• Title/Summary/Keyword: $\beta$-blocker

Search Result 123, Processing Time 0.024 seconds

Occurrence of EDC/PPCPs in Influent and Effluent of a Wastewater Treatment Plant (하수처리장 유입.유출수 내 EDC/PPCPs의 발생 특성)

  • Lee, Min-Ju;Ryu, Jae-Na;Oh, Je-Ill;Kim, Hyun-Bae
    • Journal of Korean Society of Environmental Engineers
    • /
    • v.31 no.9
    • /
    • pp.783-792
    • /
    • 2009
  • This study investigated 31 selected EDCs(Endocrine Disrupting Compounds) and PPCPs(Pharmaceutical and Personal Care Products) in the influent and effluent of a wastewater treatment plant(WWTP) nearby Seoul metropolitan area. The chemical compounds of EDC/PPCPs detected from the plant influent sample include stimulant, X-ray contrast media and fire retardant. The total amount of each compound class were 59.67%, 20.20% and 9.00% respectively. However, in the effluent sample, the major micropolutants detected were oral beta-blocker(30.54%), fire retardant(20.49%), X-ray contrast media(18.17%). The EDC/PPCPs occurrence levels of this study were somewhat lower than previous domestic studies'. When compared to those of overseas, the values were even lower. Some pharmaceutical compound levels particularly measured in European studies were even several thousand times high. This study then compared PECs(Predicted Environmental Concentration) and MECs(Measured Environmental Concentration) of 9 selected pharmaceuticals compounds. The calculated PECs were substantially different with the MECs, while the occurrence order between the PECs and MECs in terms of concentrations of the compounds were similar.

Inhibitory Effects of Potassium Channel Openers on the Oxytocin-induced Contraction of the Rat Uterus in vitro (쥐자궁근의 운동성에 대한 $K^+$채널 개방제의 이완 작용)

  • Kim, Hee-Jeong;Lee, Mun-Han;Ryu, Pan-Dong
    • The Korean Journal of Pharmacology
    • /
    • v.30 no.2
    • /
    • pp.191-203
    • /
    • 1994
  • $K^+$ channel openers (KCOs) are known to have a wide range of effects by opening the $K^+$ channel in plasma membranes of various smooth muscles, cardiac muscle and pancreatic ${\beta}-cell$. In the present study, we investigated the effects of 5 types of KCOs, cromakalim, RP49356, pinacidil, nicorandil and diazoxide on the contractility of isolated rat uterus. All KCOs tested inhibited the uterine contraction induced by 0.2 nM oxytocin in a dose-dependent manner. Individual KCO and its $pD_2$ values were cromakalim 6.5, RP49356 6.3, pinacidil 5.92, nicorandil 4.43 and diazoxide 4.18. The relaxant effects of KCO were inhibited by glibenclamide (0.3, 1 and $10\;{\mu}M$) with $pA_2$ values of cromakalim 6.91, RP49356 6.59, pinacidil 6.55, nicorandil 5.97 and diazoxide 6.37. In addition, the relaxant effect of cromakalim or pinacidil was antagonised by TEA, a non-selective $K^+$ channel blocker, but not by apamin. Contractions induced by low concentration of KCI (< 40 mM) were inhibited by cromakalim $(100{\mu}M)$ and nicorandil $(300{\mu}M)$, but those evoked by higher concentration (> 40 mM) of KCI were little affected. In ovariectomized rat uterus, cromakalim dose-dependently inhibited oxytocin-induced contraction and glibenclamide $(10{\mu}M)$ inhibited the relaxant effect of cromakalim with $pD_2$ and $K_B$ values of 7.48 and $1.26{\times}10^{-7}M$, respectively. In estrogen-primed rat uterus, these values were 6.51 and $1.57{\times}10^{-7}M$, respectively, indicating that the cromakalim is less effective on the estrogen-treated uterine smooth muscle. Our results suggest that the KCO-sensitive $K^+$ channels participate in the motility of uterine smooth muscle and such channels are, at least in part, under the control of estrogen. In addition, our data Indicate that the type of $K^+$ channels activated by KCO is ATP-sensitive $K^+$ channels which is blocked by glibenclamide.

  • PDF

Up-regulation of Heme Oxygenase-1 Expression by cAMP-elevating Agents in RAW 264.7 cells

  • Ko, Young-Shin;Park, Min-Kyu;Kang, Young-Jin;Lee, Young-Soo;Seo, Han-Geuk;Lee, Duck-Hyung;Yunchoi, Hye-Sook;Chong, Won-Seog;Chang, Ki-Churl
    • Biomolecules & Therapeutics
    • /
    • v.10 no.2
    • /
    • pp.71-77
    • /
    • 2002
  • Heme oxygenase-1 (HO-1) is the inducible from of the rate-limiting enzyme of heme degradation; it regulates the cellular contents of heme. HO-1 is up-regulated by various stimuli including oxidative stress so that it is thought to participate in general cellular defense mechanisms against oxidative stress in mammalian cells. To investigate the role of the cAMP-dependent protein kinase A (PKA) signaling pathway on nitrogen oxidative stress-induced HO-1 gene expression, RAW 264.7 cell cultures were treated with sodium nitroprusside (SNP). SNP increased the expression of HO-1 mRNA and protein, time- and concentration-dependently. Treatment with H89, PKA inhibitor, but not LY83583, guanylate cyclase inhibitor, significantly diminished the HO-1 expression by SNP, indicating that cAMP plays a crucial role in the induction of HO-1. Incubation with cAMP-elevating agents, such as forskolin or isoproterenol resulted in up-regulation of the expression of HO-1. Forskolin-induced expression of HO-1 was inhibited by H89. Furthermore, propranolol, $\beta$-adrenoceptor blocker, inhibited the isoproterenol-induced HO-1 expression, supporting the importance of cAMP in the induction of HO-1 expression. Higenamine-S, but not higenamineR, enhanced the HO-1 expression induced by SNP. Furthermore, cellular toxicity induced by hydrogen peroxide was attenuated by the presence of SNP, which was further increased by the presence of ZnPPIX, HO-1 inhibitor. Collectively, these results strongly suggest that up-regulation of HO-1 expression in RAW 264.7 cells involves PKA signal pathway.

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
    • /
    • v.9 no.2
    • /
    • pp.103-108
    • /
    • 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.

Functional Expression of P2Y Receptors in WERI-Rb1 Retinoblastoma Cells

  • Kim, Na-Hyun;Park, Kyu-Sang;Sohn, Joon-Hyung;Yeh, Byung-Il;Ko, Chang-Mann;Kong, In-Deok
    • The Korean Journal of Physiology and Pharmacology
    • /
    • v.15 no.1
    • /
    • pp.61-66
    • /
    • 2011
  • P2Y receptors are metabotropic G-protein-coupled receptors, which are involved in many important biologic functions in the central nervous system including retina. Subtypes of P2Y receptors in retinal tissue vary according to the species and the cell types. We examined the molecular and pharmacologic profiles of P2Y purinoceptors in retinoblastoma cell, which has not been identified yet. To achieve this goal, we used $Ca^{2+}$ imaging technique and western blot analysis in WERI-Rb-1 cell, a human retinoblastoma cell line. ATP ($10\;{\mu}M$) elicited strong but transient $[Ca^{2+}]_i$ increase in a concentration dependent manner from more than 80% of the WERI-Rb-1 cells (n=46). Orders of potency of P2Y agonists in evoking $[Ca^{2+}]_i$ transients were 2MeS-ATP>ATP>>UTP=${\alpha}{\beta}$-MeATP, which was compatible with the subclass of $P2Y_1$ receptor. The $[Ca^{2+}]_i$ transients evoked by applications of 2MeS-ATP and/or ATP were also profoundly suppressed in the presence of $P2Y_1$ selective blocker (MRS 2179; $30\;{\mu}M$). $P2Y_1$ receptor expression in WERI-Rb-1 cells was also identified by using western blot. Taken together, $P2Y_1$ receptor is mainly expressed in a retinoblastoma cell, which elicits $Ca^{2+}$ release from internal $Ca^{2+}$ storage sites via the phospholipase C-mediated pathway. $P2Y_1$ receptor activation in retinoblastoma cell could be a useful model to investigate the role of purinergic $[Ca^{2+}]_i$ signaling in neural tissue as well as to find a novel therapeutic target to this lethal cancer.

Treatment of the Headache (두통의 치료)

  • Chung, Kyung-Cheon
    • Korean Journal of Psychosomatic Medicine
    • /
    • v.7 no.2
    • /
    • pp.263-273
    • /
    • 1999
  • Headache is a symptom with varied etiologies and extraordinarily frequent. Headaches can be a symptom of another diseases, such as meningitis, subarachnoid hemorrhage or brain tumor, may represent the disease entity itself as the case in migraine. The international Headache Society criteria were the first to distinguish between primary and secondary headache disorders. When evaluating a patient who presents with headache, the physician abviously needs to identify or exclude the myriad conditions that can cause secondary headache and initial diagnostic workup should be considered. If patient meets the criteria for a primary headache disorder, treatment commonly initiated without additional neurodiagnostic tests. The headache type, its associated feature, and the duration and the intensity of the pain attack all can influence the choice of acute therapy in migraine. Pharmacologically, such as NSAIDs, combination analgesics, vasoactive antimigraineous drugs, neuroleptics, antidepressants, or corticosteroids. Other approches to managing headache include a headache diary to identify triggers, biofeedback, relaxation technique and behavioral modification. Daily preventive medication should be considered by his attack frequency and intensity, and maintained for 4 to 6 months. Tension-type headaches are distinguished between episodic and chronic tension-type headache, but physician must make sure that patient is not drug-overuse or independent during symptomatic abortive therapy or preventive medication. The most difficult headache patients to treat are those with chronic daily headache. They often have physical dependency, low frustration tolerance, sleep problems, and depression. So discontinuation of overused medication is crucial. New developments in migraine therapy are broadening the scope of abortive and prophylactic treatment choices available to the physician. The enhanced ease of the use of sumatriptan and DHE will likely increase patient compliance and satisfaction.

  • PDF

Characteristics of Occurrence of Pharmaceuticals in the Nakdong River (낙동강 중류수계에서 의약물질의 분포특성)

  • Lee, Sun-Hwa;Jung, Hyun-Wook;Jung, Jin-Young;Min, Hye-Ju;Kim, Bo-Ram;Park, Chan-Gap;Oh, Jeong-Eun;Onoda, Yuu;Satou, Nobuyuki
    • Journal of Korean Society of Environmental Engineers
    • /
    • v.35 no.1
    • /
    • pp.45-56
    • /
    • 2013
  • This study was suggested as fundamental data to control medical materials remained in Nakdong range gauge. The level of Iopromide detected in Nakdong mainstream was $0.0015{\sim}0.37{\mu}g/L$, Mefenamic acid $0.0087{\sim}0.056{\mu}g/L$, Diclofenac $N.D.{\sim}0.01{\mu}g/L$, Atenolol $N.D.{\sim}0.024{\mu}g/L$, Propranolol $N.D.{\sim}0.0038{\mu}g/L$, Lincomycin $0.0005{\sim}0.038{\mu}g/L$, and Trimethoprim $N.D.{\sim}0.0083{\mu}g/L$. At sewage disposal plant in the region, most of them were detected high levels of density. Especially, the level of Iopromide was found the highest up to $5.38{\mu}g/L$. At livestock wasted water disposal plant, the level of lincomycin was detected the highest figure of $477{\mu}g/L$. As a result, medical materials from Nakdong River mainstream got increasing the concentration due to inflow from sewage disposal plant in Gumi and River Geumho in Daegu, which affects residential and industrial areas significantly. Therefore, to control medical materials remained in Nakdong River efficiently, Geumho River and sewage disposal plants shall be continuously monitored and managed, which is recommendable.

Comparison of Multidetector Computed Tomography with Coronary Angiography for Evaluation of Coronary Artery Bypass Grafts (관상동맥조영술과 MDCT를 이용한 관상동맥 이식편의 비교평가)

  • Yoo, Byung-Su;Shin, Yoon-Cheol;Kim, Kun-Il;Kim, Eung-Jung;Chee, Hyun-Keun
    • Journal of Chest Surgery
    • /
    • v.39 no.1 s.258
    • /
    • pp.42-47
    • /
    • 2006
  • Background: The new Multidetector Computed Tomography (MDCT) is useful in visualization of complex coronary artery anatomy. We investigated usefulness comparing of invasive coronary angiography with noninvasive MDCT in judgment of functional degree of coronary arteries grafts after coronary artery bypass graft operation. Material and Method: We analyzed the patency of 52 conduits from 15 patients whom consented to take both 32 Channel MDCT and coronary angiography from November 2003 to November 2004. Comparisons were performed for sensitivity, specificity, positive prediction value and negative prediction value between coronary angiography and 3 dimensional reconstruction image using MDCT. Result: The average graft used was 3.4 $\pm$ 0.8 per patient. Average heart rate during MDCT was 86/minute (Range, 60$\∼$110/minute) without administration of $\beta$-blocker. All patients could hold breath as much as necessary. The average graft patency obtained through corollary angiography was 96.2$\%$. In MDCT group, the sensitivity, the specificity, the positive predictive value and the negative predictive value for diagnosis was 100$\%$, 98.0$\%$, 100$\%$ and 66.6$\%$ respectively. Conclusion: The effectiveness of 32 Channel MDCT may be compared to coronary angiography in grasping about patency and bloodstream of graft conduits after coronary artery bypass graft. Also MDCT has the advantage of noninvasiveness and inexpensiveness compared to coronary angiography.

Inhibitory Effects of Naeso-san on Pacemaker Potentials in Interstitial Cells of Cajal of Murine Small Intestine (생쥐 소장 카할세포의 내향성 향도잡이 전압에 미치는 내소산의 억제효과에 관한 연구)

  • Hong, Noo Ri;Ahn, Tae Seok;Park, Hyun Soo;Chae, Han;Kwon, Young Kyu;Kim, Byung Joo
    • Journal of Physiology & Pathology in Korean Medicine
    • /
    • v.28 no.6
    • /
    • pp.630-635
    • /
    • 2014
  • The purpose of this study was to investigate the effects of Naeso-san in interstitial cells of Cajal (ICCs) in murine small intestine. First, we isolated ICCs from murine small intestine. After that, we cultured these cells for 1 days. The patch-clamp technique was applied on ICCs that formed network-like structures in culture (1 days). Spontaneous rhythms were routinely recorded from cultured ICCs under current-clamp conditions, and the ICCs within networks displayed more robust electrical rhythms (pacemaker potentials). To understand the relationship between Naeso-san and pacemaker activity in ICCs, we examined the effects of Naeso-san on pacemaker potentials of ICCs. In current clamp mode (I = 0), the addition of Naeso-san (10 mg/ml - 50 mg/ml) decreased the amplitude and frequency of the pacemaker potentials of ICCs in a dose dependent manner. However, these effects were blocked by intracellular $GDP{\beta}S$, a G-protein inhibitor, and glibenclamide, a specific ATP-sensitive K+ channels blocker. Pretreatment with SQ-22536, an adenylate cyclase inhibitor, did not block the Naeso-san induced effects, whereas pretreatment with ODQ, a guanylate cyclase inhibitor, or L-NAME, an inhibitor of nitric oxide (NO) synthase blocked the Naeso-san induced effects. Our findings provide insight into unraveling the modulation of Naeso-san in pacemaker potentials of ICCs and developing therapeutic agents against gastrointestinal motility disorders.

Effects of Lemakalim, a Potassium Channel Opener, on the Contractility and Electrical Activity of the Antral Circular Muscle in Guinea-Pig Stomach

  • Kim, Sung-Joon;Jun, Jae-Yeoul;Choi, Youn-Baik;Kim, Ki-Whan;Kim, Woo-Gyeum
    • The Korean Journal of Physiology
    • /
    • v.28 no.1
    • /
    • pp.37-50
    • /
    • 1994
  • Synthetic potassium channel openers (KCOs) are agents capable of opening K-channels in excitable cells. These agents are known to have their maximal potency in the smooth muscle tissue, especially in the vascular smooth muscle. Much attention has been focused on the type of K-channel that is responsible for mediating the effects of KCOs. As the KCO-induced changes are antagonized by glibenclamide, an $K_{ATP}$ (ATP-sensitive K-channel) blocker in the pancreatic ${\beta}-cell,\;K_{ATP}$ was suggested to be the channel responsible. However, there also are many results in favor of other types of K-channel $$(maxi-K,\;small\;conductance\;K_{Ca,}\; SK_{ATP}) mediating the effects of KCOs. Effects of lemakalim, (-)enantiomer of cromakalim (BRL 34915), on the spontaneous contractions and slow waves, were investigated in the antral circular muscle of the guinea-pig stomach. Membrane currents and the effects on membrane currents and single channel activities were also measured in single smooth muscle cells and excised membrane patches by using the patch clamp method. Lemakalim induced hyperpolarization and inhibited spontaneous contractions in a dose-dependent manner. These effects were blocked by glibenclamide and low concentrations of tetraethyl ammonium (< mM). Glibenclamide blocked the effect of lemakalim on the membrane potential and slow waves. The mechanoinhibitory effect of lemakalim was blocked by pretreatment with glibenclamide. In a whole ceIl patch clamp condition, lemakalim largely increased outward K currents. These outward K currents were blocked by TEA, glibenclamide and a high concentration of intracelIular EGTA (10 mM). Volatage-gated Ca currents were not affected by lemakalim. In inside-out patch clamp experiments, lemakalim increased the opening frequency of the large conductance $Ca^{2+}-activated$ K channels $(BK_{Ca},\;Maxi-K).$ From these results, it is suggested that lemakalim induces hyperpolarization by opening K-channels which are sensitive to internal Ca and such a hyperpolarization leads to the inhibition of the spontaneous contraction.

  • PDF