• Title/Summary/Keyword: atenolol

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Balloon dilation of double chambered right ventricle in a dog (우심실 양분증 이환견에 대한 풍선확장술 시술 증례)

  • Kim, Jin-Wook;Yoon, Byung-Gook;Park, Jun-Seok;Kim, Jung-Kuk;Lee, Ki-Ho;Park, Hyung-Jin;Hur, Chan;Seo, Kyoung-Won;Song, Kun-Ho
    • Korean Journal of Veterinary Service
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    • v.40 no.1
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    • pp.67-70
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    • 2017
  • A 4 months old, intact male Shih-tzu was referred to the Veterinary Medical Teaching Hospital of Chungnam National University for evaluation of the cause of cardiac murmur and syncope. Thoracic radiography revealed right-sided cardiomegaly. Echocardiography showed marked hypertrophy of right ventricular free wall and obstruction of right ventricular outflow tract, indicating double chambered right ventricle (DCRV). The dog was medicated with atenolol and sildenafil for DCRV, however, clinical signs did not control by medication. Balloon dilation for DCRV was performed to ameliorate patient's clinical signs. The peak systolic pressure gradient across the obstruction region was decreased and clinical signs was improved by balloon dilation procedure. This is the first case report of balloon dilation for the treatment of canine DCRV in South Korea.

Synthesis of [18F]-Labelled Nebivolol as a β1-Adrenergic Receptor Antagonist for PET Imaging Agent (베타1-아드레날린 수용체를 표적으로 하는 심근영상제로서 18F 표지된 nebivolol의 합성)

  • Kim, Taek-Soo;Park, Jeong Hoon;Lee, Jun Young;Yang, Seung Dae;Chang, Dong-Jo
    • Journal of Radiation Industry
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    • v.10 no.4
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    • pp.181-187
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    • 2016
  • Selective ${\beta}_1$-agonist and antagonists are used for the treatment of cardiac diseases including congestive heart failure, angina pectoris and arrhythmia. Selective ${\beta}_1$-antagonists including nebivolol have high binding affinity on ${\beta}_1$-adrenergic receptor, not ${\beta}_2$-receptor mainly expressed in smooth muscle. Nebivolol is one of most selective ${\beta}_1$-blockers in clinically used ${\beta}_1$-blockers including atenolol and bisoprolol. We tried to develop clinically useful cardiac PET tracers using a selective ${\beta}_1$-blocker. Nebivolol is $C_2$-symmetric and has two chromane moiety with a secondary amino alcohol and aromatic fluorine. We adopted the general synthetic strategy using epoxide ring opening reaction. Unlike formal synthesis of nebivolol, we prepared two chromane building blocks with fluorine and iodine which was transformed to diaryliodonium salt for labelling of $^{18}F$. Two epoxide building blocks were readily prepared from commercially available chromene carboxylic acids (1, 8). Then, the amino alcohol building block (15) was prepared by ammonolysis of epoxide (14) followed by coupling reaction with the other building block, epoxide (7). Diaryliodonium salt, a precursor for $^{18}F$-aromatic substitution, was synthesized in moderate yield which was readily subjected to $^{18}F$-aromatic substitution to give $^{18}F$-labelled nebivolol.

Effects of ${\alpha}_1-Adrenergic$ Stimulation on Membrane Potential, Twitch Force, Intracellular $Na^+,\;and\;H^+$ Activity in Hyperthyroid Guinea Pig Ventricular Muscle (갑상선 기능 항진 기니픽 심근에서 ${\alpha}_1-Adrenergic$ 수용체 자극이 막전위, 수축력 및 세포내 $Na^+$$H^+$ 활성도에 미치는 영향)

  • Kim Jin-Sang;Chae Soo-Wan;Cho Kyu-Park
    • The Korean Journal of Pharmacology
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    • v.31 no.1 s.57
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    • pp.39-51
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    • 1995
  • The roles of ${\beta}-adrenoceptor$ were well known in hyperthyroidal heart, but not with ${\alpha}-adrenoceptor$. So we studied the effects of phenylephrine on membrane potential, intracellular sodium activity ($a^{i}_{Na}$), twitch force, and intracellular pH ($pH_i$) by continuous intracellular recordings with ion-selective and conventional microelectrodes in the papillary muscles of hyperthyroid guinea pig heart. ${\alpha}_1-adrenoceptor$ stimulation by phenylephrine (10^{-5}\;or\;3{\times}10^{-5}M$) produced the following changes: variable changes in action potential duration, a hyperpolarization ($1.5{\pm}0.1mM$) of the diastolic membrane potential, an increase in $a^{i}_{Na}\;(0.4{\pm}0.15mM)$, a stronger positive inotropic effect ($220{\pm}15%$), an increase in $pH_i\;(0.06{\pm}0.002\;unit)$. These changes were flocked by prazosin and atenolol. This indicated that the changes in membrane potential, $a^{i}_{Na}$ twitch force, and $pH_i$ are mediated by a stimulation of the ${\alpha}_1-adrenoceptor$. Ethylisopropylamiloride ($10^{-5}$) also blocked the increase in $a^{i}_{Na}$ and twitch force. On the other hand, strophanthidin, tetrodotoxin, $Cs^+$ or verapamil did not block the increase in $a^{i}_{Na}$ and twitch force. Thus, it was suggested that ${\alpha}_1-adrenoceptor$ stimulation increased $a^{i}_{Na}\;and\;pH_i$ by stimulation of $Na^{+}-H^{+}$ exchange, thereby allowing intracellular alkalinization and $a^{i}_{Na}$ increase. These results were very different from euthyroidal heart which showed ${\alpha}_1-adrenoceptor$-induced decrease in $a^{i}_{Na}$ and initial negative inotropic effect. From the above results, it was concluded that ${\alpha}_1-adrenoceptor$ had a important role in hyperthy-roidal heart.

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The Occurrences of Pharmaceutical and Personal Care Products (PPCPs) in Mankyung River, South Korea (만경강 수중에서 신체보초제품(PPCPS)의 잔류)

  • Kim, Joon-Woo;Kim, Jong-Gu;Jang, Hyo-Sang;Cho, Hyeon-Seo;Takao, Yuji;Arizono, Koji
    • Journal of Environmental Science International
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    • v.18 no.3
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    • pp.245-254
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    • 2009
  • In recent years, environmental pollution by phannaceuticals and personal care products (PPCPs) in the aquatic environment is of great concern worldwide. Recent studies have been reported to occur in a variety of environmental organisms such as surface, drinking and ground water, soils, sediments and hospitals. The purpose of this study was to evaluate the occurrence and environmental behavior of fourteen human PPCPs in surface waters of Mankyung River in South Korea. We were conducted to field survey for water quality and PPCPs analysis at November, 2006. PPCPs were analyzed by liquid chromatograph coupled with a tandem mass spectrometer (HPLC-MS/MS). The concentration of COD was measured to be 2.37$\sim$19.71 mg/L, which was belong to 4$\sim$5 grade in water quality criteria of lake. Station 2 that there is no pollution in upper stream, was appeared to lower concentration. The concentration of TN and TP, that is cause matter of eutrophication, were found to be 7.78$\sim$35.42 mg/L and 0.08$\sim$0.95 mg/L, respectively, which were exceeding 5 grade in Lake water quality criteria. The 11 kind of PPCPs compounds except levofloxacin and triclosan were detected to Mankyung river. PPCPs concentrations of STP(Sewer Treatment Plant) effluents and aquatic environment in Mankyung river have been detected in the range from dozens of ng/L to hundreds of ${\mu}g/L$ that by order of atenolol, carbamazepine, propranolol, Ibuprofen, erythromycin, ifenprodil, clarithromycin, mefenamic acid, fluconazole, indomethacin, disopyramide. PPCPs concentration of Station 1 and 5, which was influenced by Jeonju STP and Wanju STP, was detected high values. Station 2 that there is no pollution, showed lower values. Station 3 which joined Gosan stream and Jeonju stream and station 4 which influenced by stock wastewater was detected to low values.

$\beta$-차단제의 약효검색범

  • 안형수
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1992.05a
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    • pp.47-47
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    • 1992
  • $\beta$수용체에 대한 차단약으로 propranolol이 1964년에 도입된 후, 현재까지 수십여종의 $\beta$-차단약이 개발되었다. 그중 특이 $\beta$1 수용체에 대해 선택적인 억제효과를 지닌 atenolol, metoprolol, betaxolol, celiprolol 및 최근에 bisoprolol 등이 개발되어 임상적으로 부정맥, 협심증, 고혈압의 치료에 사용되고 있다. 그 작용기전으로는 심박출량의 감소, renin 유리억제, 중추억제효과 등이 제시되고 있으나, 이들의 약효검색은 주로 $\beta$1수용체가 많이 존재하는 심장에 대한 억제효과를 중심으로 실시한다. 즉, SHR 및 개를 사용한 생체실험과 심장, 심방 ($\beta$1) 및 기완지, 혈관($\beta$2)을 이용한 적출장기실험을 통하여 isoproterenol에 대한 억제효과를 용량반응 곡선으로 그리고, Van rossum 법에 의해 pA$_2$ 치를 구하여 $\beta$-차단제의 효력을 평가한다. 특히, pA$_2$ 치가 클수록 $\beta$-차단제의 효력이 큰 약물이다. 또한 수용체 결합실험으로 소의 심실 세포막을 분리하여 $^3$H-DHA 와의 결합실험을 통해 해리항수(Kd) 를 측정하고, 이어서 $^3$H-DHA의 일정농도와 함께 미지의 $\beta$-차단제를 여러 농도로 변화시켜 가하여 치환곡선을 작성한다. 여기에서 얻은 치환약의 $IC_{50}$/ 치로부터 치환약의 해리항수(Ki)를 산출한다. 이때 약물과 수용체의 친화력은 해리항수의 역수이므로 해리항수가 적을수록 $\beta$ 수용체에 대한 친화력이 큰 약물이다. 시사되었으며, 이 조직에서 또한 5-$HT_2$와 5-$HT_3$ 수용체의 존재를 확인하고 각각의 기능을 분명히 했다.가 수월하게 하였고 메모리를 동적으로 관리할 수 있게 하였다. 또한 기존의 smpl에 디버깅용 함수 및 설비(facility) 제어용 함수를 추가하여 시뮬레이션 프로그램 작성을 용이하게 하였다. 예를 들면 who_server(), who_queue(), pop_Q(), push_Q(), pop_server(), push_server(), we(), wf(), printfct() 같은 함수들이다. 또한 동시에 발생되는 사건들의 순서를 조종하기 위해, 동시에 발생할 수 있는 각각의 사건에 우선순위를 두어 이 우선 순위에 의하여 사건 리스트(event list)에서 자동적으로 사건들의 순서가 결정되도록 확장하였으며, 설비 제어방식에 있어서도 FIFO, LIFO, 우선 순위 방식등을 선택할 수 있도록 확장하였다. SIMPLE는 자료구조 및 프로그램이 공개되어 있으므로 프로그래머가 원하는 기능을 쉽게 추가할 수 있는 장점도 있다. 아울러 SMPLE에서 새로이 추가된 자료구조와 함수 및 설비제어 방식등을 활용하여 실제 중형급 시스템에 대한 시뮬레이션 구현과 시스템 분석의 예를 보인다._3$", chain segment, with the activation energy of carriers from the shallow trap with 0.4[eV], in he amorphous regions.의 증발산율은 우기의 기상자료를 이용하여 구한 결과 0.05 - 0.10 mm/hr 의 범위로서 이로 인한 강우손실량은 큰 의미가 없음을 알았다.재발이 나타난 3례의 환자를 제외한 9례 (75%)에서는 현재까지 재발소견을 보이지 않고 있다. 이러한 결과는 다른 보고자들과 유사한 결과를 보이고 있지만 아직까지 증례가 많지 않기 때문에 생존율을 얻기에는 미흡한 점이

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Interaction between norepinephrine and angiotensin II on Na+ uptake in primary cultured rabbit renal proximal tubule cells (초대배양한 토끼 신장 근위세뇨관세포의 Na+ uptake에 대한 norepinephrine 과 angiotensin II의 상호작용)

  • Park, Soo-hyun;Koh, Hyun-ju;Han, Ho-jae
    • Korean Journal of Veterinary Research
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    • v.38 no.3
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    • pp.525-534
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    • 1998
  • 신장 근위세뇨관세포들은 사구체에서 여과된 물질의 재흡수, 분비 및 대사에 관여하는 여러 호르몬들의 수용체들을 가지고 있다. 이들중에서 norepinephrine(NE)과 angiotensin II(ANG II)는 $Na^{+}/H^+$ 상호운반계를 조절함으로써 혈압조절에 관여하는 것으로 알려져 있으나 이들의 상호관계에 대해선 연구보고가 많지 않다. 본 연구는 초대배양한 토끼신장 근위세뇨관세포를 이용한 $Na^+$ uptake 실험을 통하여 NE이 어떠한 수용체를 통하여 $Na^{+}/H^+$ 상호운반계를 조절하는지 그리고 이러한 작용에 있어서 NE과 ANG II의 상호관계를 알아보고자 실시하였다. NE(>$10^{-9}M$)은 $Na^+$ uptake를 유의성 있게 증가시켰다($10^{-9}M$ NE : $27{\pm}4%$ increase vs. Control;p < 0.05). $\alpha$ 길항제(phentolamine, $10^{-10}M$)는 NE($10^{-9}M$)에 의해 유도된 $Na^+$ uptake를 유의성 있게 차단하였으나 (phentolamine+NE : $29{\pm}5%$ inhibition vs. NE ; p〈 0.05), ${\alpha}_1$ (pra-zosin, $10^{-10}M$) 및 ${\alpha}_2$ 길항제(yohimbine, $10^{-10}M$)는 부분적으로 차단하였다. ${\beta}$ 길항제(propra-nolol, $10^{-10}M$)도 역시 NE에 의해 유도된 $Na^+$ uptake를 유의성 있게 차단하였으나(propranolol+NE : $24{\pm}6%$ inhibition vs. NE ; p< 0.05), ${\beta}_1$(atenolol, $10^{-10}M$) 및 ${\beta}_2$ 길항제(butoxamine, $10^{-10}M$)는 부분적으로 차단하였다. 이러한 결과들은 NE에 의해 유도된 $Na^+$ uptake 증가작용은 ${\alpha}$(${\alpha}_1$${\alpha}_2$ )와 ${\beta}$(${\beta}_1$${\beta}_2$) 수용체 모두를 통하여 일어난다는 것을 시사해주고 있다. ANG II($10^{-11}M$) 또는 NE(${\alpha}_1$, ${\alpha}_2$, ${\beta}_1$, ${\beta}_2$ 작동제) 단독처리군의 $Na^+$ uptake는 대조군에 비해 유의성 있게 증가하였으나 (ANG II : $23{\pm}9%$ increase vs. Control; p < 0.05), 병합처리시 상승작용은 나타나지 않았다. ${\alpha}$ 또는 ${\beta}$ 길항제 처리시 NE 및 ANG II에 의해 유도되었던 $Na^+$ uptake 증가는 유의성 있게 차단되었다(phentolamine+NE+ANG II : $25{\pm}3%$ inhibition, propranolol+NE+ANG II : $24{\pm}6%$ inhibition vs. NE+ANG II, respectively ; p〈 0.05). 이 결과들은 $Na^+$ uptake에 있어서 ${\alpha}$(${\alpha}_1$${\alpha}_2$)와 ${\beta}$(${\beta}_1$${\beta}_2$) 수용체와 ANG II의 관련성을 시사해 준다. 결론적으로 토끼 신장 근위세뇨관세포에서 NE은 ${\alpha}_1$, ${\alpha}_2$, ${\beta}_1$${\beta}_2$ 수용체를 통하여 $Na^+$+ uptake를 증가시켰으며 이들 수용체는 ANG II $Na^+$ uptake 증가작용에 관여하였다.

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Simultaneous analysis of β-lactam antibiotics and β-blockers by LC-MS/MS (LC-MS/MS를 이용한 베타락탐계 항생제와 베타차단제의 동시분석)

  • Son, Bo-young;Kim, Jun-il;An, Chi-hwa;Lee, Su-won;Kim, Bogsoon;Chung, Deukmo
    • Analytical Science and Technology
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    • v.29 no.4
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    • pp.179-185
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    • 2016
  • An effective analytical method has been developed for the determination of β-blockers(atenolol, metoprolol and propranolol) and 6 β-lactams(amoxicillin, penicillin G, cefaclor, cefadroxil, cephalexin and cephradine) in water samples using two different cartridges. The samples were extracted by solid-phase extraction (SPE) with the usage of polymeric hydrophile-lipophile balance(HLB cartridges) and strong cation-exchange mixed-mode polymeric sorbent (MCX cartridges). A XDB-C18 column(1.8 μm; 3.0 mm × 100 mm) was used for the sufficient chromatographic resolution. The calibration curves showed good linearity with high correlation coefficients (>0.995). The method detection limits (MDL) and the limits of quantification(LOQ) were from 1.1 to 3.9 ng/L and from 5 to 13 ng/L, respectively. The method was applied for the determination of the target compounds in tributaries and raw water of the Han River and these were found at N.D. to 0.209 μg/L.