• 제목/요약/키워드: beta blocker

검색결과 123건 처리시간 0.02초

Ginsenoside Re inhibits pacemaker potentials via adenosine triphosphate-sensitive potassium channels and the cyclic guanosine monophosphate/nitric oxide-dependent pathway in cultured interstitial cells of Cajal from mouse small intestine

  • Hong, Noo Ri;Park, Hyun Soo;Ahn, Tae Seok;Kim, Hyun Jung;Ha, Ki-Tae;Kim, Byung Joo
    • Journal of Ginseng Research
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    • 제39권4호
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    • pp.314-321
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    • 2015
  • Background: Ginseng belongs to the genus Panax. Its main active ingredients are the ginsenosides. Interstitial cells of Cajal (ICCs) are the pacemaker cells of the gastrointestinal (GI) tract. To understand the effects of ginsenoside Re (GRe) on GI motility, the authors investigated its effects on the pacemaker activity of ICCs of the murine small intestine. Methods: Interstitial cells of Cajal were dissociated from mouse small intestines by enzymatic digestion. The whole-cell patch clamp configuration was used to record pacemaker potentials in cultured ICCs. Changes in cyclic guanosine monophosphate (cGMP) content induced by GRe were investigated. Results: Ginsenoside Re ($20-40{\mu}M$) decreased the amplitude and frequency of ICC pacemaker activity in a concentration-dependent manner. This action was blocked by guanosine 50-[${\beta}-thio$]diphosphate [a guanosine-5'-triphosphate (GTP)-binding protein inhibitor] and by glibenclamide [an adenosine triphosphate (ATP)-sensitive $K^{+}$ channel blocker]. To study the GRe-induced signaling pathway in ICCs, the effects of 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one (a guanylate cyclase inhibitor) and RP-8-CPT-cGMPS (a protein kinase G inhibitor) were examined. Both inhibitors blocked the inhibitory effect of GRe on ICC pacemaker activity. L-NG-nitroarginine methyl ester ($100{\mu}M$), which is a nonselective nitric oxide synthase (NOS) inhibitor, blocked the effects of GRe on ICC pacemaker activity and GRe-stimulated cGMP production in ICCs. Conclusion: In cultured murine ICCs, GRe inhibits the pacemaker activity of ICCs via the ATP-sensitive potassium ($K^{+}$) channel and the cGMP/NO-dependent pathway. Ginsenoside Re may be a basis for developing novel spasmolytic agents to prevent or alleviate GI motility dysfunction.

녹내장 환자의 불안과 우울에 관한 연구 (Anxiety and Depression Levels in Patients with Glaucoma)

  • 김종원
    • 정신신체의학
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    • 제3권2호
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    • pp.166-173
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    • 1995
  • 저자는 녹내장환자의 정신과적 문제를 조사해 보고자 안과 외래에서 통원 치료중인 녹내장환자 38명의 불안과 우울정도를 STAI의 T-A와 BDI를 이용하여 측정, 37명의 정상 대조군과 비교하였으며, 성별, 연령, 학력, 종교, 결혼 상태에 따른 차이, 치료방법, 치료기간, 병합된 신체질환과의 관계들을 조사하여 다음과 같은 결과를 얻었다. 1) 연령, 학력, 종교, 결혼상태에 따른 불안 및 우울점수의 유의한 차이는 없었다. 2) 불안점수는 녹내장환자군과 정상 대조군사이에 유의한 차이가 없었으며 여자 환자의 불안이 정상 대조군에 비해 높은 경향을 보였다. 3) 녹내장환자는 정상 대조군에 비해 여자에서 우울점수가 유의하게 높았으며 (p < .01) 남자에서는 차이가 없었다. 4) 녹내장환자의 18.4%(남자환자의 10.5%, 여자환자의 26.4%)가 우울증으로 추정되며 28.9%(남자환자의 10.5%, 여자환자의 47.4%)가 우울한 경향을 보이고 있었다. 5) 베타 차단제 투여나 신체 질환의 유무, 또한 치료기간과 우울 증상의 유의한 상관관계는 없었다. 6) 녹내장환자에게 심리적 부담이 되는 요소로는 실명할 가능성에 대한 두려움, 매일 안약을 사용하거나 투약을 해야 하는 점 등이었다.

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실험견에서 Metoprolol 약리효과의 약동/력학적 검토 (Pharmacokinetic/Pharmacodynamic Analysis of Metoprolol in Dogs)

  • 오동진;장인진;이경훈;임동석;김형기;신상구;박찬웅;신재국
    • 대한약리학회지
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    • 제31권2호
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    • pp.251-259
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    • 1995
  • Pharmacokinetics and pharmacodynamics of metoprolol, a selective beta-l blocker, were examined for 360 minutes after intravenous bolus administration of metoprolol to 6 dogs. Plasma concentration and excreted amount in the urine metoprolol were measured by liquid chromatography with fluorescence detection. PR interval and heart rate were measured by ECG monitoring. Blood pressure was monitored through intraarterial catheter in femoral artery and cardiac output by thermodilution method using Swan-Ganz catheter. To analyze the effect site concentration-response relationship, plasma concentration and pharmacological effects were simultaneously fitted to a two pharmacokinetic compartment linked to pharmacodynamic model with NONLIN program. Results are as follows. 1) The plasma concentration of metoprolol after intrvenous injection decreased biexponentially. The terminal half-life estimated was $1.33{\pm}0.40$ hours and the volume of distribution at steady state (Vdss) and the total body clearance were $1.04{\pm}0.4\;L/kg,\;6.55{\pm}2.21\;L/hr$, respectively. The central compartment volume of distribution and peripheral compartment volume of distribution were $0.35{\pm}0.14L/kg\;and\;0.69{\pm}0.34L/kg$. The renal clearance and intercompartment clearance were $0.53{\pm}0.25\;L/min\;and\;0.35{\pm}0.19\;L/min$. 2) Simulated biophase concentration-response curve shows hyperbolic relationship and the estimated concentration-effect relationship was best explained by Emax model when the prolongation of PR interval and the reduction of the heart rate were used as pharmacodynamic parameters. Emax and EC50 were estimated to be $26.3{\pm}4.7\;msec\;and\;88.8{\pm}82.3\;g/ml$ for PR interval, and $48.7{\pm}18.8\;beats/min\;and\;113.5{\pm}78.7\;ng/ml$ for heart rate, respectively. 3) The changes of cardiac output-effect site concentration relationship was best fitted by a linear model and the slope of the relationship was $0.005{\pm}0.003$. Diastolic blood pressure-effect site concentration relationship was also explained by the linear model and the slope of the relationship was $0.038{\pm}0.034$.

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