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A non-steroidal anti-inflammatory drug (NSAID) has many adverse effects including cardiovascular (CV) risk. Diclofenac among the nonselective NSAIDs has the highest CV risk such as congestive heart failure, which resulted commonly from the impaired cardiac pumping due to a disrupted excitation- contraction (E-C) coupling. We investigated the effects of diclofenac on the L-type calcium channels which are essential to the E-C coupling at the level of single ventricular myocytes isolated from neonatal rat heart, using the whole-cell voltage-clamp technique. Only diclofenac of three NSAIDs, including naproxen and ibuprofen, significantly reduced inward whole cell currents. At concentrations higher than 3μM, diclofenac inhibited reversibly the Na＋ current and did irreversibly the L-type Ca2＋ channels-mediated inward current (IC50=12.89±0.43μM) in a dose-dependent manner. However, nifedipine, a well-known L-type channel blocker, effectively inhibited the L-type Ca2＋ currents but not the Na＋ current. Our finding may explain that diclofenac causes the CV risk by the inhibition of L-type Ca2＋ channel, leading to the impairment of E-C coupling in cardiac myocytes.

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기사명 저자명 페이지 원문 목차
Altered gene expression in cerulein-stimulated pancreatic acinar cells :pathologic mechanism of acute pancreatitis Ji Hoon Yu ;Joo Weon Lim ;Hyeyoung Kim pp.409-416

Hexane-soluble fraction of the common fig, Ficus carica, inhibits osteoclast differentiation in murine bone marrow-derived macrophages and RAW 264.7 cells Young Ran Park ;Jae Soon Eun ;Hwa Jung Choi ;Manoj Nepal ;Dae Keun Kim ;Seung-Yong Seo ;Rihua Li ;Wo pp.417-424

The antinociceptive effect of sigma-1 receptor antagonist, BD1047, in a capsaicin induced headache model in rats Young Bae Kwon ;Young Chan Jeong ;Jung Kee Kwon ;Ji Seon Son ;Kee Won Kim pp.425-429

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Diclofenac, a non-steroidal anti-inflammatory drug, inhibits L-type Ca^2+^ channels in neonatal rat ventricular cardiomyocytes Oleg V. Yarishkin ;Eun Mi Hwang ;Donggyu Kim ;Jae Cheal Yoo ;Sang Soo Kang ;Deok Ryoung Kim ;Jae-Hee pp.437-442

Electrically-evoked neural activities of rd1 mice retinal ganglion cells by repetitive pulse stimulation Sang Baek Ryu ;Jang Hee Ye ;Jong Seung Lee ;Yong Sook Goo ;Chi Hyun Kim ;Kyung Hwan Kim pp.443-448

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Intraocular injection of muscimol induces illusory motion reversal in goldfish Sang-Yoon Lee ;Chang-Sub Jung pp.469-473

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Efficient management design for swimming exercise treatment Kyunghun Kim ;Taewon Kyung ;Wonhyun Kim ;Chungsick Shin ;Youngjae Song ;Moo Yeol Lee ;Hyunwoo Lee ;Y pp.497-502

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참고문헌 (41건) : 자료제공( 네이버학술정보 )

참고문헌 목록에 대한 테이블로 번호, 참고문헌, 국회도서관 소장유무로 구성되어 있습니다.
번호 참고문헌 국회도서관 소장유무
1 Involvement of ATP-sensitive K + channels in the peripheral antinociceptive effect induced by dipyrone 네이버 미소장
2 Sildenafil increases diclofenac antinociception in the formalin test 네이버 미소장
3 The L-type calcium channel in the heart: the beat goes on. 네이버 미소장
4 Diclofenac toxicity to hepatocytes: a role for drug metabolism in cell toxicity. 네이버 미소장
5 Renal effects of cyclooxygyenase-2-selective inhibitors. 네이버 미소장
6 Dissociation Between Ionic Remodeling and Ability to Sustain Atrial Fibrillation During Recovery From Experimental Congestive Heart Failure 네이버 미소장
7 Physiological Basis for Contractile Dysfunction in Heart Failure 네이버 미소장
8 Doering CJ, Zamponi GW. Molecular pharmacology of high voltage- activated calcium channels. J Bioenerg and Biomem 35: 491−505, 2003. 미소장
9 The non-steroidal anti-inflammatory drug, diclofenac, inhibits Na + current in rat myoblasts 네이버 미소장
10 Contractions in guinea-pig ventricular myocytes triggered by a calcium-release mechanism separate from Na+ and L-currents. 네이버 미소장
11 Regulation of contraction and relaxation by membrane potential in cardiac ventricular myocytes 네이버 미소장
12 An Optimized Protocol for Culture of Cardiomyocyte from Neonatal Rat 네이버 미소장
13 COX-2 inhibitors, other NSAIDs, and cardiovascular risk: the seduction of common sense. 네이버 미소장
14 "Voltage-activated Ca release" in rabbit, rat and guinea-pig cardiac myocytes, and modulation by internal cAMP 네이버 미소장
15 Electrocardiography of the Failing Heart 네이버 미소장
16 Contribution of a voltage-sensitive calcium release mechanism to contraction in cardiac ventricular myocytes. 네이버 미소장
17 Hudson M, Rahme E, Richard H, Pilote L. Risk of congestive heart failure with nonsteroidal anti-inflammatory drugs and selective cyclooxygenase 2 inhibitors: a class effect? Arthritis and Rheumatism 57: 516−523, 2007. 미소장
18 L-type Ca2+ currents in ventricular myocytes from neonatal and adult rats. 네이버 미소장
19 Do Selective Cyclo-Oxygenase-2 Inhibitors And Traditional Non-Steroidal Anti-Inflammatory Drugs Increase The Risk Of Atherothrombosis? Meta-Analysis Of Randomised Trials 네이버 미소장
20 Quantitative Analysis of the Expression and Distribution of Calcium Channel α 1 Subunit mRNA in the Atria and Ventricles of the Rat Heart 네이버 미소장
21 Diclofenac inhibition of sodium currents in rat dorsal root ganglion neurons 네이버 미소장
22 Nickel Block of Three Cloned T-Type Calcium Channels: Low Concentrations Selectively Block α1H 네이버 미소장
23 No effect of short term ranitidine intake on diclofenac pharmacokinetics. 네이버 미소장
24 Calcium content of the sarcoplasmic reticulum in isolated ventricular myocytes from patients with terminal heart failure. 네이버 미소장
25 Liu LY, Fei XW, Li ZM, Zhang ZH, Mei YA. Diclofenac, a nonsteroidal anti-inflammatory drug, activates the transient outward K＋ current in rat cerebellar granule cells. Neuropharmacol 48: 918−926, 2005. 미소장
26 Down-regulation of sodium current in chronic heart failure: effect of long-term therapy with carvedilol. 네이버 미소장
27 Cardiovascular risk and inhibition of cyclooxygenase: a systematic review of the observational studies of selective and nonselective inhibitors of cyclooxygenase 2. 네이버 미소장
28 Effects of clonixin on the electrical activity of cardiac pacemaker cells 네이버 미소장
29 Morales MA, Salazar T, Paeile C. Effects of flunixin and mefenamic acid on cardiac pacemaker cells. Structure-activity relationship and comparison with clonixin. Gen Pharmacol 24: 775−780, 1993. 미소장
30 Open state block by fendiline of L-type Ca++ channels in ventricular myocytes from rat heart. 네이버 미소장
31 Pharmacological evidence for the activation of K + channels by diclofenac 네이버 미소장
32 Perez-Reyes E. Molecular characterization of a novel family of low voltage-activated, T-type, calcium channels. J Bioenerg Biomem 30: 313−318, 1998. 미소장
33 Molecular characterization of two members of the T-type calcium channel family. 네이버 미소장
34 Ca2+ Handling and Sarcoplasmic Reticulum Ca2+ Content in Isolated Failing and Nonfailing Human Myocardium 네이버 미소장
35 Electrical remodeling in ischemia and infarction 네이버 미소장
36 A sodium-channel mutation causes isolated cardiac conduction disease. 네이버 미소장
37 Mechanism of diclofenac analgesia: direct blockade of inflammatory sensitization 네이버 미소장
38 Waksman JC, Brody A, Phillips SD. Nonselective nonsteroidal anti-inflammatory drugs and cardiovascular risk: are they safe? Ann Pharmacother 41: 1163−1173, 2007. 미소장
39 Willis JV, Kendall MJ, Flinn RM, Thornhill DP, Welling PG. The pharmacokinetics of diclofenac sodium following intravenous and oral administration. Eur J Clin Pharmacol 16: 405−410, 1979. 미소장
40 An inactivation stabilizer of the Na+ channel acts as an opportunistic pore blocker modulated by external Na+. 네이버 미소장
41 Regulation of a voltage-sensitive release mechanism by Ca^2^+-calmodulin-dependent kinase in cardiac myocytes 네이버 미소장

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