• Biomolecules & Therapeutics
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• 제4권1호
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• pp.7-18
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• 1996

5-Hydroxytryptamine(5-HT, serotonin), when given into the vein, produced antidiuretic action accompanied with reduction of glomerular filtration(GFR), renal plasma flow(RPF), osmolar clearance(Cosm) and amounts of sodium or potassium excreted in urine( $E_{Na}$ , $E_{K}$), with the augmented reabsorption rates of sodium and potassium in renal tubules. 5-HT, when infused into a renal artery, exhibited diuretic action accompanied with the augmented RPF and increased $E_{Na}$ and $E_{K}$ in only infused kidney. Antidiuretic action of 5-HT infused into the vein was not influenced by ketanserin, 5-H $T_2$receptor blockade, given into a renal artery, vein or carotid artery, by methysergide, 5-H $T_1$receptor blockade, given into a renal artery, whereas above antidiuretic action was inhibited by methysergide given into vein or carotid artery. Diuretic action of 5-HT infused into a renal artery in only experimental kidney was blocked by ketanserin injected into a renal artery, was not influenced by methysergide administered into a renal artery. Above results suggest that 5-hydroxytryptamine(5-HT) produced the antidiuretic action through central 5-H $T_1$receptor and the diuretic action through 5-H $T_2$receptor located in renal tubules of kidney.ney.

• 통합자연과학논문집
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• 제11권2호
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• pp.87-92
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• 2018

5-Hydroxytryptamine receptor 7 ($5-HT_7R$) is one of G-Protein coupled receptors, which is found to be involved in the pathophysiology of various neurological disorders including depression, sleep disorders, memory deficiency and neuropathic pain. After activation of $5-HT_7R$ by serotonin, it activates the production of the intracellular signaling molecule cyclic AMP. The availability of 3D structure of the receptor would enhance the development of new drugs. Hence, in the present study, homology modelling of human 5-hydroxytryptamine receptor 7 ($5-HT_7R$) was performed using comparative modelling (Easy Modeller) and threading (I-TASSER) approaches. The generated models were validated using Ramachandran plot and ERRAT plot and the best models were selected based on the validation results. The 3D model developed here could be useful for identifying crucial residues and further docking study.

• 통합자연과학논문집
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• 제9권2호
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• pp.128-135
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• 2016

5-hydroxytryptamine (serotonin) receptor ($5-HT_7R$) 7 is one of G-Protein coupled receptors, which is activated by the neurotransmitter Serotonin. After activation by serotonin, $5-HT_7$ activates the production of the intracellular signaling molecule cyclic AMP. $5-HT_7$ receptor has been found to be involved in the pathophysiology of various disorders. It is reported that $5-HT_7$ receptor antagonists can be used as antidepressant agents. In this study, we report the important structural and chemical parameters for 2-methoxyphenylpiperazinylakanamides as $5-HT_7R$ inhibitors. A 3D QSAR study based on comparative molecular field analysis (CoMFA) was performed. The best predictions were obtained for the best CoMFA model with $q^2$ of 0.594 with 6 components, $r^2$ of 0.986, Fisher value as 60.607, and an estimated standard error of 0.043. The predictive ability of the test set was 0.602. Results obtained the CoMFA models suggest that the data are well fitted and have high predictive ability. The contour maps are generated and studied. The contour analyses may serve as tool in the future for designing of novel and more potent $5-HT_7R$ derivatives.

• Biomolecules & Therapeutics
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• 제1권1호
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• pp.77-83
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• 1993

Serotonin (5-hydroxytryptamine, 5-HT) has been known to have peripheral actions as well as central actions. Recently physiological roles of 5-HT as a central neurotransmitter have been studied in detail and this is a subject of the present study. Plausible central actions mediated by 5-HT receptor seem to be a control of appetite, bring about psychiatric disorders such as anxiety or dementia, and migraine headache. In this study, thirty-five medicinal plants were tested for their antagonistic activities to 5-HT mediated actions. Through the preliminary screening, methanol extracts of three medicinal plants (Saussureae Radix, Sanguisorbae Radix and Xanthii Fructus) were shown to possess relatively specific antagonistic activities to 5-HT mediated ileal contraction over acetylcholine. To luther investigate the central antagonistic activities of the selected plant in vivo, m-chlorophenylpiperazine (mCPP) which is known to be a 5-H $T_{1c}$ receptor agonist was injected to mouse to induce an anxious and/or hypolocomotion states, and also social interaction test, which was based on the method described by File (S.E. File, 1980), was performed to see whether ethylacetate fraction of Sanguisorbae Radix methanol extract possessed a specific anxiolytic activity.y.

• 생물정신의학
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• 제4권2호
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• pp.162-167
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• 1997

There is no doubt that dopamine plays a critical role in the etiopathogenesis of schizophrenia. However, there appeared some limitations in explaining the complex phenomena of schizophrenia. Recent research data suggest that dysfunction in serotonergic system may be involved. Before the dopamine hypothesis of schizophrenia became established, the interest in serotonin(5-hydroxytryptamine, 5-HT) as an etiological substrate of this illness occurred. Recently the importance and extent of 5-HT's involvement in the pathophysiology and mechanism of action of antipsychotic drug is actively investigated. In recent years, therapeutic success of clozapine and risperidones has increased attention on the interaction between the 5-HT and dopamine systems in schizophrenia. This led to the concept of serotonin-dopamine antagonist for antipsychotics. The authors review the evidence for the role of 5- HT in schizophrenia and serotonin-dopamine interaction.

• 약학회지
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• 제35권4호
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• pp.326-331
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• 1991

Brain serotonin and its utilization was investigated on stressed rats after feeding high tryptophan diet for a month. High tryptophan fed rats displayed significantly higher level of serum tryptophan, brain tryptophan, serotonin (5-hydroxytryptamine; 5-HT) and 5-hydroxyindoleacetic acid (5-HIAA) than the control diet fed rats. When rats were treated with 3 hour immobilization (IMMB) stress, serotonin turnover was slightly increased, but not statistically significant, in control diet group rats. However in high tryptophan diet rats, 3 hr IMMB stress resulted in statistically significantly (p<0.05) decreased the serum tryptophan, brain tryptophan and 5-HT level. The concentration of 5-HIAA was significantly increased indicating accelerated utilization of the brain 5-HT of the high trp. fed rat. The utilization pattern of the serotonin was found to be similar among young and adult rats. Rats on a tryptophan enriched diet displayed higher coping ability to the stress as they exhibited smaller increment of corticosterone level. A possble involvement of opioid system was suggested in serotonin utilization by measuring total $^{3}$[H]-naloxone binding in brain.

• Applied Microscopy
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• 제20권1호
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• pp.17-35
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• 1990

Effect of 5-hydroxytryptamine(5-HT, serotonin) and its precursor tryptophan on the cell proliferation of brain and somite parts of 4 day chick embryo in Dulbeco's modified essential medium was examined morphologically at cellular level. It was realized that the externally added 5-HT and/or tryptophan disturbed cell proliferation and severve necrosis occured. Electron micrograph showed that the development of cell organelles were greatly impaired. The activities of both acetylcholine esterase and $Mg^{2+}$ -dependent ATPase of the brain tissues of 5 day chick embryo, which received 1mg of tryptophan and/or 0.1mg of 5-HT at primitive streak stage after 24 hrs incubation of the fertilized egg, were much lower(about 20-25%) than those of control group. These results were supported by the electron micrographs of chemically treated cells. Control cells showed clear densed bands of acetylcholine esterase activity around nucleus and rough endoplasmic reticulum but tryptophan or 5-HT treated groups showed discontinued activity bands. In the case of $Mg^{2+}$-ATPase, the control groups showed clear continuous activity bands but tryptophan and/or 5-HT treated groups were discontinuous. From the previous and present studies, it seems that the intracelluar 5-HT level is very important for the cell proliferation and normal morphogenesis.

• 한국발생생물학회지:발생과생식
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• 제13권4호
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• pp.341-351
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• 2009

대하, Fenneropenaeus chinensis의 난소 성숙에 대한 serotonin(5-hydroxytryptamine, 5-HT), ecdysone(20-hydroxyecdysone, 20-E) 그리고 HCG(human chorionic gonadotropin)의 효과를 조사하였다. 대하에 5-HT(체중 g당 $5{\mu}g,\;20{\mu}g$), 20-E(체중g당 $5{\mu}g,\;10{\mu}g,\;20{\mu}g$) 그리고 HCG(체중 g당 5 IU, 10 IU)를 5일 간격으로 3회 주사한 후 10일이 더 지난 시점에 채집하여 성 성숙도지수(GSI)의 변화와 난소의 조직학적 변화를 조사하였다. 호르몬제의 효과를 비교하기 위해 멸균한 생리식염 수만을 주사한 대조구와 아무 것도 처리하지 않은 무처리구를 설정하였다. 20-E와 HCG를 처리한 실험구에서는 난소 성숙 효과가 전혀 나타나지 않았으나, 이른 봄에 5-HT를 체중 g당 $20{\mu}g$로 처리한 실험구에서는 유의한 난소 성숙효과를 보였다. 본 실험 결과에서 대하에 5-HT를 체중 g당 $20{\mu}g$ 이상 처리하면 난소성숙을 유도할 수 있다는 것을 보여주었으며, 이는 대하의 종묘 생산에 유용하게 사용될 수 있을 것이다.

• 한국발생생물학회지:발생과생식
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• 제5권1호
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• pp.9-16
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• 2001

Biogenic amine 류에는 catecholamine, indoleamine 그리고 histamine이 있으며, 동물의 다양한 생리 현상과 행동양식 조절에 중요한 역할을 담당한다. 이중 indoleamine 류인 세로토닌(serotonin혹은 5-hydroxytryptamine, 5-HT)의 경우 최근 들어 그 수용체 아형의 유전자 규명과 발현 조절, 중추신경계 및 표적 기관에서의 역할, 특히 항우울 효과와 같이 행동 및 심리적인 영향 등에 대해 광범위하게 연구되고 있다. 본 논문은 5-HT의 합성 경로, 수용체 아형, 생식과 관련된 기능에 대해 서술하였다. 특히 생식과 관련된 5-HT의 신경내분비학적인 역할로 GnRH-LH-sex steroids 축 조절 기능과 이에 관여하는 수용체 아형들, 생식 조절에 있어서 5-HT 효과의 성적 이형 양상, 중추신경계 이외 기관에서의 역할, 성행동의 조절에 대한 연구 결과들을 요약하였다. 5-HT의 기능에 대한 연구는 특히 현재 주목 받고 있는 '삶의 질' 고양과 밀접하게 연관되어있는 유망한 주제 가운데 하나로 판단된다.

• 한국생물물리학회:학술대회논문집
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• 한국생물물리학회 2003년도 정기총회 및 학술발표회
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• pp.59-59
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• 2003

Serotonin (5-HT; 5-hydroxytryptamine) exerts multiple effects on central nervous system as well as behaviors such as mood and appetite. The signaling of serotonin is mediated by 7 families of serotonin receptors, designated 5-HT$_1$ to 5-HT$_{7}$. Six families of this receptor are G-protein coupled 7TM receptors, and the third intracellular loop of these receptors is proposed to interact with specific types of G-proteins. To investigate the specific interaction between the third intracellular loop of 5-HT$_{6}$ with G$\square$s, we have constructed a chimera protein that represent the third intracellular loop of 5-HT$_{6}$ within a leucine zipper motifs, In addition an alpha subunit of human G-protein that interact with 5-HT$_{6}$ was cloned into a bacterial expression vector. The two proteins were expressed in E. coli and purified in homogeneity. The interaction of the prepared proteins was examined by ELISA assay. The affinity between the two proteins and effect of insertion mutations were discussed.ussed.d.