• Bulletin of the Korean Chemical Society
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• 제25권2호
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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.

• The Korean Journal of Physiology and Pharmacology
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• 제7권1호
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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.

• 생명과학회지
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• 제9권5호
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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.

• 생명과학회지
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• 제9권5호
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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.

• 생명과학회지
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• 제9권5호
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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.

• 대한약리학회지
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• 제22권1호
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• pp.45-50
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• 1986

후신경구절제(OB) 흰쥐에 있어서 muricide의 발생은 중추성 ${\alpha}$-adrenoceptors의 기능항진과 밀접한 관계가 있다는 가설하에 다음 실험을 행하였다. Muricide를 일으키는 OB 흰쥐의 전뇌내 noradrenaline(NA)의 전환율은 대조군에 비하여 현저히 낮았으나 $_{{\alpha}_2}$-adrenoceptor 길항약물인 yohimbine이나 idazoxan 투여시 NA 전환은 muricide의 억제와 함께 현저히 증가되었다. OB흰쥐의 전뇌 피질막의 $[^3H]$ yohimbine에 대한 최대결합능(Bmax)은 대조군에 비하여 현저히 높았다. ${\alpha}$-Adrenoceptor 효능약물 및 길항약물에 대한 친화도는 아무런 변동이 없었다. 이상의 결과로 보아 OB흰쥐에서 야기되는 muricide는 중추성 ${{\alpha}_2}$-adrenoceptor의 기능 항진과 밀접한 관련이 있다고 사료되는 바이다.

• 생명과학회지
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• 제9권5호
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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.

• 분석과학
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• 제8권2호
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• pp.215-220
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• 1995

흰쥐 뇌의 선조체로부터 catecholamine, indoleamine 및 대사산물을 동시분석할 수 있는 간편한 방법을 제시하였다. 기기는 ECD를 장착한 HPLC를 사용하였고, 고정상인 $C_{18}$ 컬럼에서, 이 동상은 10mM citric acid, 0.13mM $Na_4EDTA$, 0.58mM SOS를 함유하는 35mM sodium acetate buffer(pH 3.4) : MeOH=85:15가 최적이었다. 이 때 컬럼온도는 $30^{\circ}C$였다. 이 조건으로 dopamine(DA), 3, 4-dihydroxyphenyl acetic acid(DOPAC), homovanilic acid(HVA), 5-hydroxyindole acetic acid(5-HIAA), serotonin(5-HT) 및 noradrenaline(NA)을 미량까지 분석할 수 있었고, 검출한계는 각 성분에 대해 1회 주입당 2~10pg이었다. 이 방법으로 흰쥐의 주령 및 성별에 따른 선조 체내 생체아민과 대사산물의 함량을 비교하였다. 7주령 쥐에서 암컷은 수컷보다 DA와 5-HT의 함량이 유의성 있게 높은 것으로 나타났으며, 주령이 증가함에 따라 암컷에서 DOPAC의 함량이 유의적으로 증가하였다.

• 대한약리학회지
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• 제30권1호
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• pp.29-37
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• 1994

배외측 뇌교의 전기자극은 척수 수준에서 동통의 역치를 증가시키고, 또한 말초로 부터 오는 유해성 자극에 의해 야기되는 척수후각세포의 흥분성을 억제하여 진통효과를 나타낸다. 이러한 진통효과는 noradrdnergic 원심신경을 매개로 한다고 하였지만, 이직까지 이를 직접적으로 뒷받침하는 신경화학적인 증거는 보고되지 않았다. 따라서 본 실험은 뇌교에 위치한 청반핵(Locus coeruleus)의 전기자극시, 척수 수준에서 일어나는 동통조절효과를 쥐꼬리 회피 반사(Tail Flick Reflex)를 이용해 관찰하고, 이러한 동통조절효과는 어떤 신경전달물질을 매개로해서 일어나며, 또한 생체내에서 직접 유리 되는지 살펴보기 위해 Push Pull technique을 이용해 척수액내 noradrenaline의 농도 변화를 HPLC로 측정하였다. 청반핵자극시의 동통조절기전을 알아보기위해 yohimbine, naloxone 그리고 vehicle의 3group 으로 나누어 각 길항제의 효과를 실험하였다. 청반핵 자극시 TF latency의 증가(>6.Ssec)를 보이는 역치 자극강도가 yohimbine $30{\mu}g$을 척수내로 투여한 후에는 $135\;{\mu}A$로서 안정시의 $55\;{\mu}A$에 비해 147% 증가되어 유의한 변화를 보여주었다(P<0.01, n=5). $Naloxone\;20{/mu}g$을 투여한 실험군 에서도 초기 역치자극강도 $54\;{\mu}A$에서 $120\;{\mu}A$로서 123% 증가되어 역시 유의한 변화를 보여주었다(P<0.01, n=5). 그러나 vehicle group에서는 투여 전, 후 역치자극강도의 변화가 없었다. 청반핵 자극이 없는 안정상태에서의 TF latency 값은 모두 3.1 sec였고 yohimbine과 naloxone투여후에는 각각 2.5 sec,2.6sec로 감소되어, 긴장성 억제가 차단되는 것으로 나타났다(각각 P<0.05,P<0.1,n=5).청반핵의 전기자극$(100\;{\mu}A)$은 척수액내 noradrenaline의 농도를 증가시켰으나(평균 4.18mg/ml에서 7.74 ng/ml로, p<0.05, n=10),dopamine의 농도는 증가되지 않았다. 이상의 결과는 청반핵 자극에 의한 척수내 동통조절효과는 opioid 계외에 부분적으로 noradrdnaline을 매개로 해서 이루어지며, 이에 관여하는 수용체는 ${\alpha}_2$ 임을 보여주었다.

• The Korean Journal of Physiology
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• 제22권1호
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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.