The Effects of 5-HT4 Receptor Agonist, Mosapride Citrate, on Visceral Hypersensitivity in a Rat Model

被引:4
|
作者
Lee, Jae Woong [2 ]
Sung, Ki Woon [3 ]
Lee, Oh Young [4 ]
Lee, Seo Eun [3 ,5 ]
Sohn, Chong Il [1 ]
机构
[1] Sungkyunkwan Univ, Sch Med, Kangbuk Samsung Hosp, Div Gastroenterol,Dept Internal Med, Seoul 110746, South Korea
[2] Hanil Gen Hosp, Div Gastroenterol, Seoul, South Korea
[3] Hanyang Univ, Coll Med, Dept Physiol, Seoul 133791, South Korea
[4] Hanyang Univ, Coll Med, Dept Internal Med, Seoul 133791, South Korea
[5] Hanyang Univ, Grad Sch Biomed Sci & Engn, Dept Biomed Sci, Seoul 133791, South Korea
关键词
Mosapride citrate; Colorectal distension; Visceral hypersensitivity; Irritable bowel; IRRITABLE-BOWEL-SYNDROME; IN-VITRO; INHIBITORY CONTROLS; ABDOMINAL-PAIN; COLORECTAL DISTENSION; RECTAL DISTENSION; SENSITIVITY; SEROTONIN; COLON; TEGASEROD;
D O I
10.1007/s10620-012-2101-z
中图分类号
R57 [消化系及腹部疾病];
学科分类号
摘要
Mosapride citrate is known to affect gastric motility. However, whether mosapride citrate has any effect on visceral pain in the colon or rectum is not certain. The aim of this study was to assess the effects of mosapride citrate on visceral pain in a rat visceral hypersensitivity model. The perception of visceral pain was evaluated by the visceromotor response to colorectal distension observed on electromyographs of the abdominal musculature in urethane-anesthetized rats. Visceral hypersensitivity was induced by the intrarectal instillation of 4% acetic acid or 1.5% zymosan. Mosapride citrate was administered intraperitoneally 3 h later. VMRs to CRD were recorded prior to the instillation of acetic acid or zymosan and before and after mosapride citrate treatment. The intracolonic instillation of acetic acid resulted in a significant increase in VMRs of the abdominal muscles to CRD, compared with the pretreatment state (174 +/- A 24%, P < 0.05). The intracolonic instillation of zymosan resulted in a significant increase in VMRs of the abdominal muscles to CRD, compared with the pretreatment state (144 +/- A 9%, P < 0.05). Intraperitoneal injection of mosapride citrate resulted in a significant reduction in the VMRs to CRD in an acetic acid-induced visceral hypersensitivity rat model (61 +/- A 9%, P < 0.05). The intraperitoneal injection of mosapride citrate also resulted in a significant reduction in the VMRs to CRD in a zymosan-induced visceral hypersensitivity rat model (67 +/- A 9%, P < 0.05). Mosapride citrate diminished visceral pain in rats.
引用
收藏
页码:1517 / 1524
页数:8
相关论文
共 50 条
  • [41] Effects of 5-HT2B, 5-HT3 and 5-HT4 receptor antagonists on gastrointestinal motor activity in dogs
    Morita, Hiroki
    Mochiki, Erito
    Takahashi, Nobuyuki
    Kawamura, Kiyoshi
    Watanabe, Akira
    Sutou, Toshinaga
    Ogawa, Atsushi
    Yanai, Mitsuhiro
    Ogata, Kyoichi
    Fujii, Takaaki
    Ohno, Tetsuro
    Tsutsumi, Souichi
    Asao, Takayuki
    Kuwano, Hiroyuki
    WORLD JOURNAL OF GASTROENTEROLOGY, 2013, 19 (39) : 6604 - 6612
  • [42] Safety Profile of Tegaserod, a 5-HT4 Receptor Agonist, for the Treatment of Irritable Bowel Syndrome
    William L. Hasler
    Philip Schoenfeld
    Drug Safety, 2004, 27 : 619 - 631
  • [43] The 5-HT4 receptor antagonist ML10375 inhibits the constitutive activity of human 5-HT4(c) receptor
    Blondel, O
    Gastineau, M
    Langlois, M
    Fischmeister, R
    BRITISH JOURNAL OF PHARMACOLOGY, 1998, 125 (04) : 595 - 597
  • [44] Clinical Pharmacokinetics of Tegaserod, a Serotonin 5-HT4 Receptor Partial Agonist with Promotile Activity
    Silke Appel-Dingemanse
    Clinical Pharmacokinetics, 2002, 41 : 1021 - 1042
  • [45] Cognitive effects of SL65.0155, a serotonin 5-HT4 receptor partial agonist, in animal models of amnesia
    Micale, Vincenzo
    Leggio, Gian Marco
    Mazzola, Carmen
    Drago, Filippo
    BRAIN RESEARCH, 2006, 1121 : 207 - 215
  • [46] A Multivalent Approach to the Design and Discovery of Orally Efficacious 5-HT4 Receptor Agonists
    McKinnell, R. Murray
    Armstrong, Scott R.
    Beattie, David T.
    Choi, Seok-Ki
    Fatheree, Paul R.
    Gendron, Roland A. L.
    Goldblum, Adam
    Humphrey, Patrick P.
    Long, Daniel D.
    Marquess, Daniel G.
    Shaw, J. P.
    Smith, Jacqueline A. M.
    Turner, S. Derek
    Vickery, Ross G.
    JOURNAL OF MEDICINAL CHEMISTRY, 2009, 52 (17) : 5330 - 5343
  • [47] Structure of the human serotonin 5-HT4 receptor gene and cloning of a novel 5-HT4 splice variant
    Bender, E
    Pindon, A
    van Oers, I
    Zhang, YB
    Gommeren, W
    Verhasselt, P
    Jurzak, M
    Leysen, J
    Luyten, W
    JOURNAL OF NEUROCHEMISTRY, 2000, 74 (02) : 478 - 489
  • [48] Investigations on 5-HT4 Receptor Expression and Effects of Tegaserod on Human Platelet Aggregation In Vitro
    Serebruany, Victor L.
    El Mouelhi, Mohamed
    Pfannkuche, Hans-Juergen
    Rose, Kristine
    Marro, Martin
    Angiolillo, Dominick J.
    AMERICAN JOURNAL OF THERAPEUTICS, 2010, 17 (06) : 543 - 552
  • [49] The in vitro pharmacological profile of TD-5108, a selective 5-HT4 receptor agonist with high intrinsic activity
    Smith, J. A. M.
    Beattie, D. T.
    Marquess, D.
    Shaw, J. -P.
    Vickery, R. G.
    Humphrey, P. P. A.
    NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY, 2008, 378 (01) : 125 - 137
  • [50] The in vitro pharmacological profile of TD-5108, a selective 5-HT4 receptor agonist with high intrinsic activity
    J. A. M. Smith
    D. T. Beattie
    D. Marquess
    J.-P. Shaw
    R. G. Vickery
    P. P. A. Humphrey
    Naunyn-Schmiedeberg's Archives of Pharmacology, 2008, 378 : 125 - 137