• Title/Summary/Keyword: $5-HT_6R$

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The Effect of Electroacupuncture at Sobu(HT8) on the EEG and HRV (소부(HT8) 전침이 뇌파(EEG)와 심박변이도(HRV)에 미치는 영향)

  • Yoon, Dae Shik;Hong, Seung-Won;Lee, Yong-Sub
    • Korean Journal of Acupuncture
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    • v.30 no.4
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    • pp.305-318
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    • 2013
  • Objectives : The aim of this study was to examine the effect of electroacupuncture(EA) at an acupoint, HT8(Sobu), on normal humans by using power spectral analysis. We examined the effect on the Heart Rate Variability(HRV), and the balance of the autonomic nervous system. Methods : Thirty-two healthy volunteers participated in this study. EEG(Electroencephalogram) power spectrum exhibits site-specific and state-related differences in specific frequency bands. A thirty-two channel EEG study was carried out on thirty-two subjects(14 males; mean age=23.5 years old, 18 females; mean age=21.5 years old). HRV and EEG were simultaneously recorded before and after acupuncture. Results : In the ${\alpha}$(alpha) band, during the HT8-acupoint treatment, the power values in the ${\alpha}$(alpha) band significantly decreased(p<0.05) at 28 channels. In the ${\beta}$(beta) band significantly decreased(p<0.05) at 26 channels. In ${\delta}$(delta) band significantly decreased(p<0.05) at 18 channels. In ${\theta}$(theta) band significantly decreased(p<0.05) at 20 channels. ${\alpha}/{\beta}$ values were increased at 6 channels and decreased at 10 channels.${\beta}/{\theta}$ values were increased at 10 channels and decreased at 19 channels. Mean-RR(RR-interval), Complexity, RMSSD(Root mean square of successive differences), SDSD(Standard deviations differences between adjacent normal R-R intervals), norm HF showed a significantly increased and mean-HRV, norm LF, LHR(LF/HF Ratio) showed a significantly decreased after HT8-acupoint treatment(p<0.05). Conclusions : These results suggest that EA at the HT8 mostly causes significant changes on alpha(28 channels), beta(26 channels), delta(18 channels), theta(20 channels) bands and mean-HRV, mean-RR, complexity, RMSSD, SDSD, norm LF, norm HF and LHR. If practicing EA at the HT8, it will regulate the function of the cerebral cortex, decrease activity of the sympathetic and increase parasympathetic nervous activity.

Roles of Monoamine Neurotransmitters in Regulation of Hypothalamic PITUITITARY-ADRENAL AXIS(HPA) (III) - Role of 5-hydroxytryptamine in Controlling the Stress-Induced Elevation of Corticosterone in Rat - (시상하부-뇌하수체-부신계 조절에 대한 Monoamine 신경전달물질의 역할에 관한 연구(III)-뇌 5-hydroxytyptamine(Serotonin)이 Stress 시 Corticosteroid 변동에 미치는 영향)

  • Suh, Yoo-Hun;Lim, Jung-Kyoo;Park, Chan-Woong
    • The Korean Journal of Pharmacology
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    • v.19 no.2
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    • pp.45-55
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    • 1983
  • A role for brain serotonin(5-HT) in regulation of the HPA axis has been suggested but remains contoversial and poorly defined. The present experiments were designed to check kinetic parameters of 5-HT turnover in rat hypothalamus and remainder brain areas before and after stress and to test whether using various different pharmacologic approaches to stimulate or eliminate the control serotonergic system have any consistent effect on the stress-induced activation of HPA system. Steady state brain serotonin and 5-HIAA concentrations during 1 min ether stress were significantly elevated without significant rise in the levels of plasma corticosterone, which highly increased 2 minutes after stress. This suggests that the increase in serotonergic neuron activity precede that in HPA activity. Furthermore, during 1 ruin-ether stress or 30 min immobilization stress there is a marked increase in hypothalamic and remainder brain serotonin (5-HT) turnover or synthesis rates assessed by both the pargline/5-HT method and pargyline/5-HIAA method. The stress-induced corticosterone levels were increased by serotonin precursors and serotonin agonist in a dose-related fashion. The stress- induced corticosterone levels were highly elevated by L-tryptophan (100 mg/kg) and Potentiated by monoamine oxidase inhibitor, pargyline or serotonin agonist, 5-MeoDMT. The stress-induced elevation of corticosterone and 5-HT levels in rat brain were not significantly decreased by the administration of 5-HT synthesis inhibitor, PCPA and 5-HT neurotoxin, 5,7-DHT. However, the stress-induced elevation of corticosterone and 5-HT levels were decreased by the destruction of midline raphe nuclei. There was a strong positive correlation between plasma corticosterone and 5-HT concentrations changed by drugs which mainly manipulating 5-HT system in the hyhothalamus and in the remainder of the brain. In conclusion, our present data stongly suggest that 5-HT is an important key neurotransmitter involved in the stress-induced activation of the HPA system.

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Chemical Modification of Alisol B 23-acetate and Their Cytotoxic Activity

  • Lee, Sang-Myung;Min, Byung-Sun;Bae, Ki-Hwan
    • Archives of Pharmacal Research
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    • v.25 no.5
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    • pp.608-612
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    • 2002
  • The twelve-protostane analogues were synthesized from alisol B 23-acetate and assessed for their in vitro antitumor activity against six different human and murine tumor cell lines. Of the compounds synthesized, 23S-acetoxy-24R(25)-epoxy-11$\beta$,23S-dihydroxyprotost-13(17)-en-3-hy-droxyimine (12) exhibited significant cytotoxic activities against A549, SK-OV3, B16-F10, and HT1080 tumor cells with $ED_{50}/$ values of 10.0, 8.7 ,5.2, and 3.1 ${\mu}g$/ml, respectively. Furthermore, 23S-acetoxy-13(17),24R(25)-diepoxy-11$\beta$-hydroxyprotost-3-one (5), 13(17),24R(25)-diepoxy-11$\beta$, 23S-dihydroxyprotostan-3-one (6), 24R,25-epoxy-11$\beta$,23S-dihydroxyprotost-13(17)-en-3-one (7), and 11$\beta$,23S,24R,25-tetrahydroxyprotost-13(17)-en-3-one (9) showed moderate cytotoxic activities against 816-F10 and HT1080 tumor cells. These results mean that a hydroxyimino group at C-3 position in the protostane-type terpene enhances cytotoxic activity.

Expression of Serotonin(5-HT) Receptor Isotypes in Reproductive Organs of Male Rat (수컷 흰쥐 생식기관에서의 세로토닌 수용체 아형 유전자 발현)

  • 이성호
    • Development and Reproduction
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    • v.6 no.2
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    • pp.111-115
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    • 2002
  • 5-Hydroxytryptamine(5-HT; serotonin) system has been implicated in the modulation of male sexual behaviors and the secretion of reproductive hormones. In human males, selective serotonin re-uptake inhibitors(SSRIs) are known to improve the major male sexual dysfunction, premature ejaculation, through the central nervous system-mediated pathways. As numerous hormone and local factors, 5-HT may have peripheral role in the regulation of male sexual function. The expression of 5-HT receptor subtypes in the target tissue, however, has not been explored yet. The present study was undertaken to test whether the 5-HT receptor subtypes are expressed in the reproductive tissues of male rat, especially in ejaculatory machinery such as seminal vesicle and vas deferens. To do this, reverse transcription-polymerase chain reaction(RT-PCR) and Southern blot analysis were employed. The transcripts for the 1A, 1B and 2C subtypes of 5-HT receptor were amplified in all the tested tissues. The present study demonstrated the expression of 5-HT receptor in the rat ejaculatory machinery, suggesting that 5-HT may play a pivotal role in the male sexual function via not only central pathway but also peripheral route. Further study on the receptor subtype-specific effect and their harmonized mode of action will be needed to establish the understanding of ejaculation mechanism and drug design.

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Antioxidant and Anti-Proliferative Activities of Rubus Fruits in Korea (국내산 나무딸기류 과일의 항산화 및 암세포 항증식 활성)

  • Jung, Hana;Lee, Hee Jae;Cho, Hyunnho;Hwang, Keum Taek
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.41 no.12
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    • pp.1649-1655
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    • 2012
  • This study was conducted to determine the polyphenols, flavonoids and antioxidant activity (FRAP) of the extracts (crushed by hand or a homogenizer) of Rubus fruits (blackberry, Korean raspberry, black raspberry, boysenberry and golden raspberry) produced in Korea. In addition, their nitric oxide (NO) scavenging activity in RAW 264.7 cells and anti-proliferative activity in HT-29 and KATO-3 cells were investigated. Polyphenol and flavonoid contents in the Rubus fruits ranged from 0.6 to 8.9 and from 0.1 to 7.9 mg/g fresh fruit, respectively. Black raspberry had the highest polyphenol and flavonoid contents among the Rubus fruits. The homogenized extracts of blackberry, Korean raspberry and golden raspberry fruits showed significantly higher polyphenol and FRAP values than the hand-crushed extracts. FRAP values of the Rubus fruit extracts were significantly correlated with their polyphenol (R=0.995) and flavonoid (R=0.967) contents. The Rubus fruit extracts suppressed the NO secretions in LPS-treated RAW264.7 cells. There were no significant differences between extracts obtained by crushing by hand and those obtained using a homogenizer. Proliferation rates of HT-29 and KATO-3 cancer cells treated with the Rubus fruit extracts at 0.1, 0.25 and 0.5 mg/mL were reduced by 3~32% and 0~57%, respectively. The homogenized extracts of blackberry and Korean raspberry fruits had significantly higher anti-proliferation activity against HT-29 cancer cells than the hand-crushed extracts. However, extraction method did not show any significant difference on proliferation of KATO-3 cancer cells. The NO scavenging activity of the Rubus fruit extracts were significantly correlated with the anti-proliferation activities of the HT-29 (R=0.602) and KATO-3 cells (R=0.498).

Detection of Dopamine and Serotonin by Competitive Enzyme-Linked Immunosorbent Assay (경쟁적 ELISA를 이용한 도파민과 세로토닌의 검출)

  • Namkung, Su Min;Choi, Jeong Su;Park, Ji Hyang;Yang, Man Gil;Lee, Min Woo;Kim, Suhng Wook
    • Korean Journal of Clinical Laboratory Science
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    • v.49 no.3
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    • pp.220-226
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    • 2017
  • Dopamine (DA) and serotonin (5-Hydroxytryptamine, 5-HT) are neurotransmitters and hormones that exist in small amounts but have important role in the body. Serum and 24-hour urine are used as specimens, and are usually examined by HPLC-MS. In this study, we tried to detect DA and 5-HT by competitive ELISA using antigen-antibody (Ab) reaction. After immobilizing $5{\mu}g/mL$ BSA conjugate on a 96-well surface, hormone and primary Ab, which are respectively diluted to different concentrations, were treated. Then, HRP-conjugated secondary Ab and TMB were added to measure absorbance. The regression equation and $R^2$ value were calculated based on absorbance, and sensitivity of Ab to hormone as well as the correlation between hormone concentration and absorbance were determined. In DA ELISA, $R^2$, the correlation between the concentration of hormone and absorbance, was the highest by 0.91 when anti-dopamine Ab was diluted 6,000 times and 7,000 times. In 5-HT ELISA, $R^2$ was bigger than 0.90 in every concentration except 3,000 times and 6,000 times. Both DA and 5-HT were not effectively detected at low concentrations (less than $1.0{\times}10^{-7}M$); and because reference value of serum DA is lower than this, HPLC-MS was required to detect serum DA. However, competitive ELISA may be effective in detecting 24-hour urine DA, serum, and 24-hour 5-HT. Further studies are needed to detect hormones more accurately at lower concentrations.

Development of fishing gear and fishery operation system for the croaker drift gill net 2. Performance tests of labor saving type model net hauler (조기유자망 어구의 개량 및 생력화 조업시스템 개발 2. 생력형 모형 양망기의 성능 시험)

  • Kim, Suk-Jong;Koo, Myung-Sung
    • Journal of the Korean Society of Fisheries and Ocean Technology
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    • v.41 no.3
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    • pp.199-206
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    • 2005
  • As the basic study about improvement of yellow croaker drift gill net fishing implement and development of the fishing system, this study drew problem after synthetically analyzing hauling system of yellow croaker drift gill net used in the coast of Chuja Island and tested several characters and analyzed in hauling process with 5 step net hauler model for improving the problem. The analysis results are as follows. When the angle between axises of drum centers was small, it showed the tendency that hauling time was fast. Hauling time was faster when drum was 5 step rather than 3 step. When drum was 5 step, slippery phenomenon was small and hauling was stable. Tension was larger when drum was 5 step rather than 3 step. When drum was 5 step, the range of change of the maximum and minimum value was small and hauling was stable. When drum was 3 step, there was following formula between hauling time ($Ht_3$) and angle between axises of drum centers ($A_g$) $Ht_3$ : ($7.15Hs^{-0.81}$) $A_g^{-0.81}$, when drum was 5 step there was following formula.$Ht_5$ : ($6.45Hs^{-0.75}$) $A_g0.10$, here, Hs is hauling speed. When drum was 3 step and hauling speed was 28cm/sec, tension was $T=0.08A_8^3-1.60A_g^3-0.49A_g+369.56(r=0.99)$, when drum was 5 step, tension was, $T=-0.01A_g^3+1.96A_g^2-34.05A_g+414.58$ (r-0.99), here, T was tension(g).

Angled Capillary Method for Determining Erythrocyte Sedimentation Rate of Goat (경사모세관법(傾斜毛細管法)에 의한 산양혈액(山羊血液)의 적혈구침강율(赤血球沈降率) 측정(測定))

  • Shin, Sung-shik;Lee, Bang-whan;Shin, Jong-uk
    • Korean Journal of Veterinary Research
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    • v.26 no.1
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    • pp.187-194
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    • 1986
  • The purpose of this study is to develop a new method which enables the goat ESR to be used as an effective clinical test. Blood samples were taken from 61 Korean native goats aged above one year old and the effect of tube inclinations, tube bores, tube lengths, environmental temperatures during tests and packed erythrocyte volumes (PCV) on the ESR were observed. The results were summarized as follows. 1. The ESR/hr using capillary hematocrit tube (Micro-Ht-tube) was gradually increased as the tube angle inclined from 90 (vertical) to 15 degrees and the best angle in view of both security and fast sedimentation rate was found to be an angle of 45 degrees. 2. The 45-degree angled ESR ($45^{\circ}$-ESR) increased as the diameter of tube bore decreased. 3. The tube length did not affect the $45^{\circ}$-ESR in percent. 4. The $45^{\circ}$-ESR increased with the increased environmental temperature during the ESR test. 5. The heparinized Micro-Ht tubes did not affect the $45^{\circ}$-ESR of EDTA-blood in healthy group but in anemic group. In the anemic group, the ESRs by the heparinized Micro-Ht-tubes were slightly higher than those by non-heparinized Micro-Ht-tubes. 6. By using the autologous plasma, PCV of the blood was adjusted to be 10, 20, 30, 40 and 50ml/100ml and $45^{\circ}$-ESRs were determined in the Micro-Ht-tubes. The $45^{\circ}$-ESRs increased as the values of PCV decreased. The regression of the $45^{\circ}ESR$ to PCV was curvilinear with the second degree polynomial, $Y=42.1838-1.7355X+0.0180X^2$(r=0.9997). 7. The $45^{\circ}$-ESR/hr, using non-heparinized Micro-Ht-tubes at $20^{\circ}C$, was determined in 35 healthy Korean native goats. The average PCV was $30.6{\pm}1.4ml/100ml$. The observed ESR values averaged $6.8{\pm}1.7%$ and the corrected ESR values to the standard PCV of 31ml/100ml averaged $6.5{\pm}1.2%$. From these results, the angled capillary tube method was found to be desirable ESR test of goat blood in which EDTA-blood is filled in nonheparinized Micro-Ht-tubes held at an angle of 45 degrees for an hour at $20^{\circ}C$.

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Neuroprotective Compounds Isolated from Lysimachia christinae

  • Gahee Ryu;Choong Je Ma
    • Natural Product Sciences
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    • v.29 no.1
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    • pp.10-16
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    • 2023
  • We previously reported that dried Lysimachia christinae whole plant extract exerted significant neuroprotective activity. In this study, we tried to isolate neuroprotective compounds of L. christinae. We evaluated the neuroprotective activity of the four fractions (hexane, chloroform, ethyl acetate, and n-butanol fractions) of methanol extract. Among them, ethyl acetate and n-butanol fractions showed most potent neuroprotective activity against glutamate excitotoxicity. Nine compounds were isolated from ethyl acetate and n-butanol fractions of L. christinae extract and identified as cynaroside (1), (3,4,5,6-tetrahydroxytetrahydro-2H-pyran-2-yl)methyl-3-hydroxy-2-octyldopentaconta-23,33-dienoate (2), androst-16-ene-3,6-diol (3), 2-hydroxy-24-propoxytetracos-4-enoic acid (4), 2-hydroxy-24-methoxytetracos-4-enoic acid (5), 12-(stearoyloxy)octadec-9-enoic acid (6), β-sitosterol (7), (E)-4-(3,4-dimethoxyphenyl)but-3-en-1-yl palmitate (8) and (1S,2S,3R,4R)-4-(((2S,3R,4R,5R,6S)-2-(((2R,3R,4S,5R,6R)-2-(3,4-dimethoxyphenethoxy)-3,5-dihydroxy-6-(hydroxymethyl) tetrahydro-2H-pyran-4-yl)oxy)-4,5-dihydroxy-6-methyltetrahydro-2H-pyran-3-yl)oxy)cyclohexane-1,2,3-triol (9) by spectroscopic data such as UV, IR, NMR, Mass spectroscopy. Their neuroprotective activity was evaluated by MTT assay. Cynaroside (1) and androst-16-ene-3,6-diol (3) had significant neuroprotective activity against glutamate-injured HT22 cells. The neuroprotective efficacy of cynaroside (1) and androst-16-ene-3,6-diol (3) was related to their anti-oxidative activity.

Determination of Novel Synthetic 5HT2C Agonist KOPC20010 by Gas-Chromatography/Mass Spectrometry and its Bioavailability in Sprague-Dawley Rats

  • Im, Hye-Yeon;Pae, Ae-Nim;Yang, Ha-Yun;Park, Woo-Kyu;Seo, Ji-Eun;Haque, Md. Mamunul;Kwon, Oh-Seung
    • Journal of Pharmaceutical Investigation
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    • v.41 no.1
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    • pp.31-36
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    • 2011
  • $5HT_{2C}$ receptor among fourteen 5-HT subtypes plays important roles in several disorders such as depression, anxiety, epilepsy, schizophrenia and sleep disorders. The purpose of the study is to investigate pharmacokinetic parameters and bioavailability of a newly synthesized selective agonist of $5-HT_{2C}$ receptor, KOPC-20010 (KP10) in rats after intravenous and oral administration for the development of therapeutic anti-obesity agents. KP10 was administered orally (40 mg/kg) or intravenously (20 mg/kg), blood was collected via a catheter, and analyzed by GC/MSD. The calibration curve of KP10 in plasma and urine showed high linearity ($r^2$ >0.999). The retention times of KP10 in plasma and urine were 8.7 and 9.7 min, respectively. After oral administration of 40 mg/kg, pharmacokinetic parameters were calculated as follows; $C_{max}$ value was $1242.9{\pm}1195.5$ ng/mL at $1.1{\pm}0.6$ hr ($T_{max}$). $AUC_{0->24hr}$ and $AUC_{0>{\infty}}$ were $8034.2{\pm}960.7$ and $10464.1{\pm}681.5\;ng{\cdot}hr/mL$, respectively. The terminal half-life was $21.9{\pm}7.6$ hr. $AUC_{0->24hr}$ and $AUC_{0>{\infty}}$ were $4292.4{\pm}523.0$ and $6111.2{\pm}756.2\;ng{\cdot}hr/mL$, respectively, after 20 mg/kg of intravenous administration. The terminal half-life after intravenous administration was $25.1{\pm}9.4$ hr. Bioavailability of KP10 was determined to 86%. The excretion amount into the urine within 48 hr was approximately 4.7 to 6.7% of the dose administered. These data may be beneficial to the anti-obesity drug development of KP10.