• Title/Summary/Keyword: noradrenaline (NA)

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NMR Spectroscopic Analysis on the Chiral Recognition of Noradrenaline by β-Cyclodextrin ( β-CD) and Carboxymethyl- β-cyclodextrin (CM- β-CD)

  • Lee, Sang-Hoo;Yi, Dong-Heui;Jung, Seung-Ho
    • Bulletin of the Korean Chemical Society
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    • v.25 no.2
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    • pp.216-220
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    • 2004
  • ${\beta}$-CD and CM- ${\beta}$-CD as chiral NMR shift agents were used to resolve the enantiomers of noradrenaline (NA). The stoichiometry of each complex formed between the CDs and the enantiomers of NA was found to be 1 : 1 through the continuous variation plots. The binding constants (K) of the complexes were determined from $^1H$ NMR titration curves. This result indicated that both ${\beta}$-CD and CM- ${\beta}$-CD formed the complexes with the S(+)-NA more preferentially than its R(-)-enantiomer. The K values for the complexes with ${\beta}$-CD ($K_{S(+)}$ = 537 $M^{-1}$ and $K_{R(-)}$ = 516 $M^{-1}$ was larger than those with CM- ${\beta}$-CD ($K_{S(+)}$ = 435 $M^{-1}$ and $K_{R(-)}$ = 313 $M^{-1}$), however, enantioselectivity (${\alpha}$) of S(+)- and R(-)-NA to CM- ${\beta}$-CD ( ${\alpha}$ = 1.38) was larger than that to ${\beta}$-CD ( ${\alpha}$ = 1.04), indicating that CM- ${\beta}$-CD was the better chiral NMR solvating agents for the recognition of the enantiomers of NA. Two dimensional rotating frame nuclear Overhauser enhancement spectroscopy (ROESY) experiments were also performed to explain the binding properties in terms of spatial fitting of the NA molecule into the macrocyclic cavities.

Effects of Noradrenaline on the Membrane Potential of Prostatic Neuroendocrine Cells of Rat

  • Kim, Jun-Hee;Shin, Sun-Young;Uhm, Dae-Yong;Kim, Sung-Joon
    • The Korean Journal of Physiology and Pharmacology
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    • v.7 no.1
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    • pp.47-52
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    • 2003
  • The prostate gland contains numerous neuroendocrine cells that are believed to influence the function of the prostate gland. Our recent study demonstrated the expression of both ${\alpha}1$- and ${\alpha}2$-ARs, signaling the release of stored $Ca^{2+}$ and the inhibition of N-type $Ca^{2+}$ channels, respectively, in rat prostate neuroendocrine cells (RPNECs). In this study, the effects of NA on the resting membrane potential (RMP) of RPNECs were investigated using a whole-cell patch clamp method. Fresh RPNECs were dissociated from the ventral lobe of rat prostate and identified from its characteristic shape; round or oval shape with dark cytoplasm. Under zero-current clamp conditions with KCl pipette solution, the resting membrane potential (RMP) of RPNECs was between -35 mV and -85 mV. In those RPNECs with relatively hyperpolarized RMP (<-60 mV), the application of noradrenaline (NA, $1{\mu}M$) depolarized the membrane to around -40 mV. In contrast, the RPNECs with relatively depolarized RMP (>-45 mV) showed a transient hyperpolarization and subsequent fluctuation at around -40 mV on application of NA. Under voltage clamp conditions (holding voltage, -40 mV) with CsCl pipette solution, NA evoked a slight inward current (<-20 pA). NA induced a sharp increase of cytosolic $Ca^{2+}$ concentration ($[Ca^{2+}]_c$), measured by the fura-2 fluorescence, and the voltage clamp study showed the presence of charybdotoxin-sensitive $Ca^{2+}$-activated $K^+$ currents. In summary, adrenergic stimulation induced either depolarization or hyperpolarization of RPNECs, depending on the initial level of RMP. The inward current evoked by NA and the $Ca^{2+}$-activated $K^+$ current might partly explain the depolarization and hyperpolarization, respectively.

Effects of Rose Fruit Extract Drinks on Sociopsychological Stress (사회.심리적 스트레스에 미치는 장미 추출 음료의 영향)

  • 최진호;김대익;박수현;김동우;조원기;유병팔
    • Journal of Life Science
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    • v.9 no.5
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    • pp.612-619
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    • 1999
  • The effects of anti-stress rose fruit (ASRF) extract drink (ASRF-0.1% and ASRF-0.5% concentrations) were tested for the anti-stress action. ICR male mice (20$\pm$2 g) were fed with basic experimental diets and given free access to water containing these ingredients for 18 days. Psychological stress/sociopsychological stress exposed by foot-shock for 1 hour for 3 days. Both ASRF-0.1 and ASRF-0.5 groups in the sociopsychological stress resulted in a significant decrease of 24.3% and 38.0% in plasma corticosterone (CS) secretion compared with psychological stress (control group). Noradrenaline (NA) secretion in the brain were significantly increased 35.9% in ASRF-0.5 group, but NA secretion in ASRF-0.1 group could not be obtained significant result compared with control group. MHPG-SO4 (3-Methoxy-4-hydroxy-phenylethy leneglycol sulfate) levels in the brain resulted in a marked decreases of 16.5% and 18.9% respectively in ASRF-0.1 and ASRF-0.5 groups. NA/MHPG-SO4 ratios in the brain of ASRF-0.1 and ASRF-0.5 groups resulted in a significantly increase of 16.5% and 67.0%, respectively, compared with control group. These results suggest that anti-stress rose fruit (ASRF) drink also can effectively ridded the sociopsychological stress.

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Effects of Chrysanthemum Extract Drinks on Sociopsychological Stress (사회.심리적 스트레스에 미치는 국화 추출 음료의 영향)

  • 최진호;김대익;박수현;김동우;조원기;유병팔
    • Journal of Life Science
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    • v.9 no.5
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    • pp.604-611
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    • 1999
  • The effects of anti-stress chrysanthemum flower (ASCF) extract drink (ASCF-0.1% and ASCF-0.5% concentrations) were tested for the anti-stress action. ICR male mice (20$\pm$2 g) were fed with basic experimental diets and given free access to water containing these ingredients for 18 days. Psychological stress/sociopsychologcal stress exposed by foot-shock for 1 hour for 3 days. Both ASCF-0.1 and ASCF-0.5 groups in the sociopsychological stress resulted in a significant decrease of 28.1% and 27.3% in plasma corticosterone (CS) secretion compared with psychological stress (control group). Noradrenaline (NA) secretions in the brain were significantly increased 49.7% and 53.9%, respectively, in ASCF-0.1 and ASCF-0.5 groups compared with control group. MHPG-SO4 (3-Methoxy-4-hydroxyphenylethy-leneglycol sulfate) levels in the brain resulted in a marked decreases of 12.9% and 16.6%, respectively in ASCF-0.1 and ASCF-0.5 groups. NA/MHPG-SO4 ratios in the brain of ASCF-0.1 and ASCF-0.5 groups resulted in a significantly increase of 71.3% and 81.0%, respectively, compared with control group. These results suggest that anti-stress chrysanthemum flower (ASCF) drink can effectively ridded the sociopsychological stress.

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Effects of Mind Tonic Drinks on Sociopsychological Stress (사회.심리적 스트레스에 미치는 마인드 토닉(Mind Tonic) 음료의 영향)

  • 최진호;김대익;박수현;김동우;조원기;유병팔
    • Journal of Life Science
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    • v.9 no.5
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    • pp.596-603
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    • 1999
  • The effects of anti-stress mind tonic (ASMT) drink (ASMT-0.1% and ASMT-0.5% concentration) were tested for the anti-stress action. ICR male mice (20$\pm$2 g) were fed with basic experimental diets free access to water containing these ingredients for 18 days. Psychological stress/sociopsychological stress were exposed by foot-shock for 1 hour for 3 days. Both ASMT-0.1 and ASMT-0.5 groups in the sociopsychological stress resulted in a significant decrease of 19.1% and 41.9% in plasma corticosterone (CS) secretion compared with psychological stress (control group). Noradrenaline (NA) secretions in the brain were significantly increased 23.4% and 35.9%, respectively, in ASMT-0.1 and ASMT-0.5 groups compared with control group. MHPG-SO4 (3-Methoxy-4-hydroxyphenylethyleneglycol sulfate) levels in the brain resulted in a marked decreases of 27.1% and 19.6%, respectively in ASMT-0.1 and ASMT-0.5 groups. NA/MHPG-SO4 ratios in the brain of ASMT-0.1 and ASMT-0.5 groups resulted in a significantly increase of about 70% compared with control group. These suggest that mind tonic anti-stress drink can effectively ridded the sociopsychological stress.

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Possible Relationship between Hyperactivity of Central $_{{\alpha}2_}$-Adrenoceptors and Muricidal Behavior in Olfactory Bulbectomized Rats (후신경구절제 흰쥐에서 Muricide 발생기전으로서 $_{{\alpha}2_}$-Adrenoceptors의 기능항진에 관한 연구)

  • Lee Won-Suk;Rhim Byung-Yong;Hong Ki-Whan
    • The Korean Journal of Pharmacology
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    • v.22 no.1 s.38
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    • pp.45-50
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    • 1986
  • The involvement of central $_{{\alpha}2}$-adrenoceptors in the development of muricide (mouse-killing behavior) in the olfactoly bulbectomized (OB) rats was strudied. The fractional turnover rate of noradrenaline (NA) in forebrain from OB muricidal rats was significantly lowered than that from sham rats. However, after yohimbine or idazoxan treatment, NA turnover was significantly increased in concert with inhibition of the development of muricide in OB rats. By radioligand binding studies with $[^3H]$ yohimbine, the maximum binding $(B_{max})$ of $[^3H]$ yohimbine to cerebral cortical membrane from OB rats was significantly higher than that from sham rats without change of affinity for agonists and antagonists$(K_i)$. With these results it was suggested that muricidal behavior of OB rats has a close relevance to the hyperactivity of central $_{{\alpha}2}$-adrenoceptor system.

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Effects of Sea Tangle (Laminaria japonica) and Fucoidan Beverages on Sociopsychological Stress (사회.심리적 스트레스에 미치는 다시마 (Laminaria japonica)와 후코이단 음료의 영향)

  • 최진호;김대익;박수현;김동우;이종수;유종현;정유섭
    • Journal of Life Science
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    • v.9 no.5
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    • pp.537-547
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    • 1999
  • This study was designed to investigate the effects of sea tangle (Laminaria japonica) extract (Dasi-Ex group: dry base 4.0%) and fucoidan-added (Fuco-I, II, III group: fucoidan of 1.0%, 2.0%, 3.0% added to Dasi-Ex) beverages on the anti-stress action. ICR male mice (20$\pm$2g) were fed basic experimental diets and given free through water bottle filled with these beverages instead of water for 18 days including sociopsychological stress. Body weight gains were consistently lower in Dasi-Ex and Fuco-I,II,III groups compared with control group, expecting in a inhibitory effect of obesity. Dasi-Ex group resulted in a significant decrease of 25% in serum corticosterone (CS) secretion, while Fuco-I,IIand IIIgroups resulted in a marked decreases of 45~55% in serum CS secretion compared with control group. Noradrenaline (NA) secretions were significantly increased about 15% in Dasi-Ex group, and 20~22% in Fuco-I,II,III groups compared with control group. Significant differences in brain MHPG-SO4 levels of Dasi-Ex group could not be obtained, but Fuco-I,II,III groups resulted in a marked decreases of 20~25% in brain MHPG-SO4 ratio of brain, but Fuco-I,II and III groups resulted in a marked increases of 45~60% in NA/MHPG-SO4 ratio of brain compared with control group. These results suggest that fucoidan beverage may play a effective role in a ridding of the sociopsychological stress by pivotal anti-stress effect of fucoidan.

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The Optimum Conditions for the Simultaneous Determination of Neurotransmitters in Rat Brain Striatum by High Performance Liquid Chromatography with Electrochemical Detection (HPLC-ECD를 이용한 흰쥐 뇌의 선조체 중 신경전달물질의 동시분석시 최적 조건)

  • Kang, Jong-Seong;Mun, Min-Seon;Shin, Hyung-Seon;Lee, Soon-Chul
    • Analytical Science and Technology
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    • v.8 no.2
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    • pp.215-220
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    • 1995
  • A simple, efficient and sensitive method was described for the simultaneous determination of catecholamine, indoleamine and related metabolites from the homogenates of the rat brain striatum by HPLC-ECD. The optimum mobile phase on a reverse phase $C_{18}$ column was 35mM sodium acetate buffer(included 10mM citric acid, 0.13mM $Na_4EDTA$, 0.58mM SOS, pH3-4):MeOH=85:15. The column temperature was $30^{\circ}C$. Dopamine(DA), 3, 4-dihydroxyphenyl acetic acid(DOPAC), homovanilic acid(HVA), 5-hydroxyindole acetic acid(5-HIAA), serotonin(5-HT) and noradrenaline(NA) could be separated and analysed to very small amount. The detection limits of this method were 2~10pg per injection for all components. The effects of age and sex of rat on the contents of the catecholamines and their metabolites in rat brain striatum were studied. The levels of DA and 5-HT contents of the 7 week old female rats were higher than those of the 7 week old male rats. As the age of rat increases, the contents of DOPAC increased significantly.

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Effects of Locus Coeruleus/Subcoeruleus Stimulation on the Tail Flick Reflex and Efflux of Noradrenaline into the Spinal Cord Superfusates (청반핵 자극으로 인한 노르아드레날린의 유리가 동통의 조절에 미치는 영향)

  • Park, Kyung-Pyo;Kim, Jong-Sung;Suh, Dae-Chul;Park, Hyoung-Sup
    • The Korean Journal of Pharmacology
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    • v.30 no.1
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    • pp.29-37
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    • 1994
  • Inhibition of the nociceptive Tail Flick Reflex (TFR) was observed with electrical stimulation of the locus coeruleus/subcoeruleus (LC/SC) in the male Sprague - Dawley rats under light anesthesia, and the involved neurotransmitter (s) were characterized. Electrical stimulation of LC/SC induced the analgesia with the stimulation threshold (intensity of the current, given for 100 usec and in 100 Hz frequency, which caused the TF latency longer than 6.5 sec) around 55 uA. Intrathecal administrations of ${\alpha}_2$ antagonist, yohimbine (30 ug) or opioid antagonist, naloxone (20 ug) increased the stimulation threshold by 147% and 123% respectively (from 55 uA to 135 uA,9 and from 54 uA to 123 uA;P0.01, n=5, each). The basal TF latency without stimulation (3.1 sec) was reduced by the antagonists (to 2.5 sec by yohimbine, p<0.05, n=5; to 2.6 sec by naloxone, p<0.1, n=5), vehicle only did not show any effect. Noradrenaline(NA) in the spinal cord superfusates measured with HPLC was increased by the LC/SC stimulation, from 4.18 ng/ml before to 7.74 ng/ml after stimulation (P<0.05, n=10). The result suggest that analgesia induced by LC/SC stimulation is mediated, at least in part, by the noradrenergic system in which ${\alpha}_2$ receptor is involved, as well as the opioid system.

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$Na^{+}/Ca^{2+}$ Exchange System in Atrial Trabeculae and Vascular Smooth Muscle of the Rabbit (토끼 심방근 및 혈관 평활근에서의 $Na^{+}/Ca^{2+}$ 교환기전에 관한 연구)

  • Kim, Hee-Ju;Moon, Hyung-Ro;Earm, Yung-E;Ho, Won-Kyung
    • The Korean Journal of Physiology
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    • v.22 no.1
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    • pp.13-29
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    • 1988
  • In order to elucidate the regulatory mechanism of intracellular calcium ion concentrations, contractions or contractures induced by $Na^{+}-removal$, calcium-application or ouabain-treatment as an index of $Na^+/Ca^{2+}$ exchange activity were studied in atrial muscle or vascular smooth muscle (aorta and renal artery) of the rabbit. The magnitude of low sodium contractures in atrial trabeculae increased with sigmoid shape when external sodium concentrations were reduced to sodium-free condition, whereas that of calcium contracture intensified in a parabolic pattern when external calcium concentrations were elevated to 8 mM. $Na^{+}-removal$ contractures were induced in a duration-dependent manner to $K^{+}-free$ exposure and same findings were observed with ouabain treatment. $Na^{+}-free$ contractures were not affected by verapamil treatment, but stimulated by $100{\mu}M\;Mn^{2+}$ and inhibited by high concentrations of $Mn^{2+}\;(2{\sim}8mM)$ in a dose-dependent manner. Ryanodine which is known to suppress the release of calcium from internal store abolished spontaneous twitch contractions induced by $K^{+}-free$ solution, but had no effect on the development $Na^{+}-free$ contractures. Na-free contractures were not always induced in vascular smooth muscle preparations. Contractures by $O\;mM\;Na^+$ were usually seen in aorta, but not often in renal artery.$50\;mM\;K^+$, noradrenaline (NA) and angiotensin II (AII) always evoked very large contraction in all preparations of vascular smooth muscle. Contractures developed by $O\;mM\;Na^+$ were not sensitive to verapamil treatment as in atrial trabeculae, but were abolished by $100{\mu}M\;Mn^{2+}$. In contrast to $Na^{+}-free$ contractures, $Mn^{2+}(100{\mu}M)$ had no effect on the contractures induced by NA or 50 mM$K^+$. Caffeine in the concentration of 10 mM evoked transient contracture in the distal renal artery. The rate of spontaneous relaxation in caffeine contracture was dependent upon the concentrations of external sodium, and had double component of relaxation when the rate of relaxation was plotted in the semilogarithmic scale of relative tension versus time. Especially late components of relaxation had more direct relation to $Na^+$ concentrations. It could be concluded that $Na^+/Ca^{2+}$ exchange mechanism in the heart has a large capacity, inhibited by $Mn^{2+}$ but not by verapamil and ryanodine, while $Na^+/Ca^{2+}$ exchange system in vascular smooth muscle has a very low capacity especially in small artery, inhibited by low concentration of $Mn^{2+}\;(100{\mu}M)$ but not affected by verapamil and ryanodine.

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