The Korean Journal of Physiology and Pharmacology
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• 제17권6호
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• pp.485-491
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• 2013

The present study was designed to investigate the putative effect of neurosteroid modulation on global ischaemia-reperfusion-induced cerebral injury in mice. Bilateral carotid artery occlusion followed by reperfusion, produced a significant rise in cerebral infarct size along with impairment of grip strength and motor coordination in Swiss albino mice. Administration of carbamazepine (16 mg/kg, i.p.) before global cerebral ischaemia significantly attenuated cerebral infarct size and improved the motor performance. However, administration of indomethacin (100 mg/kg, i.p.) attenuated the neuroprotective effect of carbamazepine. Mexiletine (50 mg/kg, i.p.) did not produce significant neuroprotective effect. It may be concluded that the neuroprotective effect of carbamazepine may be due to increase in synthesis of neurosteroids perhaps by activating enzyme ($3{\alpha}$ HSD) as indomethacin attenuated the neuroprotective effect of carbamazepine. The sodium channel blocking effect of carbamazepine may not be involved in neuroprotection as mexiletine, a sodium channel blocker, did not produce significant neuroprotective effect.

• Archives of Pharmacal Research
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• 제29권7호
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• pp.566-569
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• 2006

This study examined whether or not acute stress is linked to increases in the neurosteroid levels, which is a well-known neurotransmitters associated with stress stimuli. The ginsenoside, Rb1, was tested in order to better understand its potential effects on altering the neurosteroid levels and ultimately attenuating stress. The optimal stressed condition was checked by measuring the 5a-dihydroprogesterone (DHP) and allopregnanolone (THP) levels in the brain after immobilization stress at various times. Based on this result, an acute stress model was set up to give 30 min of immobilization stress. The DHP and THP brain levels of the stressed mice were then investigated after administering Rb1 orally (10 mg/kg). These results were compared with the neurosteroid level in the stressed mice not given Rb1. Saline was administered orally to the nonstressed mice to check the placebo effect. Acute immobilization stress induced an increase in the THP and DHP concentration in the frontal cortex and cerebellum. When Rb1 was administered orally prior to immobilization stress, the THP level in the frontal cortex and cerebellum was significantly lower than that in the stressed animals not given Rb1. On the other hand, the DHP level was lower in the cerebellum only. This suggests that the metabolism of the brain neurosteroids is linked to psychological stress, and Rb1 attenuates the stressinduced increase in neurosteroids.

• Journal of Photoscience
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• 제9권2호
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• pp.5-8
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• 2002

Photoperiodism is an important adaptive phenomenon in various physiological parameters including reproduction to cope with seasonal changes. Involvement of extraretinal photoreceptors in the photoperiodism in non-mammalian vertebrates has been well established. In addition, circadian clock system is known to be involved in the photoperiodic time measurement. The pathway consists of light-input system, time measurement system (circadian clock), gonadotropin releasing hormone (GnRH) production in the hypothalamus, luteinizing hormone (LH) and follicle stimulating hormone (FSH) production in the pituitary, and final gonadal development. Recently, several laboratories reported photopigments newly cloned in the pineal, eyes and deep brain in addition to already known visual pigments in the retina. These are pinopsin, parapinopsin, VA-opsin, melanopsin, etc. All these photopigments belong to the opsin family having retinal as the chromophore. However, the function of these photopigments remains unknown. I reviewed the studies on the location of the photopigments by immunocytochemistry. I also discussed the results on the action spectra for induction of gonadal development in relation with the location of the photoreceptors. Various physiologically active substances distribute in the vertebrate brain. Such substances are GnRH, GnIH, neuropeptide Y, vasoactive intestinal peptide, c-Fos, galanin, neurosteroids, etc. I summarized the immunhistochemical studies on the distribution and the photoperiodic changes of these substances and discussed the route from the deep brain photoreceptor to GnRH cells.

• The Korean Journal of Pain
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• 제28권1호
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• pp.4-10
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• 2015

Etifoxine (etafenoxine, $Stresam^{(R)}$) is a non-benzodiazepine anxiolytic with an anticonvulsant effect. It was developed in the 1960s for anxiety disorders and is currently being studied for its ability to promote peripheral nerve healing and to treat chemotherapy-induced pain. In addition to being mediated by $GABA_A{\alpha}2$ receptors like benzodiazepines, etifoxine appears to produce anxiolytic effects directly by binding to ${\beta}2$ or ${\beta}3$ subunits of the $GABA_A$ receptor complex. It also modulates $GABA_A$ receptors indirectly via stimulation of neurosteroid production after etifoxine binds to the 18 kDa translocator protein (TSPO) of the outer mitochondrial membrane in the central and peripheral nervous systems, previously known as the peripheral benzodiazepine receptor (PBR). Therefore, the effects of etifoxine are not completely reversed by the benzodiazepine antagonist flumazenil. Etifoxine is used for various emotional and bodily reactions followed by anxiety. It is contraindicated in situations such as shock, severely impaired liver or kidney function, and severe respiratory failure. The average dosage is 150 mg per day for no more than 12 weeks. The most common adverse effect is drowsiness at the initial stage. It does not usually cause any withdrawal syndromes. In conclusion, etifoxine shows less adverse effects of anterograde amnesia, sedation, impaired psychomotor performance, and withdrawal syndromes than those of benzodiazepines. It potentiates $GABA_A$ receptor-function by a direct allosteric effect and by an indirect mechanism involving the activation of TSPO. It seems promising that non-benzodiazepine anxiolytics including etifoxine will replenish shortcomings of benzodiazepines and selective serotonin reuptake inhibitors according to animated studies related to TSPO.

• 한국자원식물학회:학술대회논문집
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• 한국자원식물학회 2000년도 The 7th International Symposium
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• pp.116-122
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• 2000

The molecular modification of antiepileptic drugs and direct synthesis of new drugs with the predetermined antiepileptic properties are perspective. New neurochemical attacking to solve the problem including prevention and inhibition of seizures seems to be related to ginsenosides and ginseng polypeptides. The main study based on the severity of febrile convulsions of rat pups has been done from the earlier investigations of antiepileptical action of ginsenosides between KGTRI and MSU (Chepurnov, Park et al., 1995) with different kinds of experimental models of epilepsy. From the cultured cell line DAN25 of ginseng root, the extracts of ginsenosides made in "BIOKHIMMASH" were studied by the project of preclinical anticonvulsant screening (Stables, Kupferberg, 1997). The inhibition of severity of convulsions, decrease of seizures threshold, decrease of audiogenic seizures in rats of different strains and normalization of cerebral blood flow (measured by hydrogen test) were demonstrated in rats after i.c.v., intraperitoneally and orally administration, respectively. The antiepileptical effects by the combination of compounds from ginseng; were compared with the iuluence of Rg1, Rb1, Rc and with the well known antiepileptical drugs such as carbamazepine, valproic acid. The base for the research is obtained by using the WAG/Rij strain (Luijtelaar, Coenen, Kuznetcova), an excellent genetic model for human generalized absence epilepsy. The improving action of gensinosides was effectively demonstrated on the model of electrical kindling of amygdala of WAG/Rij rats with genetically determined absences, and the influences of ginsenosides on the slow wave discharges have also been being investigated. The different characteristics of a kindling process exerted in the sex-different region of the amygdala and demonstrated that the level of sex steroids and content of neurosteroids in amygdaloid tissue can modify the development of seizures. The chemical structures of ginsenosides not only have some principal differences from well-known antiepileptical drugs but the Plant Pharmacology gives us unique possibility to develop new class of antiepileptic drugs and to improve its biological activity.

• Applied Biological Chemistry
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• 제40권2호
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• pp.112-116
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• 1997

소의 뇌에서 neurosteroid의 지방산 에스터를 합성하는 neurosteroid acyltransferase(NSAT)의 뇌에서의 부위별, 세포분획별 분포 및 효소적 특성을 연구하였다. 소의 뇌 NSAT 활성도는 소뇌(小腦)에서 가장 높았으며 그 다음이 중뇌(中腦)이었다. 가장 활성도가 낮은 부위는 대뇌(大腦)로 소뇌(小腦)의 50% 수준이었다. 또한 소뇌 (小腦) microsome에서의 활성도가 다른 세포분획에 비해 매우 높아 NSAT가 microsomal 효소임을 알 수 있었다. NSAT의 최적온도는 $40^{\circ}C$이었으며, pH=4.9에서 최적 pH를 나타냈다. DHEA를 기질로 하였을 때 NSAT의 $K_m$과 $V_{max}$는 각각 $32.6\;{\mu}M$과 4.86 nmole/mg protein/h였다. 또한 DHEA를 기질로 하였을 때 pregnenolone $({\Delta}5P)$은 NSAT에 대하여 경쟁적 저해제로, testosterone은 비경쟁적 저해제로 작용하였다. ${\Delta}5P$와 testosterone의 Ki는 각각 $22.8\;{\mu}M$과 $28.2\;{\mu}M$이었다. 따라서 소의 NSAT는 C-3의 ${\beta}-hydroxyl$ 기와 C-17의 ${\beta}-hydroxyl$ 기를 에스터화하는 과정에서 다른 conformation을 가짐을 시사한다.

• 한국산학기술학회:학술대회논문집
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• 한국산학기술학회 2000년도 추계학술대회
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• pp.226-229
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• 2000

일반적으로 안경집은 일회적으로 사용하고 버리는 것이라 생각하는 사람이 많다. 안경집을 주로 생산하고 있는 대동사출금형과의 공동 노력으로 다기능성 안경집을 개발한 것을 소개한다. 일상적인 고정관념을 버리면 편리하고 기능성이 높은 제품을 만들 수 있다는 신념으로 개발한 결과 어린이나 젊은이들이 졸아할 문방구 겸용 안경집을 개발할 수 있었다. 완구는 소비자가 일상적으로 많이 접촉하기 때문에 곰팡이나 세균이 서식하지 않도록 항균 세라믹을 이용하여 항균처리하였다. 또한 상온에서 인체에 이로운 원적외선이 방출될 수 있도록 고안하였다. 단순한 색상의 무료함을 줄이기 위하여 어린이나 젊은이들이 좋아하는 상용화된 캐릭터를 사용하여 제품의 다양화를 꾀하였고, 4개의 조각으로 만들어 어린이들이나 젊은이들이 조립할 수 있도록 하여 흥미를 더할 수 있도록 하였다. 또한 소비자들이 선호하는 색을 알아보기 위하여 기존의 안경집을 활용하여 색상성호도 조사를 실시하였다. 젊은층은 자극적이고 화려한 색깔을 선호하는 한편 기성세대는 무난한 색깔을 선호하였다. 또한 콘택트 렌즈를 착용하는 경우에도 안경을 사용하는 경우가 많다. 이 경우 콘택트 렌즈와 안경을 따로 가지고 다녀야 하는 불편이 있다. 이에 착안하여 안경과 콘택트 렌즈를 겸용으로 사용하는 소비자를 위하여 안경과 콘택트 렌즈를 동시에 담을 수 있는 안경집을 개발(실용신안 출원번호:8928)하였다. 이 고안은 콘택트 렌즈를 안경집에 보관하기 위한 것으로 콘택트렌즈가 식염수에 잠겨 보관된 렌즈캡을 안경집내에 별도로 삽입되는 케이스에 수납하도록 구성하여 안경과 함께 콘택트 렌즈를 보관해 휴대하는 안경집 보관용 콘택트 렌즈 케이스에 관한 것으로 이것의 특징은 뚜껑이 열리고 닫히도록 구성된 안경집에 있어서 뚜껑 안쪽에 거울이 마련되고 뚜껑이 연결되는 선단부 안쪽에 끼움홈과 체결홈이 형성된 체결부를 갖는 안경집과 이것에 결합되는 체결구가 마련되어 개폐되는 커버가 형성된 케이스로 구성된다.로 금형설계 및 제작기간을 단축하고자 한다.ere demonstrated in rats after i.c.v., intraperitoneally and orally administration, respectively. The antiepileptical effects by the combination of compounds from ginseng; were compared with the iuluence of Rg1, Rb1, Rc and with the well known antiepileptical drugs such as carbamazepine, valproic acid. The base for the research is obtained by using the WAG/Rij strain (Luijtelaar, Coenen, Kuznetcova), an excellent genetic model for human generalized absence epilepsy. The improving action of gensinosides was effectively demonstrated on the model of electrical kindling of amygdala of WAG/Rij rats with genetically determined absences, and the influences of ginsenosides on the slow wave discharges have also been being investigated. The different characteristics of a kindling process exerted in the sex-different region of the amygdala and demonstrated that the level of sex steroids and content of neurosteroids in amygdaloid tissue ca