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      KCI등재 SCIE SCOPUS

      Gastroprokinetic agent, mosapride inhibits 5-HT3 receptor currents in NCB-20 cells

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      https://www.riss.kr/link?id=A106341941

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      다국어 초록 (Multilingual Abstract)

      Mosapride accelerates gastric emptying by acting on 5-hydroxytryptamine type 4 (5-HT4) receptor and is frequently used in the treatment of gastrointestinal (GI) disorders requiring gastroprokinetic efficacy. We tested the effect of mosapride on 5-hydroxytryptamine type 3 (5-HT3) receptor currents because the 5-HT3 receptors are also known to be expressed in the GI system and have an important role in the regulation of GI functions. Using the whole-cell voltage clamp method, we compared the currents of the 5-HT3 receptors when 5-HT was applied alone or was co-applied with mosapride in cultured NCB-20 cells known to express 5-HT3 receptors. The 5-HT3 receptor current amplitudes were inhibited by mosapride in a concentration-dependent manner. Mosapride blocked the peak currents evoked by the application of 5-HT in a competitive manner because the EC50 shifted to the right without changing the maximal effect. The rise slopes of 5-HT3 receptor currents were decreased by mosapride. Pre-application of mosapride before co-application, augmented the inhibitory effect of mosapride, which suggests a closed channel blocking mechanism. Mosapride also blocked the opened 5-HT3 receptor because it inhibited the 5-HT3 receptor current in the middle of the application of 5-HT. It accelerated desensitization of the 5-HT3 receptor but did not change the recovery process from the receptor desensitization. There were no voltage-, or use-dependency in its blocking effects. These results suggest that mosapride inhibited the 5-HT3 receptor through a competitive blocking mechanism probably by binding to the receptor in closed state, which could be involved in the pharmacological effects of mosapride to treat GI disorders.
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      Mosapride accelerates gastric emptying by acting on 5-hydroxytryptamine type 4 (5-HT4) receptor and is frequently used in the treatment of gastrointestinal (GI) disorders requiring gastroprokinetic efficacy. We tested the effect of mosapride on 5-hydr...

      Mosapride accelerates gastric emptying by acting on 5-hydroxytryptamine type 4 (5-HT4) receptor and is frequently used in the treatment of gastrointestinal (GI) disorders requiring gastroprokinetic efficacy. We tested the effect of mosapride on 5-hydroxytryptamine type 3 (5-HT3) receptor currents because the 5-HT3 receptors are also known to be expressed in the GI system and have an important role in the regulation of GI functions. Using the whole-cell voltage clamp method, we compared the currents of the 5-HT3 receptors when 5-HT was applied alone or was co-applied with mosapride in cultured NCB-20 cells known to express 5-HT3 receptors. The 5-HT3 receptor current amplitudes were inhibited by mosapride in a concentration-dependent manner. Mosapride blocked the peak currents evoked by the application of 5-HT in a competitive manner because the EC50 shifted to the right without changing the maximal effect. The rise slopes of 5-HT3 receptor currents were decreased by mosapride. Pre-application of mosapride before co-application, augmented the inhibitory effect of mosapride, which suggests a closed channel blocking mechanism. Mosapride also blocked the opened 5-HT3 receptor because it inhibited the 5-HT3 receptor current in the middle of the application of 5-HT. It accelerated desensitization of the 5-HT3 receptor but did not change the recovery process from the receptor desensitization. There were no voltage-, or use-dependency in its blocking effects. These results suggest that mosapride inhibited the 5-HT3 receptor through a competitive blocking mechanism probably by binding to the receptor in closed state, which could be involved in the pharmacological effects of mosapride to treat GI disorders.

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      참고문헌 (Reference)

      1 Wade PR, "Use of stereoisomers of zacopride to analyze actions of 5-hydroxytryptamine on enteric neurons" 260(1 Pt 1) : G80-G90, 1991

      2 박용수, "Tricyclic antidepressant amitriptyline inhibits 5-hydroxytryptamine 3 receptor currents in NCB-20 cells" 대한약리학회 22 (22): 585-595, 2018

      3 Machu TK, "Therapeutics of 5-HT3 receptor antagonists : current uses and future directions" 130 : 338-347, 2011

      4 Gershon MD, "The serotonin signaling system : from basic understanding to drug development for functional GI disorders" 132 : 397-414, 2007

      5 Snyders D, "The heart and cardiovascular system: scientific foundations, vol. 2" Raven Press 1992

      6 Mawe GM, "Serotonin signalling in the gut--functions, dysfunctions and therapeutic targets" 10 : 473-486, 2013

      7 Thompson AJ, "Recent developments in 5-HT3 receptor pharmacology" 34 : 100-109, 2013

      8 Lazaraki G, "Recent advances in pharmacological treatment of irritable bowel syndrome" 20 : 8867-8885, 2014

      9 Galligan JJ, "Multiple mechanisms of fast excitatory synaptic transmission in the enteric nervous system" 81 : 97-103, 2000

      10 Curran MP, "Mosapride in gastrointestinal disorders" 68 : 981-991, 2008

      1 Wade PR, "Use of stereoisomers of zacopride to analyze actions of 5-hydroxytryptamine on enteric neurons" 260(1 Pt 1) : G80-G90, 1991

      2 박용수, "Tricyclic antidepressant amitriptyline inhibits 5-hydroxytryptamine 3 receptor currents in NCB-20 cells" 대한약리학회 22 (22): 585-595, 2018

      3 Machu TK, "Therapeutics of 5-HT3 receptor antagonists : current uses and future directions" 130 : 338-347, 2011

      4 Gershon MD, "The serotonin signaling system : from basic understanding to drug development for functional GI disorders" 132 : 397-414, 2007

      5 Snyders D, "The heart and cardiovascular system: scientific foundations, vol. 2" Raven Press 1992

      6 Mawe GM, "Serotonin signalling in the gut--functions, dysfunctions and therapeutic targets" 10 : 473-486, 2013

      7 Thompson AJ, "Recent developments in 5-HT3 receptor pharmacology" 34 : 100-109, 2013

      8 Lazaraki G, "Recent advances in pharmacological treatment of irritable bowel syndrome" 20 : 8867-8885, 2014

      9 Galligan JJ, "Multiple mechanisms of fast excitatory synaptic transmission in the enteric nervous system" 81 : 97-103, 2000

      10 Curran MP, "Mosapride in gastrointestinal disorders" 68 : 981-991, 2008

      11 Miyake A, "Molecular cloning of human 5-hydroxytryptamine3 receptor : heterogeneity in distribution and function among species" 48 : 407-416, 1995

      12 Neijt HC, "Kinetics of the membrane current mediated by serotonin 5-HT3 receptors in cultured mouse neuroblastoma cells" 411 : 257-269, 1989

      13 Wu ZS, "Ion channels gated by acetylcholine and serotonin : structures, biology, and drug discovery" 36 : 895-907, 2015

      14 Nemeth PR, "Interactions between serotonin and cisapride on myenteric neurons" 108 : 77-83, 1985

      15 Fakhfouri G, "Impact of 5-HT3 receptor antagonists on peripheral and central diseases" 17 : 741-747, 2012

      16 Nemeth PR, "Gastrointestinal motility stimulating drugs and 5-HT receptors on myenteric neurons" 166 : 387-391, 1989

      17 Longstreth GF, "Functional bowel disorders" 130 : 1480-1491, 2006

      18 Zheng Y, "Efficacy and safety of 5-hydroxytryptamine 3 receptor antagonists in irritable bowel syndrome : a systematic review and meta-analysis of randomized controlled trials" 12 : e0172846-, 2017

      19 Gunthorpe MJ, "Diltiazem causes open channel block of recombinant 5-HT3 receptors" 519 Pt 3 : 713-722, 1999

      20 Karasawa T, "Comparison of gastrokinetic effects of AS-4370, cisapride and BRL24924" 183 : 2181-, 1990

      21 Akuzawa S, "Comparison of [3H]YM060 binding to native and cloned rat 5-HT3 receptors" 296 : 227-230, 1996

      22 Holbrook JD, "Characterisation of 5-HT3C, 5-HT3D and 5-HT3E receptor subunits : evolution, distribution and function" 108 : 384-396, 2009

      23 Morales M, "Cellular and subcellular immunolocalization of the type 3 serotonin receptor in the rat central nervous system" 36 : 251-260, 1996

      24 Nayak SV, "Calcium changes induced by presynaptic 5-hydroxytryptamine-3 serotonin receptors on isolated terminals from various regions of the rat brain" 91 : 107-117, 1999

      25 van Hooft JA, "Allosteric potentiation of the 5-HT3 receptor-mediated ion current in N1E-115 neuroblastoma cells by 5-hydroxyindole and analogues" 36 : 649-653, 1997

      26 Zhou Q, "Alcohols potentiate the function of 5-HT3 receptor-channels on NCB-20 neuroblastoma cells by favouring and stabilizing the open channel state" 507(Pt 2) : 335-352, 1998

      27 Yoshikawa T, "Affinity of mosapride citrate, a new gastroprokinetic agent, for 5-HT4 receptors in guinea pig ileum" 77 : 53-59, 1998

      28 Yoshida N, "AS-4370, a new gastrokinetic agent, enhances upper gastrointestinal motor activity in conscious dogs" 257 : 781-787, 1991

      29 Sugita S, "5-hydroxytryptamine is a fast excitatory transmitter at 5-HT3 receptors in rat amygdala" 8 : 199-203, 1992

      30 Walstab J, "5-HT3 receptors : role in disease and target of drugs" 128 : 146-169, 2010

      31 Thompson AJ, "5-HT3 receptors" 12 : 3615-3630, 2006

      32 Gregory RE, "5-HT3 receptor antagonists for the prevention of chemotherapy-induced nausea and vomiting. A comparison of their pharmacology and clinical efficacy" 55 : 173-189, 1998

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      연월일 이력구분 이력상세 등재구분
      2023 평가예정 해외DB학술지평가 신청대상 (해외등재 학술지 평가)
      2020-04-29 학술지명변경 외국어명 : THE KOREAN JOURNAL OF Physiology & Pharmacology -> The Korean Journal of Physiology & Pharmacology KCI등재
      2020-01-01 평가 등재학술지 유지 (해외등재 학술지 평가) KCI등재
      2011-01-01 평가 등재학술지 유지 (등재유지) KCI등재
      2009-01-01 평가 등재학술지 유지 (등재유지) KCI등재
      2007-01-01 평가 등재학술지 유지 (등재유지) KCI등재
      2006-10-12 학술지명변경 한글명 : 대한 생리.약리학회지 -> The Korean Journal of Physiology & Pharmacology
      외국어명 : THE KOREAN JOURNAL OF Physilogy & Pharmacology -> THE KOREAN JOURNAL OF Physiology & Pharmacology
      KCI등재
      2004-01-01 평가 등재학술지 선정 (등재후보2차) KCI등재
      2003-01-01 평가 등재후보 1차 PASS (등재후보1차) KCI등재후보
      2001-07-01 평가 등재후보학술지 선정 (신규평가) KCI등재후보
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      기준연도 WOS-KCI 통합IF(2년) KCIF(2년) KCIF(3년)
      2016 1.85 0.36 1.29
      KCIF(4년) KCIF(5년) 중심성지수(3년) 즉시성지수
      1.05 0.9 0.575 0.09
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