• 약학회지
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• 제44권1호
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• pp.52-59
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• 2000

An exceptionally conserved sequence that is shared among most G protein-coupled neurotransmitter receptors is an aspartate-arginine-tyrosine triplet that is located at the second cytoplasmic domain. Using the ml subtype of muscarinic acetylcholine receptors as an example, a point mutation of the arginine residue at position 123 into asparagine was induced. This mutation resulted in a complete blockade of the carbachol-induced increases of PI hydrolysis and intracellular $Ca^2$$^{+}$ level, in spite of the expression of the wild-type and mutant receptors at similar concentrations in Chinese hamster ovary cells. In marked contrast, the muscarinic agonist carbachol induced concentration-dependent enhancement of the activity of NO synthase at mutant ml receptors although the enhancement was significantly smaller than at wild-type ml receptors. These data suggest that this highly conserved arginine residue plays an important role in coupling of muscarinic receptors to the second messenger systems and the presence of alternate mechanisms of activation of neuronal NO synthase which might be operative in the absence of large changes in the concentration of cellular $Ca^{2+}$.2+/.

• The Korean Journal of Physiology and Pharmacology
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• 제8권5호
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• pp.289-293
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• 2004

To investigate whether VacA (vacuolating toxin) produced by Helicobacter pylori Korean stain 99 induces intestinal secretion, purified VacA was added to T84 cell monolayers mounted in Ussing chambers, and electrical parameters were monitored. Mucosal addition of low pH-pretreated VacA increased short circuit current (Isc). The effect was time- and dose-dependent and saturable. The time-to-peak Isc was concentration-dependent. Chloride channel inhibitors, niflumic acid or 5-nitro-2-(3-phenylpropylamino)-benzoate (NPPB), inhibited VacA-stimulated Isc. Carbachol (CCh)-induced increase of Isc was prolonged by the addition of VacA to the mucosal side only. The effect was unaltered by the addition of niflumic acid. VacA did not show cytopathic effects. These studies indicate that VacA is a nonlethal toxin that acts in a polar manner on T84 monolayers to potentiate $Cl^-$ secretion and the response to CCh secretion without decrease in monolayer resistance. VacA may contribute to diarrhea diseases in human intestinal epithelial cells.

• 약학회지
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• 제35권4호
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• pp.341-347
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• 1991

It was reported that protein carboxymethylation is involved in amylase secretion of parotid gland by isoproterenot. It was also suggested that a small part of the total cellular protein carboxymethylation is directly involved in pancreatic enzyme secretion. On the contrary, other authors reported that there is no relationship between protein carboxymethylation and secretion in pancreas and parotid gland. In recent study, it was proposed that a methyl acceptor protein plays a limited modulatory role in the coupling of cytosolic $Ca^{++}$ accumulation and exocytosis. In this study, the effects of cholinergic and adrenergic agents on the activities of protein methylase II in pancreatic tissues were examined to test the relationship between protein methylation and pancreatic secretion. The results are as follows. The activity of amylase was slightly increased at the concentration of $10^{-5}$ M of isoproterenol and norepinephrine. The activities of protein methylase I and II were decreased by isoproterenol and norepinephrine, but the activities of protein methylase III were hardly changed. The cholinergic stimulants acetylcholine and carbachol at a concentration of $10^{-5}$ M increased the activities of protein methylase I and decreased the activitiy of protein methylase III compared with control.

• 대한수의학회지
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• 제15권2호
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• pp.223-231
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• 1975

In mammals there are two distinct cellular units of the gastric glands which are responsible for the secretion of acid and pepsin respectively, namely, the parietal cells for acid and the peptic or chief cells for pepsin. On the other hand, the bird does net have separate parietal and chief cells in the glandular stomach. There exist only a single cell type in the asian gastric secretory-glands. In spite of this single cell type, however, variation in pepsin and acid secretion can he seen. Present study was conducted to know distribution, secretion and formation of the pepsinogen granules in chicken and rat stomach which observing by light and electron microscope. 1. In chicken, the pepsinogen granules are distributed in all submucosal gland cells and yet there are no distinction of parietal and chief cells. In rat, the pepsinogen granules are distributed in chief cells which lined the lower two-thirds of the gastric tubles and the parietal cells occupy upper third of the tuble. 2. Carbachol markedly stimulates the secretion of pepsinogen granules in chiken and rat, but Histamine is slightly. 3. After Histamine and Carbachol treatment, the pepsinogen granules are formated continuously and reaccmulated as control after 3 to 4 hours.

• 대한소아치과학회지
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• 제25권2호
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• pp.352-367
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• 1998

Intracellular pH (pHi) plays an important role in the regulation of cellular processes by influencing the acitivity of various enzymes in cells. Therefore, almost every type of mammalian cell possesses an ability to regulate its pHi. One of the most prominent mechanisms in the regulation of pHi is $Na^+/H^+$ exchanger. This exchanger has been known to be activated when cells are stimulated by the binding of agonist to the muscarinic receptors. Therefore, the aims of this study were to compare the rates of $H^+$ extrusion through $Na^+/H^+$ exchanger before and during muscarinic stimulation and to investigate the possible existence of $HCO_3^-$ transporter which is responsible for the continuous supply of $HCO_3^-$ ion to saliva. Acinar cells were isolated from the rat mandibular salivary glands and loaded with pH-sensitive fluoroprobe, 2', 7'-bis(2-carboxyethyl)-5(6)-carboxyfluorescein(BCECF), for 30min at room temperature. Cells were attached onto the coverglass in the perfusion chamber and the changes in pHi were measured on the iverted microscope using spectrofluorometer. 1. By switching the perfusate from $HCO_3^-$-free to $HCO_3^-$-buffered solution, pHi decreased by $0.39{\pm}0.02$ pH units followed by a slow increase at an initial rate of $0.04{\pm}0.007$ pH units/min. The rate of pHi increase was reduced to $0.01{\pm}0.002$ pH units/min by the simultaneous addition of 1 mM amiloride and $100{\mu}M$ DIDS. 2. An addition and removal of $NH_4^+$ caused a decrease in pHi which was followed by an increase in pHi. The increase of pHi was almost completely blocked by 1mM amiloride in $HCO_3^-$-free perfusate which implied that the pHi increase was entired dependent on the activation of $Na^+/H^+$ exchanger in $HCO_3^-$-free condition. 3. An addition of $10{\mu}M$ carbachol increased the initial rate of pHi recovery from $0.16{\pm}0.01$ pH units/min to $0.28{\pm}0.03pH$ units/min. 4. The initial rate of pHi decrease induced by 1mM amiloride was also increased by the exposure of the acinar cells to $10{\mu}M$ carbachol ($0.06{\pm}0.008pH$ unit/min) compared with that obtained before carbachol stimulation ($0.03{\pm}0.004pH$ unit/min). 5. The intracellular buffering capacity ${\beta}1$ was $14.31{\pm}1.82$ at pHi 7.2-7.4 and ${\beta}1$ increased as pHi decreased. 6. The rate of $H^+$ extrusion through $Na^+/H^+$ exchanger was greatly enhanced by the stimulation of the cells with $10{\mu}M$ carbachol and there was an alkaline shift in the activity of the exchanger. 7. An intrusion mechanism of $HCO_3^-$ was identified in rat mandibular salivary acinar cells. Taken all together, I observed 3-fold increase in $Na^+/H^+$ exchanger by the stimulation of the acinar cells with $10{\mu}M$ carbachol at pH 7.25. In addition, I have found an additional mechanism for the regulation of pHi which transported $HCO_3^-$ into the cells.

• 대한한의학회지
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• 제27권1호
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• pp.146-154
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• 2006

Objectives : Siguan points (LI4, LR3) have been most frequently applied for various diseases, especially different digestive disorders such as constipation, abdominal pain or various intestinal inflammatory diseases. The fact that gastrointestina movement is closely connected with physiologic functions or pathologic process of alimentary canal led us to ask the question if Siguan points affects on intestinal motility. Design: To investigate the effect of Siguan acupuncture on the intestinal movement in both physiologic and pathologic conditions, we divided the experimental animals into 12 groups. Six groups were pre-treated with loperamide (0.5 mg/kg, sc) or scoploamine (0.5 mg/kg, sc) to suppress the intestinal movement and another three groups were pretreated with carbachol (0.5 mg/kg, po) to activate it, whereas the rest three groups didn't receive any pretreatment to be kept in the physiological condition. After the administration with charcoal meal, mice were acupunctured bilaterally on sham point or Siguan points as the manner of tap-stimulation, with the exception of no acupuncture groups. Methods : Mice were scarified in twenty minutes after the administration of charcoal to measure the distance of charcoal passage from stomach-duodenal junction. The effect on intestinal movement was presented by calculating the relative distance where charcoal arrived to total length of small intestine. Results : In physiological state, charcoal meal passed around 53%, and there was no significant difference between Siguan points and sham points groups. On the other hand. Siguan points-sitimulation significantly ameliorated loperamide or scoplolamine-induced suppressed travel rate of 17.3 % and 18.6% in sham point into 26% and 26.3% respectively (p<0.05). In carbachol-induced accelerated condition, Siguan points-stimulation didn't affect intestinal motility comparing to sham point group passed about 97.6%. Conclusions : These results postulate that acupuncture at Siguan points have a therapeutic effect by restoring cholinergic activity on pathogenically suppressed intestinal peristalsis, but does not affect the gastrointestinal motility in the normal or accelerated condition.

• 대한약리학회지
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• 제5권1호
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• pp.65-72
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• 1969

전신마취가토(全身麻醉家兎) 및 춘체가토(春體家兎)에 tetrabenazine(40mg/kg)을 투어(投與)한 후(後) norepinephrine 및 tyramine에 대(對)한 승압반응(昇壓反應) 및 심박증가(心搏增加) 반응(反應)을 검색하여 다음과 같은 결과를 얻었다. 1) 전신가토(全身家兎)에서 TBZ투여(投與) 2시간(時間) 이내(以內)에는 NE에 대(對)한 승압반응(昇壓反應)은 강화(强化)되지 않았다. 2) 전신가토(全身家兎)에서 TBZ투여(投與) 5시간후(時間後)에는 NE에 대(對)한 승압반응(昇壓反應)은 강화(强化)되었으며 10시간후(時間後)에는 강화(强化)는 최고(最高)에 달(達)하였고, 24시간(時間), 48시간후(時間後)에는 점차(漸次)이 강화(强化)는 소실(消失)되었다. 3) 춘체가토(春體家兎)에서 TBZ투여(投輿) 10시간후(時間後)에는 NE에 대(對)한 승압반응(昇壓反應)은 현저(顯著)히 강화(强化)되었고 심박증가반응(心搏增加反應)도 증강(增强)한 경향(傾向)을 보였다. 그러나 24시간 후(時間 後)에는 이러한 강화(强化)는 볼 수 없었다. 4) 전신가토(全身家兎)에서 TBZ투여(投與)로 NE승압반응(昇壓 反應)이 강화(强化)되어 있는 상태하(狀態下)에서는 desipramine으로써 더 이상 반응(以上 反應)이 증가(增加)되지 않았다. 5) 춘체가토(春體家兎)에서 TBZ투여(投與)로 NE승압반응(昇壓 反應)이 강화(强化) 되어 있는 상태하(狀態下)에서 desipramine으로써 그 반응(反應)은 더욱 증가(增加)되었다. 6) TBZ투여(投與) 2시간(時間) 및 6시간후(時間後)에 carbachol을 주사(注射)한 가토(家兎)에서는 NE에 대(對)한 승압반응(昇壓反應)의 강화(强化)는 현저(顯著)히 억제(抑制)되었다. 7) TBZ투여(投與) 10시간후(時間後), 전신가토(全身家兎)의 tyramine에 대(對)한 승압반응(昇壓反應)은 약화(弱化)되지 않았고 춘체가토(春體家兎)의 tyramine에 대(對)한 반응(反應)은 강화(强化)되었다. 8) TBZ로서 NE에 대(對)한 supersensitivity가 발생(發生)하고 tyramine에 대(對)한 반응(反應)은 약화(弱化)되지 않고 carbachol로서 NE에 대(對)한 supersensitivity가 방지(防止)되었음은, NE에 대(對)한 supersensitivity발생(發生)에 뇌내(腦內) catecholamine 감소(減少)에 따른 교감신경계(交感神經系) tone의 감소(減少)가 관계(關係)있음을 시사(示唆)하고 있다.

• 대한약학회:학술대회논문집
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• 대한약학회 2000년도 춘계총회 및 학술대회
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• pp.114.3-115
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• 2000

• 한국어업기술학회:학술대회논문집
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• 한국어업기술학회 2000년도 춘계수산관련학회 공동학술대회발표요지집
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• pp.267-268
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• 2000

Burnstone등이 어류장의 미주신경지배에 대해서 연구한 이래로 Burka et al는 무지개송어 위장관에서 Carbachol과 5-HT가 농도의존적으로 수축함을 밝혔다. 그리고 무지개송어의 위장관수축반응은 무스카린성 M2 subtype 수용체를 경유한다고 하였으며, Ach-유발된 수축이 nicotine이나 hexamethonium을 고농도로 처치시에 억제되었고, 이는 ACh의 반응이 preganglionic cholinergic fiber에 의존함을 암시하였다. 이전의 경골어류장의 여러 수용체에 대한 연구는 주로 송어류에서 이루어져 왔으며, 타 어종에서의 연구는 별로 없었다. (중략)

• 고려인삼학회:학술대회논문집
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• 고려인삼학회 2003년도 추계 총회 및 학술대회
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• pp.38-39
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• 2003