• Title/Summary/Keyword: nicardipine

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Mechanism of Catecholamine Secretion Evoked by Lithium from the Isolated Perfused Rat Adrenal Gland (흰쥐 적출관류부신에서 리튬에 의한 카테콜아민 분비작용의 기전)

  • Lim, Dong-Yoon;Kim, Cheol;Oh, Hyeong-Geun
    • The Korean Journal of Pharmacology
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    • v.32 no.3
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    • pp.357-371
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    • 1996
  • Lithium (Li) is known to be used not only during acute manic psychosis but also acute depressive phase in manic-depression. In the present study, it was attempted to investigate the effect of lithium on catecholamine (CA) secretion from the isolated perfused rat adrenal gland and to clarify the mechanism of its action. Replacement of $Na^+$ (118.4 mM) by lithium in the normal Krebs-bicarbonate solution used to perfuse the gland produced gradually an increased response in the spontaneous catecholamine release, which was peaked at $30{\sim}60$ min after its perfusion. Li-Krebs solution was perfused into an adrenal vein for 2 hours in every experiments. Li-Krebs-evoked CA secretory responses were depressed significantly under loading with $Ca^{++}-free$ medium. This CA secretion evoked by lithium loading was also reduced markedly by the pretreatment with nicardipine ($10^{-6}$ M), TMB-8 ($10^{-5}$ M) and chlorisondamine ($10^{-6}$ M) for 20 min, respectively, while was not affected by preloading with a pirenzepine ($2{\times}10^{-6}$ M)-containing Krebs. $Na^+$ pump inhibition by pretreatment with ouabain ($10^{-4}$ M) for 20 min did make the marked depression in Li-evoked CA secretory responses. Moreover, Li-evoked CA release was also diminished markedly by preloading with tetrodotoxin ($5{\times}10^{-7}$ M)-contaming Krebs for 20 min. All these experimental results taken together suggest that lithium enhances CA secretion in a $Ca^{++}$-dependent fashion by its accumulation in the adrenomedullary chromaffin cells of the rat, and that this secretory effect may be meidated by a dual mechanism: (i) chromaffin cell depolarization and subsequent opening of voltage-sensitive $Ca^{++}$ channels and (ii) activation of a $[Li]_i-[Ca]_0$ counter-transport system.

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The Mode of Action of Pentazocine on Catecholamine Secretion from the Perfused Rat Adrenal Medulla (흰쥐 관류부신에서 Pentazocine의 카테콜아민 분비작용의 기전)

  • Lim, Dong-Yoon;Kim, Bong-Han;Heo, Jae-Bong;Choi, Cheo-Hee;Kim, Jin-Ho;Jang, Young;Lee, Jae-Joon
    • The Korean Journal of Pharmacology
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    • v.30 no.3
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    • pp.299-311
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    • 1994
  • The present study was attempted to investigate whether pentazocine, which is known to possess both opioid agonistic and antagonistic properties, produces catecholamines (CA) secretion from the isolated perfused rat adrenal gland, and to establish the mechanism of its action, and also to compare its action with that of some opioids. Pentazocine (30 to 300 ug) injected into an adrenal vein caused a dose-dependent secretory response of CA from the rat adrenal medulla. The pentazocine-evoked secretion of CA was remarkably diminished by the preloading with chlorisondamine $(10^{-6}\;M)$, naloxone $(1.22{\times}10^{-7}\;M)$, morphine $(1.7{\times}10^{-5}\;M)$, met-enkephalin $(9.68{\times}10^{-6}\;M)$, nicardipine $(10^{-6}\;M)$ and TMB-8 $(10^{-5}\;M)$ while was not influenced by the pretreatment of pirenzepine $(2{\times}10^{-6}\;M)$. The perfusion of $Ca^{++}$-free Krebs solution for 30 min into the gland also led to the marked reduction in CA secretion evoked by pentazocine. Furthermore, the CA release evoked by ACh and/or DMPP was greatly inhibited by the pretreatment with pentazocine $(1.75{\times}10^{-4}\;M)$ for 20 min. From these experimental results, it is thought that pentazocine causes markedly the increased secretion of CA from the isolated perfused rat adrenal medulla by a calcium-dependent exocytotic mechanism. The secretory effect of pentazocine appears to be mediated through activation of opioid receptors located on adrenal chromaffin cells, which may be also associated with stimulation of cholinergic nicotinic receptors.

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ATM Cell Encipherment Method using Rijndael Algorithm in Physical Layer (Rijndael 알고리즘을 이용한 물리 계층 ATM 셀 보안 기법)

  • Im Sung-Yeal;Chung Ki-Dong
    • The KIPS Transactions:PartC
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    • v.13C no.1 s.104
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    • pp.83-94
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    • 2006
  • This paper describes ATM cell encipherment method using Rijndael Algorithm adopted as an AES(Advanced Encryption Standard) by NIST in 2001. ISO 9160 describes the requirement of physical layer data processing in encryption/decryption. For the description of ATM cell encipherment method, we implemented ATM data encipherment equipment which satisfies the requirements of ISO 9160, and verified the encipherment/decipherment processing at ATM STM-1 rate(155.52Mbps). The DES algorithm can process data in the block size of 64 bits and its key length is 64 bits, but the Rijndael algorithm can process data in the block size of 128 bits and the key length of 128, 192, or 256 bits selectively. So it is more flexible in high bit rate data processing and stronger in encription strength than DES. For tile real time encryption of high bit rate data stream. Rijndael algorithm was implemented in FPGA in this experiment. The boundary of serial UNI cell was detected by the CRC method, and in the case of user data cell the payload of 48 octets (384 bits) is converted in parallel and transferred to 3 Rijndael encipherment module in the block size of 128 bits individually. After completion of encryption, the header stored in buffer is attached to the enciphered payload and retransmitted in the format of cell. At the receiving end, the boundary of ceil is detected by the CRC method and the payload type is decided. n the payload type is the user data cell, the payload of the cell is transferred to the 3-Rijndael decryption module in the block sire of 128 bits for decryption of data. And in the case of maintenance cell, the payload is extracted without decryption processing.

A Clinical Study of Renal Abscesses in Children (소아 신농양의 임상적 고찰)

  • Hwang You-Sik;Rhie Young-Jun;Ahn Sun-Young;Han Sang-Won;Lee Jae-Seung
    • Childhood Kidney Diseases
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    • v.9 no.1
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    • pp.64-68
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    • 2005
  • Purpose : Renal abscess is very rare in children and its diagnosis is difficult because symptoms are often nonspecific. In previous studies, on]y 15% to 25% of patients were reported to be diagnosed at the time of admission. Early diagnosis and treatment are important be cause mortality rate correlates positively with the time of diagnosis. The purpose of this study is to clarify the clinical features of children with renal abscess and to investigate the possible indicators of this disease for early diagnosis and Proper treatment. Methods : Twelve children diagnosed with renal abscess from Jan. 1996 to Jul. 2004 were included. The age of patients ranged from S months to 15 years. We retrospectively analyzed the demographics of patients, their symptoms, predisposing factors, diagnostic methods and causative organisms and the treatment modalities. Results : Fever was the most common manifestation, Five children(42%) had vesicoureteral reflux. Renal ultrasonography and computerized tornography were the most frequently used imaging tools to detect renal abscess. Gram negative bacteria were isolated in 7 patients and Staphylococcus aureus grew in 2 patients. All patients received intravenous antibiotics and 4 patients underwent aspiration or drainage of renal abscess. The average admission duration was 30 days. Conclusion : Renal abscess should be included in the differential diagnosis of prolonged fever in children, especially when flank pain is combined. For early diagnosis and a better prognosis, patients should be promptly investigated with ultrasonography or computerized tomography.

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An Experience of Therapeutic Plasma Exchange in 9 Pediatric Patients (소아에서 시행한 치료적 혈장교환술 9례의 임상적 고찰)

  • Lee Jee-Hyun;Jeon Ga-Won;Park Sung-Eun;Jin Dong-Kyu;Paik Kyung-Hoon
    • Childhood Kidney Diseases
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    • v.9 no.1
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    • pp.38-45
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    • 2005
  • Purpose : The purpose of this study was to analyze the therapeutic effect of plasmapheresis in various pediatric diseases. Methods : Therapeutic plasmapheresis was performed by COBE Spectra centrifugation. Nine cases were included in this study. The number an[;. method of plasmapheresis, together with the progress and prognosis of each case were retrospectively reviewed. Results : The patients' ages ranged from 26 mont]Is to 16 years of age, and the mean age was 9.9 years. There were S males and 4 females. The underlying diseases requiring plasmapheresis included 2 cases of hemolytic uremic svndrome(HUS), 1 case of lupus nephritis, 2 cases of rapidly Progressive glomerulonephritis(RPGN), 1 case of focal segmental glomorulosclerosis(FSGS), 1 case of systemic vasculitis after pulmonary hemorrhage, 1 case of acute renal failure associated with pulmonary hemoIThage, and 1 case of acute rejection after renal transplantation. The average number of plasmapheresis performed was 6.2 times with a range of 3 to 13 times. The patients with HUS, lupus nephritis, ANCA positive systemic vasculitis induced by pulmonary hemorrhage and ARF-associated pulmonary hemorrhage showed a good response to therapeutic plasmapheresis, but the patients with RPGN, refractory FSGS, and acute rejection after renal transplantation were not responsive to treatment. The most common side effect was hypocalcemia which was rarely symptomatic. Vital signs were not compromised. Conclusion : Although it is presumptuous to generalize the therapeutic effects of plasma pheresis in different diseases due to the small number of study subjects, this study shows that plasmapheresis may be an effective therapeutic modality in various pediatrics diseases and should be considered as a therapeutic option.

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Effect of Various Divalent Ions on the Calcium Current of Adrenal Medullary Chromaffin Cells in the Rat

  • Kim, Jun;Leem, Chae-Hun;Kim, Sang-Jeong
    • The Korean Journal of Physiology
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    • v.26 no.2
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    • pp.113-122
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    • 1992
  • It is well known that chromaffin cells of adrenal medulla secrete catecholamine in response to sympathetic nerve activation and the influx of $Ca^{2+}$ through the voltage dependent $Ca^{2+}$ channels (VDCC) in the cell membrane do a major role in this secretory process. In this study, we explored the effect of divalent cations on VDCC of rat chromaffin cells. Rat (Sprague-Dawley rat, 150-250 gm) chromaffin cells were isolated and cultured. Standard giga seal, whole cell recording techniques were employed to study $Ca^{2+}$ current with external and internal solutions that could effectively isolate VDCC currents $(NMG\;in\;external\;and\;TEA\;and\;Cs^{2+}\;in\;internal\;solution)$. The voltage dependence and the inactivation time course of VDCC in our cells were identical to those of bovine chromaffin cells. A persistent inward current was first activated by depolarizing step pulse from the holding potential (H.P.) of -80 mV to -40 mV, increased to maximum amplitude at around +10 mV, and became smaller with progressively higher depolarizing pulses to reverse at around +60 mV. The inactivation time constant $(\tau)$, fitted from the long duration test potential (2 sec) was $1295.2{\pm}126.8$ msec $(n=20,\;1\;day\;of\;culture,\;mean\;{\pm}S.E.M.)$ and the kinetic parameters were not altered along the culture duration. Nicardipine $(10\;{\mu}M)$ blocked the current almost completely. Among treated divalent cations such as $Cd^{2+},\;Co^{2+},\;Ni^{2+},\;Zn^{2+}\;and\;,Mn^{2+},\;Cd^{2+}$ was the most potent blocker on VDCC. When the depolarizing step pulse from -80 mV to 10 mV was applied, the equilibrium dissociation constant $(K_d)$ of $Cd^{2+}\;was\;39\;{\mu}M,\;K_d\;of\;Co^{2+}\;was\;100\;{\mu}M\;and\;K_d\;of\;Ni^{2+}];was];780{\mu}M.$ The principal findings of this study are as follows. First, the majority of $Ca^{2+}$ channels in rat chromaffin cells are well classified to L-type $Ca^{2+}$ channel in the view of kinetics and pharmacology. Second, all divalent cations tested could block the $Ca^{2+}$ current and the most potent blocker among the tested was $Cd^{2+}$.

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Regulation of L-type Calcium Channel Current by Somatostatin in Guinea-Pig Gastric Myocytes

  • Kim, Young-Chul;Sim, Jae-Hoon;Lee, Sang-Jin;Kang, Tong-Mook;Kim, Sung-Joon;Kim, Seung-Ryul;Youn, Sei-Jin;Lee, Sang-Jeon;Xu, Wen Xie;So, In-Suk;Kim, Ki-Whan
    • The Korean Journal of Physiology and Pharmacology
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    • v.9 no.2
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    • pp.103-108
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    • 2005
  • To study the direct effect of somatostatin (SS) on calcium channel current ($I_{Ba}$) in guinea-pig gastric myocytes, $I_{Ba}$ was recorded by using whole-cell patch clamp technique in single smooth muscle cells. Nicardipine ($1{\mu}M$), a L-type $Ca^{2+}$ channel blocker, inhibited $I_{Ba}$ by $98{\pm}1.9$% (n=5), however $I_{Ba}$ was decreased in a reversible manner by application of SS. The peak $I_{Ba}$ at 0 mV were decreased to $95{\pm}1.5$, $92{\pm}1.9$, $82{\pm}4.0$, $66{\pm}5.8$, $10{\pm}2.9$% at $10^{-10}$, $10^{-9}$, $10^{-8}$, $10^{-7}$, $10^{-5}$ M of SS, respectively (n=3∼6; $mean{\pm}SEM$). The steady-state activation and inactivation curves of $I_{Ba}$ as a function of membrane potentials were well fitted by a Boltzmann equation. Voltage of half-activation ($V_{0.5}$) was $-12{\pm}0.5$ mV in control and $-11{\pm}1.9$ mV in SS treated groups (respectively, n=5). The same values of half-inactivation were $-35{\pm}1.4$ mV and $-35{\pm}1.9$ mV (respectively, n=5). There was no significant difference in activation and inactivation kinetics of $I_{Ba}$ by SS. Inhibitory effect of SS on $I_{Ba}$ was significantly reduced by either dialysis of intracellular solution with $GDP_{\beta}S$, a non-hydrolysable G protein inhibitor, or pretreatment with pertussis toxin (PTX). SS also decreased contraction of guinea-pig gastric antral smooth muscle. In conclusion, SS decreases voltage-dependent L-type calcium channel current ($VDCC_L$) via PTXsensitive signaling pathways in guinea-pig antral circular myocytes.

Gintonin facilitates catecholamine secretion from the perfused adrenal medulla

  • Na, Seung-Yeol;Kim, Ki-Hwan;Choi, Mi-Sung;Ha, Kang-Su;Lim, Dong-Yoon
    • The Korean Journal of Physiology and Pharmacology
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    • v.20 no.6
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    • pp.629-639
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    • 2016
  • The present study was designed to investigate the characteristics of gintonin, one of components isolated from Korean Ginseng on secretion of catecholamines (CA) from the isolated perfused model of rat adrenal gland and to clarify its mechanism of action. Gintonin (1 to $30{\mu}g/ml$), perfused into an adrenal vein, markedly increased the CA secretion from the perfused rat adrenal medulla in a dose-dependent fashion. The gintonin-evoked CA secretion was greatly inhibited in the presence of chlorisondamine ($1{\mu}M$, an autonomic ganglionic bloker), pirenzepine ($2{\mu}M$, a muscarinic $M_1$ receptor antagonist), Ki14625 ($10{\mu}M$, an $LPA_{1/3}$ receptor antagonist), amiloride (1 mM, an inhibitor of $Na^+/Ca^{2+}$ exchanger), a nicardipine ($1{\mu}M$, a voltage-dependent $Ca^{2+}$ channel blocker), TMB-8 ($1{\mu}M$, an intracellular $Ca^{2+}$ antagonist), and perfusion of $Ca^{2+}$-free Krebs solution with 5mM EGTA (a $Ca^{2+}$chelater), while was not affected by sodium nitroprusside ($100{\mu}M$, a nitrosovasodialtor). Interestingly, LPA ($0.3{\sim}3{\mu}M$, an LPA receptor agonist) also dose-dependently enhanced the CA secretion from the adrenal medulla, but this facilitatory effect of LPA was greatly inhibited in the presence of Ki 14625 ($10{\mu}M$). Moreover, acetylcholine (AC)-evoked CA secretion was greatly potentiated during the perfusion of gintonin ($3{\mu}g/ml$). Taken together, these results demonstrate the first evidence that gintonin increases the CA secretion from the perfused rat adrenal medulla in a dose-dependent fashion. This facilitatory effect of gintonin seems to be associated with activation of LPA- and cholinergic-receptors, which are relevant to the cytoplasmic $Ca^{2+}$ increase by stimulation of the $Ca^{2+}$ influx as well as by the inhibition of $Ca^{2+}$ uptake into the cytoplasmic $Ca^{2+}$ stores, without the increased nitric oxide (NO). Based on these results, it is thought that gintonin, one of ginseng components, can elevate the CA secretion from adrenal medulla by regulating the $Ca^{2+}$ mobilization for exocytosis, suggesting facilitation of cardiovascular system. Also, these findings show that gintonin might be at least one of ginseng-induced hypertensive components.

The Evaluation of Potential Hepatotoxicity by Calcium Channel Blockers, Renin-Angiotensin System Blockade and Diuretics (칼슘채널차단제, 레닌-안지오텐신시스템 차단제, 이뇨제의 잠재적 간독성 평가)

  • Kim, Jae Yun;Lee, Ok Sang;Jung, Sun Hoi;Lee, Hye-Suk;Lee, Chang Ho;Kim, Sang Geon;Lim, Sung Cil
    • Korean Journal of Clinical Pharmacy
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    • v.22 no.4
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    • pp.330-339
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    • 2012
  • Background : Hypertension is treated with both lifestyle modification and pharmacotherapy. The Seventh Report of the Joint National Committee on Detection, Evaluation, and Treatment of High Blood Pressure (JNC-7), published in 2003, provides a streamlined management approach to hypertension for the primary care physician. The JNC-7 is the gold standard also in Korea. According to the JNC-7, special therapeutic considerations are recommended for high-risk individuals with compelling indications. The presence of compelling indications in any given patient should be considered when selecting specific pharmacotherapy to treat hypertension. However, in patients with compelling indications, it is unknown that hepatotoxicity is caused by Calcium Channel Blocker (CCB), one of 1st anti-hypertensive drugs. Now, the CCB is the most used 1st anti-hypertensive drug in Korea Therefore, we evaluated the changes in blood liver function parameters (ALT, AST, Total bilirubin, serum albumin) for the study group. Methods : We randomly collected and retrospectively analyzed Electronic Medical Record data (n=28,788) of patients, and who took calcium channel blockers(non-dihydropyridines; diltiazem, verapamil, dihydropyridines; amlodipine, barnidipine, benidipine, clinidipine, efonidipine, felodipine, isradipine, lacidipine, lercanidipine, nicardipine, nifedipine, nimodipine), with having liver function tests (LFTs) from July 1st 2009 to June 30th 2010 at the Seoul National University Hospital in Korea. Control groups are two antihypertensive agents: RAS blockade (ARB; candesartan, irbesartan, losartan, olmesartan, telmisartan, valsartan, ACE-I; cilazapril, enalapril, fosinopril, imidapril, perindopril, ramipril) and, Diuretics (loop; furosemide, torsemide, thiazide; hydrochlorothiazide[HCTZ], indapamide). Patients not having LFT results at these three standard points of time(baseline, during, medication, and after finishing medication) were excluded. The collected data were analyzed by using the SPSS (Version12.0) and Microsoft Excel (Version2007). Results : 711 patients who were treated CCB (297), RAS blockade (232) or Diuretics (182) monotherapy were selected for the study. In selected patients, liver damage degree(changes of each LFTs value) was higher in diuretics group than other groups, followed by RAS blockade and CCB. In diuretics group's was loop-diuretics group was higher than thiazide-diuretics group. In CCB group, Nondihydropyridine-CCB's damage degree was higher than Dihydropyrine-CCB's that. Conclusions : Despite the limitations due to the retrospective study, among patients with abnormal LFTs, the use of CCBs led to a less liver damage than other 1st anti-hypertensive agents. It can be recommended CCBs as one of the initial treatments of hypertension in patients with liver disease.

Regulation of $Ba^{2+}$-Induced Contraction of Murine Ureteral Smooth Muscle

  • Kim, Young-Chul;Lee, Moo-Yeol;Kim, Wun-Jae;Myung, Soon-Chul;Choi, Woong;Kim, Chan-Hyung;Xu, Wen-Xie;Kim, Seung-Ryul;Lee, Sang-Jin
    • The Korean Journal of Physiology and Pharmacology
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    • v.11 no.5
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    • pp.207-213
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    • 2007
  • This study was designed to characterize ureteral smooth muscle motility and also to study the effect of forskolin(FSK) and isoproterenol(ISO) on smooth muscle contractility in murine ureter. High $K^+$(50 mM) produced tonic contraction by $0.17{\pm}0.06mN$(n=19). Neuropeptide and neurotransmitters such as serotonin($5{\mu}M$), histamine($20{\mu}M$), and carbarchol(CCh, $10{\sim}50{\mu}M$) did not produce significant contraction. However, CCh($50{\mu}M$) produced slow phasic contraction in the presence of 25 mM $K^+$. Cyclopiazonic acid(CPA, $10{\mu}M$), SR $Ca^{2+}$-ATPase blocker, produced tonic contraction(0.07 mN). Meanwhile, inhibition of mitochondria by protonophore carbnylcyanide m-chlorophenylhydrazone(CCCP) also produced weak tonic contraction(0.01 mN). The possible involvement of $K^+$ channels was also pursued. Tetraethyl ammonium chloride(TEA, 10 mM), glibenclamide($10{\mu}M$) and quinidine($20{\mu}M$) which are known to block $Ca^{2+}$-activated $K^+$ channels($K_{Ca}$ channel), ATP-sensitive $K^+$ channels($K_{ATP}$) and nonselective $K^+$ channel, respectively, did not elicit any significant effect. However, $Ba^{2+}$($1{\sim}2mM$), blocker of inward rectifier $K^+$ channels($K_{IR}$ channel), produced phasic contraction in a reversible manner, which was blocked by $1{\mu}M$ nicardipine, a blocker of dehydropyridine-sensitive voltage-dependent L-type $Ca^{2+}$ channels($VDCC_L$) in smooth muscle membrane. This $Ba^{2+}$-induced phasic contraction was significantly enhanced by $10{\mu}M$ cyclopiazonic acid(CPA) in the frequency and amplitude. Finally, regulation of $Ba^{2+}$-induced contraction was studied by FSK and ISO which are known as adenylyl cyclase activator and $\beta$-adrenergic receptor agonist, respectively. These drugs significantly suppressed the frequency and amplitude of $Ba^{2+}$-induced contraction(p<0.05). These results suggest that $Ba^{2+}$ produces phasic contraction in murine ureteral smooth muscle which can be regulated by FSK and $\beta$-adrenergic stimulation.