• 제목/요약/키워드: carbachol

검색결과 115건 처리시간 0.028초

갑상선에서 protein kinase C에 의한 thyroxine 유리조절 (Regulation of thyroxine release in the thyroid by protein kinase C)

  • 김진상
    • 대한수의학회지
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    • 제39권6호
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    • pp.1073-1080
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    • 1999
  • Previous studies suggested that the inhibition of thyroxine ($T_4$) release by ${\alpha}_1$-adrenoceptor and muscarinic receptor stimulation results in activated protein kinase C (PKC) from mouse and guinea pig thyroids. In the present study, the effect of carbachol, methoxamine, phorbol myristate acetate (PMA), and R59022 on the release of $T_4$ from the mouse, rat, and guinea pig thyroids was compared to clarify the role of PKC in the regulation of the release of $T_4$. The thyroids were incubated in the medium containing the test agents, samples of the medium were assayed for $T_4$ by EIA kits. Forskolin, an adenylate cyclase activator, chlorophenylthio-cAMP sodium, a membrane permeable analog of cAMP, and isobutyl-methylxanthine, a phosphodiesterase inhibitor, like TSH (thyroid stimulating hormone), enhaced the release of $T_4$ from the mouse, rat, and guinea pig thyroids. Methoxamine, an ${\alpha}_1$-adrenoceptor agonist, inhibited the TSH-stimulated release of $T_4$ in mouse, but not rat and guinea pig thyroids. In contrast, carbachol, a muscarinic receptor agonist, inhibited the release of $T_4$ in guinea pig, but not mouse and rat thyroids. These inhibition were reversed by prazosin, an ${\alpha}_1$-adrenoceptor antagonist or atropine, a muscarinic antagonist or $M_1$- and $M_3$-muscarinic antagonists, in mouse or guinea pig thyroids. In addition, staurosporine, a PKC inhibitor, reversed methoxamine or carbachol inhibition of TSH stimulation. Furthermore, PMA, a PKC activator, and R59022, a diacylglycerol (DAG) kinase inhibitor, inhibited the TSH-stimulated release of $T_4$ in mouse, rat, and guinea pig thyroids. These inhibition were blocked by staurosporine. These findings suggest that the activation of receptor or DAG inhibits TSH-stimulated $T_4$ release through a PKC-dependent mechanism in thyroid gland.

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곡지(曲池)($LI_{11}$)에 대한 유침 및 전침자극이 흰쥐의 장운동에 미치는 영향 (Effect of Acupuncture and Electro-acupuncture at $LI_{11}$ on Intestinal Motility in Rats)

  • 서용석;홍권의
    • Journal of Acupuncture Research
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    • 제25권4호
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    • pp.59-69
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    • 2008
  • Objectives : The purpose of this study was to observe the effects of acupuncture and electro-acupuncture(EA) at $LI_{11}$ on intestinal motility in rats. Methods : We made over-activated and suppressed state of intestinal motility with carbachol and loperamide in rat and carried out acupuncture with needle retained(NR), low frequency(2 Hz) EA and high frequency(100Hz) EA at $LI_{11}$ before or after the administration of carbachol or loperamide. The charcoal travel rate was measured to evaluate the intestinal motility. Results : 1. NR, 2Hz EA and 100Hz EA at $LI_{11}$ showed no significant influences on intestinal motility of rat in normal state. 2. All of the pre-treatment and post-treatment of NR, 2Hz EA and 100Hz EA at $LI_{11}$ showed no significant effects than control group on intestinal motility of rat which was over-activated with carbachol. 3. The pre-treatment of 2Hz EA and 100Hz EA at $LI_{11}$ on intestinal motility of rat which was suppressed with loperamide showed no significant influences but in the L-$LI_{11}$-EA(L) and L-$LI_{11}$-EA(H) groups, intestinal motility was significantly increased than L-control group. Conclusions : These results suggest that acupuncture and EA on $LI_{11}$ have preventive effect and therapeutic effect on suppressed intestinal motility, and EA is more effective than NR.

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중추에서 혈압과 심박수 조절에 관여하는 후시상하부 콜린성 수용체의 일차적인 역할 (Primary Role of Posterior Hypothalamic Cholinergic Receptors in Central Regulation of Blood Pressure and Heart Rate in Rats)

  • 김성윤;성기욱;고현철;이상복
    • The Korean Journal of Physiology and Pharmacology
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    • 제1권6호
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    • pp.639-645
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    • 1997
  • The purpose of the present study is to determine the role of muscarinic cholinergic receptors of posterior hypothalamus in the central blood pressure regulation when respiration is controlled. In anesthetized and artificially ventilated rats, vasodepressor response was evoked by injection of L-glutamate(10 nmol) neuroexcitatory amino acid into the posterior hypothalamic area. The injection of $carbachol(0.5{\sim}8\;nmol)$ into the same area induced dose-dependent vasodepressor and bradycardic responses. Pretreatment with atropine(4 nmol) completely blocked the vasodepressor response to carbachol(2 nmol). In contrast, in spontaneously breathing rats, the injection of carbachol(8 nmol) into the posterior hypothalamic area induced the vasopressor and tachycardic responses. These results suggest that the muscarinic cholinergic receptors in the posterior hypothalamic area primarily play an inhibitory role in the central regulation of blood pressure and heart rate.

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Mode of Inhibitory Action of Amitriptyline on Carbachol-Induced Contraction of Isolated Rabbit Detrusor Muscle

  • Gill, Won-Sik;Shin, Beong-Ho;Kim, Won-Jae;Jeong, Han-Seong
    • The Korean Journal of Physiology
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    • 제26권2호
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    • pp.137-141
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    • 1992
  • The present study was aimed at elucidating the mode of inhibitory action of tricyclic antidepressants on the smooth muscle. Effects of amitriptyline on the isolated detrusor muscle strips of the urinary bladder of the rabbit were examined. The spontaneous rhythmic movement of the muscle preparation was frequently observed, which was decreased or abolished by addition of amitriptyline $(10^{-5}{\sim}10^{-3}\;M)$. The muscle preparation responded with contraction dose dependently to carbachol, of which dose response curve shifted to the right in the presence of either amitriptyline or atropine. However, amitriptyline produced a nonparallel shift, whereas atropine caused a parallel one. In calcium free medium, the contraction response to carbachol was markedly decreased, which was resumed by the addition of $CaCl_2$ (2.5mM), but not in the presence of either amitriptyline or nifedipine. KCI (60 mM) produced a potent contraction, which was abolished in the presence of amitriptyline or nifedipine. These results suggest that amitriptyline, unlike atropine, not only acts as a noncompetitive antagonist at cholinergic muscarine receptors but also inhibits Ca-influx through the muscle cell membrane.

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The Effects of Jungri-tang Gamibang on Carbachol-accelerated Mouse Small Intestinal Transit

  • Kim, Dae-Jun;Byun, Joon-Seok
    • 대한한의학회지
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    • 제30권6호
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    • pp.9-16
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    • 2009
  • Objectives: To clarify the effects of Jungri-tang Gamibang on accelerating small intestinal movement induced by the stimulation of cholinergic neurotransmission. Methods: 500, 250 and 125mg Jungri-Tang Gamibang or 20mg domperidone were dissolved or suspended in distilled water and orally pretreated on the carbachol-accelerated small intestinal transit mice once a day for 7 days at a volume of 10ml/kg (of body weight) using a Zonde needle attached to 1 ml syringes containing test drugs. Result: Significantly (p<0.01) increase of % regions of activated charcoal transit in the small intestine was detected in carbachol control compared to that of intact control. However, significant (p<0.01) decreases of % regions of activated charcoal transit were dose-dependently observed in all Jungri-Tang Gamibang extracts or domperidone-pretreated groups. Conclusions: it was concluded that Jungri-tang Gamibang enhancement in the normal intestinal motility and normalization in the accelerated intestinal motility might interfere with a variety of muscarinic, adrenergic and histaminic receptor activities or with the mobilization of calcium ions required for smooth muscle contraction non-specifically.

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Involvement of the Phospholipase C β1 Pathway in Desensitization of the Carbachol-activated Nonselective Cationic Current in Murine Gastric Myocytes

  • Kim, Byung Joo;So, Insuk;Kim, Ki Whan
    • Molecules and Cells
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    • 제22권1호
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    • pp.65-69
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    • 2006
  • In murine gastrointestinal myocytes muscarinic stimulation activates nonselective cation channels via a G-protein and $Ca^{2+}$-dependent pathway. We recorded inward cationic currents following application of carbachol ($I_{CCh}$) to murine gastric myocytes held at -60 mV, using the whole-cell patch-clamp method. The properties of the inward cationic currents were similar to those of the nonselective cation channels activated by muscarinic stimulation in other gastrointestinal smooth muscle cells. CCh-induced $I_{CCh}$ and spontaneous decay of $I_{CCh}$ (desensitization of $I_{CCh}$) occurred. Unlike the situation in guinea pig gastric myocytes, desensitization was not affected by varying $[EGTA]_i$. Pretreatment with the PLC inhibitor (U73122) blocked the activation of $I_{CCh}$, and desensitization of $I_{CCh}$ was attenuated in PLC ${\beta}_1$ knock-out mice. These results suggest that the desensitization of $I_{CCh}$ in murine gastric myocytes is not due to a pathway dependent on intracellular $Ca^{2+}$ but to the PLC ${\beta}_1$ pathway.

태충 유침 및 전침이 병태모델 흰쥐의 장운동에 미치는 영향 (Effect of Acupuncture and Electro-acupuncture at $LR_3$ on Intestinal Motility in Rats)

  • 임성철;이현
    • Journal of Acupuncture Research
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    • 제25권5호
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    • pp.27-42
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    • 2008
  • Objectives : The purpose of this study was to observe the effects of acupuncture and electro-acupuncture at $LR_3$ on intestinal motility in rat. Methods : We made over-activated state of intestinal motility with carbachol and suppressed state of intestinal motility with loperamide in rat and carried out needle retention acupuncture and high frequency electro-acupuncture at $LR_3$ in rat devided into pre-treatment group and post-treatment group. The charcoal travel rate was measured to evaluate the intestinal motility. Results : 1. High frequency electro-acupuncture at $LR_3$ have significant influences on intestinal motility of rat in normal state. 2. Pre-treatment of needle retention acupuncture, high frequency electro-acupuncture significantly decreased intestinal motility in rat which over-activated with carbachol. 3. Post-treatment of high frequency electro-acupuncture significantly increased intestinal motility in rat which suppressed with loperamide. Conclusions : These results suggest that acupuncture and electro-acupuncture at $LR_3$ are effective on intestinal motility in rat.

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쥐 해마에서 M1 무스카린 아세틸콜린 수용체의 활성에 의한 GluA2 세포내이입 연구 (Activation of the M1 Muscarinic Acetylcholine Receptor Induces GluA2 Internalization in the Hippocampus)

  • 류근오;석헌
    • 생명과학회지
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    • 제25권10호
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    • pp.1103-1109
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    • 2015
  • 뇌 해마의 콜린성 신경분포는 학습과 기역에 연관성이 있는 것으로 알려져 있으며 이의 작용제인 carbachol 투여 시 장기기억 저하가 유도됨이 알려져 왔다. 그러나 이러한 콜린성 자극에 의한 해마 신경세포의 시냅스 내 변화기작은 완전히 알려지지 않고 있다. 본 연구에서는 아세틸콜린 수용체의 활성에 의하여 유도되는 장기기억 저하 현상에 있어 alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate (AMPA) 수용체가 후시냅스 표면으로부터 사라지는 현상과 이의 조절기작에 대하여 알아보고자 한다. 이를 위하여 쥐 해마의 일차세포를 추출하고 체외에서 배양한 성숙 신경세포에 carbachol 을 투여하여 장기기억 저하를 유도 하였으며, 후시냅스의 표면으로부 터 AMPA 수용체의 아단위체인 GluA2가 M1 무스카린 수용체의 길항제에 의하여 저해 되었다. 또한 콜린성 자극 에 의한 GluA2의 내재화 현상의 작용기작 연구를 위하여 쥐 해마 절편에 carbachol 투여 후 GluA2와 직접적인 상호작용을 하는 Glutam내재화 되었음을 확인하였다. 이러한 현상은 ate receptor-interacting protein 1 (GRIP1) 과 clathrine 단백질이 매개하는 세포내이입 작용을 하는 adaptin-α 단백질의 결합 변화를 관찰하였다. GluA2는 carbachol 자극에 의해 세포내이입 과정에서 adaptin-α 와의 결합이 증가하였으며 반대로 GRIP1과는 해리되었다. 이는 아세틸콜린의 수용체의 자극에 의하여 GluA2의 내제화 작용이 수반되며, 이의 작용기작으로 GluA2의 후시 냅스 표면 발현시에 결합하고 있는 GRIP1과 해리 되면서 장기기억 저하 현상이 유도됨을 의미한다.

창포 정유가 토끼의 적출장관 운동에 미치는 영향 (Effect of Essential Oil of Acori Rhizoma on Motility of Isolated Rabbit Jejunum Segment)

  • 김영환;박준형
    • Current Research on Agriculture and Life Sciences
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    • 제10권
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    • pp.19-33
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    • 1992
  • 같은 천남성과에 속하면서도 정유의 함유성분 및 함량이 서로 다른 수창포 정유와 석창포 정유가 토끼 적출장관 운동에 미치는 영향과 차이점, 또 어떠한 작용양식에 의하여 이루어지는가를 알아보고저 carbachol pilocarpine, histamine 및 barium chloride등과의 상호작용을 비교, 검토하였던 바 다음과 같은 결론을 얻었다. 1. 수창포 정유와 석창포 정유는 모두 토끼 적출장관 운동을 이완시켰으며, 농도를 증가시킬수록 이완정도는 현저하였고, 장관운동의 이완되는 정도는 두 정유 모두 같은 농도에서는 거의 비슷하였다. 2. ED50에 해당하는 농도는 수창포 정유는 0.0045% 이었고, 석창포 정유는 0.0035%이었다. 3. 수창포 정유와 석창포 정유에 의해 이완된 토끼의 적출장관은 carbachol pilocarpine, barium chloride에 의하여 정유 투여전의 상태로 회복하였으나, histamine에 의해서는 부분적인 회복을 보였다. 4. 수창포 정유와 석창포 정유는 carbachol pilocarpine, histamine 및 barium chloride에 의하여 수축된 토끼의 적출장판을 이완시켰다. 5. 이상의 결과로 보아서 수창포 정유와 석창포 정유는 다같이 향신경성작용 및 향근육성작용에 의해 토끼 적출장관 운동을 이완시킨다고 사료된다.

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Diazepam이 흰쥐 회장 평활근의 Carbachol 유발 수축에 미치는 영향 (THE EFFECTS OF DIAZEPAM ON THE CARBACHOL INDUCED CONTRACTION OF THE ISOLATED RAT ILEUM)

  • 김정옥;권오철;하정희;이광윤;김원준
    • Journal of Yeungnam Medical Science
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    • 제6권2호
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    • pp.13-22
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    • 1989
  • Benzodiazepine 계통의 약물들은 진정, 최면제로 진정, 최면, 불안의 감소와 함께 횡문근 이완과 항 경련 작용을 가진다는 것은 이미 잘 알려진 바이나 이러한 약리 작용의 기전에 대해서는 아직 확실하게 밝혀진 바가 없다. 최근 이러한 약리 작용과 연관성을 지니는 것으로 알려진 뇌내의 benzodiazepine의 수용체(receptor)를 통한 자극 전달 기전에 calcium 이온의 역할이 큰 비중을 차지할 수 있음이 대두되었다. 또 뇌 이외의 다수의 말초 조직에서도 benzodiazepine의 수용체가 있으며, 이들도 calcium 이온과 상호 작용 할 것이라고 보고된 바가 있으나 이들의 약리 작용과 그 작용 기전에 대해서는 아직 확실히 밝혀진 바가 없다. 이에 저자는 benzodiazepine 계통 약물 중 대표적이라 할 수 있는 diazepam을 사용하여 diazepam이 장관 평활근의 수축성에 미치는 영향을 calcium 이온과 연관시켜 검색하기 위하여 흰쥐 회장 평활근에서 적출한 종주근 절편을 적출 근편 실험조내에서 diazepam 처치 전후의 carbachol, histamine 및 calcium 유발 수축성의 변화를 등척성 장력 측정기를 사용하여 관찰하여 다음과 같은 결과를 얻었다. 1. Diazepam은 흰쥐 회장 절편의 기본 장력을 농도 의존적으로 감소시켰다. 2. Diazepam은 흰쥐 회장 절편의 carbachol-유발 수축 작용을 고농도에서는 억제시켰으며 저농도에서는 오히려 증강시키는 이중 효과를 나타내었다. 3. Diazepam 존재하에서 흰쥐 회장 절편의 histamine-유발 수축 작용은 억제되었으며, diazepam의 농도가 증가함에 따라 그 억제도는 증가하였다. 4. 칼슘 배제 용액에서 칼슘 재 투여로 인한 회장 절편의 장력의 회복율은 diazepam 전처치에 의해 억제되었으며, diazepam의 농도가 증가함에 따라 그 억제도는 증가하였다. 이상의 실험 결과로 미루어 diazepam은 흰쥐 회장 종주근의 수축성을 억제시키며 이 작용은 diazepam이 평활근 세포내로의 calcium의 유입을 억제함으로써 나타나는 것으로 사료된다.

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