• 제목/요약/키워드: blocker

검색결과 627건 처리시간 0.029초

Actions of Group I Metabotropic Glutamate Receptor Agonist on Synaptic Transmission and Ionic Currents in Rat Medial Vestibular Nucleus Neurons

  • Lee, Hae-In;Chun, Sang-Woo
    • International Journal of Oral Biology
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    • 제34권4호
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    • pp.215-222
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    • 2009
  • Medial vestibular nucleus (MVN) neurons are involved in the reflex control of the head and eyes, and in the recovery of vestibular function after the formation of peripheral vestibular lesions. In our present study, whole cell patch clamp recordings were carried out on MVN neurons in brainstem slices from neonatal rats to investigate the actions of a group I metabotropic glutamate receptor (mGluR) agonist upon synaptic transmission and ionic currents. Application of the mGluR I agonist (S)-3,5- dihydroxyphenylglycine (DHPG) increased the frequency of miniature inhibitory postsynaptic currents (mIPSCs) but had no effect upon amplitude distributions. To then identify which of mGluR subtypes is responsible for the actions of DHPG in the MVN, we employed two novel subtype selective antagonists. (S)-(+)-$\alpha$-amino-a-methylbenzeneacetic acid (LY367385) is a potent competitive antagonist that is selective for mGluR1, whereas 2-methyl-6-(phenylethynyl)-pyridine (MPEP) is a potent noncompetitive antagonist of mGluR5. Both LY367385 and MPEP antagonized the DHPG-induced increase of mIPSCs, with the former being more potent. DHPG was also found to induce an inward current, which can be enhanced under depolarized conditions. This DHPG-induced current was reduced by both LY367385 and MPEP. The DHPG-induced inward current was also suppressed by the PLC blocker U-73122, the $IP_3$ receptor antagonist 2-APB, and following the depletion of the intracellular $Ca^{2+}$ pool by thapsigargin. These data suggest that the DHPG-induced inward current may be mainly regulated by the intracellular $Ca^{2+}$ store via the PLC-$IP_3$ pathway. In conclusion, mGluR I, via pre- and postsynaptic actions, may modulate the excitability of the MVN neurons.

Low-Voltage Activated $Ca^{2+}$ Current Carried via T-Type Channels in the Mouse Egg

  • Yang, Young-Sun;Park, Young-Geun;Cho, Soo-Wan;Cheong, Seung-Jin;Haan, Jae-Hee;Park, Choon-Ok;Hong, Seong-Geun
    • The Korean Journal of Physiology
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    • 제27권1호
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    • pp.107-114
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    • 1993
  • Most of voltage operated $Ca^{2+}$ channels can be divided into three types (T-, N-, and L-type), according to the electrical and pharmacological properties. Their distribution is closely related to cell specific functions. Properties of the voltage activated $Ca^{2+}$ current in mouse eggs were examined to classify channel types and to deduce the function by using whole cell voltage clamp technique. $Ca^{2+}$ currents appeared below -40 mV and reached a maximum at -15 mV (half maximum was -31 mV), then decayed rapidly (inactivation time constant ${\tau}=28.2{\pm}9.59$ ms at -10 mV within 50 ms after the onset of step depolarization. Activation and inactivation of the $Ca^{2+}$ channel was steeply dependent on voltage, in a relatively low range of $-70\;mV{\sim}-10 mV,$ half maximum of activation was -31 mV and that of inactivation was -39 mV, respectively. This current was not decreased significantly by nifedipine, a specific dihydropyridine $Ca^{2+}$ channel blocker in the range of $1\;{\mu}M\;to\;100{\mu}M.$ The inhibitory effect of $Ni^{2+}\;on\;Ca^{2+}$ current was greater than that of $Cd^{2+}.$ The conductance of $Ba^{2+}$ through the channel was equal to or lower than that of $Ca^{2+}$ These results implied that $Ca^{2+}$ current activated at a lower voltage in the mouse egg is carried via a $Ca^{2+}$ channel with similar properties that of the T-type channel.

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Effect of Dopamine on the $Ca^{2+}\;-dependent\;K^+\;currents$ in Isolated Single Gastric Myocytes of the Guinea-pig

  • Rhee, Poong-Lyul;Lee, Sang-Jin;Kim, Sung-Joon;So, In-Suk;Hwang, Sang-Ik;Kim, Ki-Whan
    • The Korean Journal of Physiology
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    • 제27권2호
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    • pp.139-150
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    • 1993
  • We have reported that dopamine potentiates spontaneous contractions dose-dependently in guinea-pig antral circular muscle strips (Hwang et al, 1991). To clarify the underlying excitatory mechanism of dopamine on the gastric smooth muscle, the effects of dopamine on voltage-dependent $Ca^{2+}\;currents\;and\;Ca^{2+}\;-dependent\;K^+\;currents$ were observed in enzymatically dispersed guinea-pig gastric myocytes using the whole-cell voltage-clamp technique. Experiments were also done using isometric tension recording and conventional intracellular microelectrode techniques. 1) The effect of dopamine on the spontaneous contraction of antral circular muscle strips of the guinea-pig was excitatory in a dose-dependent manner, and was blocked by phentolamine, an ${\alpha}-adrenoceptor$ blocker. 2) The slow waves were not changed by dopamine. 3) The voltage-operated inward $Ca^{2+}$ current was not influenced by dopamine. 4) The $Ca^{2+}\;-dependent\;K^+$ outward current, which might reflect the changes of intracellular calcium concentration, was enhanced by dopamine. This effect was abolished by phentolamine. 5) The enhancing effect of dopamine on the $Ca^{2+}\;-dependent\;K^+$ current disappeared with heparin which is known to block the action of $InsP_3$. From these results, it is suggested that dopamine acts via $InsP_3-mediated\;Ca^{2+}$ mobilization from intracellular stores and such action potentiates the spontaneous contraction of guinea-pig gastric smooth muscle.

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A Case of Peritoneal Tuberculosis Developed after Infliximab Therapy for Refractory RA

  • Min, Ji-Yeon;Bang, So-Young;Min, Seung-Yeon;Lee, Dae-Sung;Kim, Bo-Sang;Kim, Jeong-Eun;Lee, Eun-Sung;Pyo, Ju-Yeon;Sohn, Jang-Won;Kim, Tae-Hyung;Lee, Hye-Soon
    • Tuberculosis and Respiratory Diseases
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    • 제73권4호
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    • pp.234-238
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    • 2012
  • Recently, interferon gamma releasing assay has been recommended to compensate the tuberculin skin test (TST) for screening for latent tuberculosis infection (LTBI). Although it improved the detection of LTBI before treatment with tumor necrosis factor blocker, its application to immune suppressed patients is limited. We report a case of peritoneal tuberculosis (TB) developed in a patient who tested positive for TST and QuantiFERON-TB Gold (QFT-G) before infliximab therapy, to emphasize the importance of monitoring during treatment. A 52-year-old woman presented with abdominal distension. She had been diagnosed with seropositive rheumatoid arthritis six years ago. She had started taking infliximab six months ago. All screening tests for TB were performed and the results of all were negative. At admission, the results of repeated TST and QFT-G tests were positive. Histopathological examination confirmed peritoneal TB. The patient started anti-TB therapy and the symptoms were relieved.

Takayasu's Arteritis 환자에서 약에 의해 유발된 치은 비대 (DRUG INDUCED GINGIVAL HYPERPLASIA IN TAKAYASU'S ARTERITIS : DENTAL CONSIDERATION)

  • 김수현;최아미;송제선;김성오;최병재;이효설
    • 대한장애인치과학회지
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    • 제9권1호
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    • pp.36-38
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    • 2013
  • Takayasu's arteritis 환자의 치과 치료 시 침습적인 치과 술식 전 심내막염 가능성을 고려하여 예방적 항생제를 투여한다. 복용 약물에 의해 치은증식이 발생할 수 있으므로 약물의 적용에 관한 의과적 자문이 필요하다.

Risk Factors of On-Pump Conversion during Off-Pump Coronary Artery Bypass Graft

  • Yoon, Sung Sil;Bang, Jung Hee;Jeong, Sang Seok;Jeong, Jae Hwa;Woo, Jong Soo
    • Journal of Chest Surgery
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    • 제50권5호
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    • pp.355-362
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    • 2017
  • Background: Off-pump coronary artery bypass grafting (OPCABG) procedures can avoid the complications of an on-pump bypass. However, some cases unexpectedly require conversion to cardiopulmonary bypass during OPCABG. The risk factors associated with a sudden need for cardiopulmonary bypass were analyzed. Methods: This retrospective study included 283 subjects scheduled for OPCABG from 2001 to 2010. These were divided into an OPCABG group and an on-pump conversion group. Preoperative, operative, and postoperative variables were compared between the 2 groups. Results: Of the 283 patients scheduled for OPCABG, 47 (16%) were switched to on-pump coronary artery bypass grafting (CABG). The mortality of the both the OPCABG and on-pump conversion groups was not significantly different. The major risk factors for conversion to on-pump CABG were congestive heart failure (CHF) (odds ratio [OR], 3.5; p=0.029), ejection fraction (EF) <35% (OR, 4.4; p=0.012), and preoperative beta-blocker (BB) administration (OR, 0.3; p=0.007). The use of intraoperative (p=0.007) and postoperative (p=0.021) inotropics was significantly higher in the conversion group. The amount of postoperative drainage (p<0.001) and transfusion (p<0.001) also was significantly higher in the conversion group. There were no significant differences in stroke or cardiovascular complications between the groups over the course of short-term and long-term follow-up. Conclusion: Patients who undergo OPCABG and have CHF or a lower EF (<35%) are more likely to undergo on-pump conversion, while preoperative BB administration could help prevent conversions from OPCABG to on-pump CABG.

Effects of acidic pH on voltage-gated ion channels in rat trigeminal mesencephalic nucleus neurons

  • Han, Jin-Eon;Cho, Jin-Hwa;Choi, In-Sun;Kim, Do-Yeon;Jang, Il-Sung
    • The Korean Journal of Physiology and Pharmacology
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    • 제21권2호
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    • pp.215-223
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    • 2017
  • The effects of acidic pH on several voltage-dependent ion channels, such as voltage-dependent $K^+$ and $Ca^{2+}$ channels, and hyperpolarization-gated and cyclic nucleotide-activated cation (HCN) channels, were examined using a whole-cell patch clamp technique on mechanically isolated rat mesencephalic trigeminal nucleus neurons. The application of a pH 6.5 solution had no effect on the peak amplitude of voltage-dependent $K^+$currents. A pH 6.0 solution slightly, but significantly inhibited the peak amplitude of voltage-dependent $K^+$ currents. The pH 6.0 also shifted both the current-voltage and conductance-voltage relationships to the depolarization range. The application of a pH 6.5 solution scarcely affected the peak amplitude of membrane currents mediated by HCN channels, which were profoundly inhibited by the general HCN channel blocker $Cs^+$ (1 mM). However, the pH 6.0 solution slightly, but significantly inhibited the peak amplitude of HCN-mediated currents. Although the pH 6.0 solution showed complex modulation of the current-voltage and conductance-voltage relationships, the midpoint voltages for the activation of HCN channels were not changed by acidic pH. On the other hand, voltage-dependent $Ca^{2+}$ channels were significantly inhibited by an acidic pH. The application of an acidic pH solution significantly shifted the current-voltage and conductance-voltage relationships to the depolarization range. The modulation of several voltage-dependent ion channels by an acidic pH might affect the excitability of mesencephalic trigeminal nucleus neurons, and thus physiological functions mediated by the mesencephalic trigeminal nucleus could be affected in acidic pH conditions.

Inhibition of K+ outward currents by linopirdine in the cochlear outer hair cells of circling mice within the first postnatal week

  • Kang, Shin Wook;Ahn, Ji Woong;Ahn, Seung Cheol
    • The Korean Journal of Physiology and Pharmacology
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    • 제21권2호
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    • pp.251-257
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    • 2017
  • Inhibition of $K^+$ outward currents by linopirdine in the outer hair cells (OHCs) of circling mice (homozygous (cir/cir) mice), an animal model for human deafness (DFNB6 type), was investigated using a whole cell patch clamp technique. Littermate heterozygous (+/cir) and ICR mice of the same age (postnatal day (P) 0 -P6) were used as controls. Voltage steps from -100 mV to 40 mV elicited small inward currents (-100 mV~-70 mV) and slow rising $K^+$ outward currents (-60 mV~40 mV) which activated near -50 mV in all OHCs tested. Linopirdine, a known blocker of $K^+$ currents activated at negative potentials ($I_{K,n}$), did cause inhibition at varying degree (severe, moderate, mild) in $K^+$ outward currents of heterozygous (+/cir) or homozygous (cir/cir) mice OHCs in the concentration range between 1 and $100{\mu}m$, while it was apparent only in one ICR mice OHC out of nine OHCs at $100{\mu}m$. Although the half inhibition concentrations in heterozygous (+/cir) or homozygous (cir/cir) mice OHCs were close to those reported in $I_{K,n}$, biophysical and pharmacological properties of $K^+$ outward currents, such as the activation close to -50 mV, small inward currents evoked by hyperpolarizing steps and TEA sensitivity, were not in line with $I_{K,n}$ reported in other tissues. Our results show that the delayed rectifier type $K^+$ outward currents, which are not similar to $I_{K,n}$ with respect to biophysical and pharmacological properties, are inhibited by linopirdine in the developing (P0~P6) homozygous (cir/cir) or heterozygous (+/cir) mice OHCs.

범뇌하수체저하증의 호르몬 대체요법 중단 후 발생한 스트레스 심근병증 (A patient with stress induced cardiomyopathy that occurred after cessation of hormone replacement therapy for panhypopituitarism)

  • 남승완;이준원;심정한;백현성;임창조;임정수;안성균
    • Journal of Yeungnam Medical Science
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    • 제33권2호
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    • pp.125-129
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    • 2016
  • Stress induced cardiomyopathy (SC) is characterized by transient left ventricular (LV) dysfunction in the absence of coronary artery disease. We report on a patient with panhypopituitarism who developed SC resulting from withdrawal of hormonal replacement therapy (HRT). A 52-year-old male visited our hospital for progressively worsening dyspnea. The patient had discontinued HRT 7 days ago, which had been administered for 18 months after transsphenoidal adenomectomy for pituitary macroadenoma. Initial electrocardiogram showed marked sinus bradycardia. Transthoracic echocardiography showed apical ballooning with an LV ejection fraction of 25%. No significant obstructive lesions were observed on coronary angiography. With a clinical diagnosis of SC associated with panhypopituitarism, HRT was restarted, including glucocorticoid and thyroxine, along with standard heart failure management. His LV function had normalized at 2-month follow-up. He remains asymptomatic and administration of beta-blocker and angiotensin converting enzyme inhibitor were discontinued He currently only requires HRT.

The effect of atropine in preventing catheter-related pain and discomfort in patients undergoing transurethral resection due to bladder tumor; prospective randomized, controlled study

  • Sahiner, Yeliz;Yagan, Ozgur;Ekici, Arzu Akdagli;Ekici, Musa;Demir, Emre
    • The Korean Journal of Pain
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    • 제33권2호
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    • pp.176-182
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    • 2020
  • Background: Catheter-related bladder discomfort (CRBD) has been observed in many patients undergoing a urethral catheterization. CRBD may be so severe that the patients require additional analgesics. Muscarinic receptors are involved in the mechanism of CRBD. The aim of this study is to determine the effects of the antimuscarinic properties of atropine, which is frequently used in current practice on CRBD, by comparing it with sugammadex which has no antimuscarinic effects. Methods: Sixty patients selected for transurethral resection due to bladder tumors were randomized into 2 groups: an atropine group and a sugammadex group, with no antimuscarinic effect. The patients were given rocuronium (0.6 mg/kg) as a neuromuscular-blocker. In addition to the frequency and severity of CRBD postoperatively at 0, 1, 6, 12, and 24 hours, postoperative numeric rating scale (NRS) scores, and postoperative nausea and vomiting were examined. Results: The incidence of CRBD was significantly lower in the atropine group in all postoperative measurements. The score was found to be significantly lower in the atropine group when NRS measurements were performed at all time periods (P < 0.01). There was no difference between the groups in terms of nausea and vomiting (P > 0.05). Conclusions: Atropine is a cheap, easy-to-access, safe-to-use drug for reducing CRBD symptoms, without any observed adverse effects. Since it not only reduces CRBD symptoms but also has a positive effect on postoperative pain, it can be used safely to increase patient comfort in patients receiving general anesthesia and a urinary catheter.