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Effects of 5-HT4 selective receptor agonist, mosapride citrate on electrocardiogram in dogs

  • Chae, Ji Sang;Ahn, Jin Ok;Coh, Ye Rin;Park, Chong Woo;Youn, Hwa Young
    • Korean Journal of Veterinary Research
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    • v.52 no.3
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    • pp.163-167
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    • 2012
  • Mosapride stimulated dietary motility was introduced because of the arrhythmogenic effect of cisapride. Cisapride, 5-HT receptor agonist, induces prolongation of QT interval. Additionally, this condition can raise the possibility of acute, "malignant" arrhythmias such as torsade de pointes. It is hard to find any reports about effects of mosapride on cardiac parameters in dogs. By confirming electrocardiogram (ECG) parameters, the surface extremity leads ECG that was obtained from the four-limb electrodes and which was recorded by an ECG recorder after administration of mosapride 3 mg/kg PO b.i.d, and mosapride 3 mg/kg with itraconazole 5 mg/kg PO b.i.d, respectively. QT interval was shortened on the days of 3, 5, and post-day 1 in both mosapride 3 mg/kg administrated group and mosapride with itraconazole group. Heart rate increased significantly. QTc was slightly prolonged in mosapride administration group and mosapride with itraconazole group. However, all dogs of QTc were in normal variation (150~250 msec). Besides, the dogs showed no side effects reported in human medicine during the administration with these drugs. Although mosapride can increase the heart rate, this study suggest that mosapride may be useful for the dogs with disorders of gastrointestinal motility because of no fatal arrhythmogenic effect inspite of administration with itraconazole in dogs.

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

  • Park, Yong Soo;Sung, Ki-Wug
    • The Korean Journal of Physiology and Pharmacology
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    • v.23 no.5
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    • pp.419-426
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    • 2019
  • Mosapride accelerates gastric emptying by acting on 5-hydroxytryptamine type 4 ($5-HT_4$) 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 ($5-HT_3$) receptor currents because the $5-HT_3$ 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 $5-HT_3$ receptors when 5-HT was applied alone or was co-applied with mosapride in cultured NCB-20 cells known to express $5-HT_3$ receptors. The $5-HT_3$ 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 $EC_{50}$ shifted to the right without changing the maximal effect. The rise slopes of $5-HT_3$ 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 $5-HT_3$ receptor because it inhibited the $5-HT_3$ receptor current in the middle of the application of 5-HT. It accelerated desensitization of the $5-HT_3$ 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 $5-HT_3$ 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.

Synergic Effect of Trimebutine Combined with Mosapride on Gastrointestinal Dysfunction and Visceral Pain Induced in Stress Models

  • Park, Young-Joon;Park, Yong-Sul;Chung, Zoo-Chul;Nam, Yun-Sung;Chung, Yoon-Hee;Cho, Kwan-Hyung;Choi, Sung-Up;Sohn, Uy-Dong;Park, Eon-Sub;Je, Hyun-Dong;Lee, Choong-Ho;Lee, Moo-Yeol;Jeong, Ji-Hoon
    • Biomolecules & Therapeutics
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    • v.19 no.1
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    • pp.84-89
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    • 2011
  • The present study was undertaken to determine whether combined treatment with prokinetic trimebutine and mosapride has a synergic effect on gastrointestinal motility and visceral pain associated with gastrointestinal dysfunction. To develop effective gastroprokinetic agents with greater potencies than trimebutine or mosapride for the treatment of gastrointestinal tract disease, a mixture of trimebutine and mosapride was designed and prepared. In the present study, treatment with trimebutine alone showed a dose-dependent effect on propelling movements of normal small and large intestine in mice, whereas mosapride effected only small intestine motility. Co-administration of trimebutine with mosapride, a well-established prokinetic drug, produced a synergistic influence on normal small intestine motility, but demonstrated an unclear effect on large intestine motility, with a slight tendency to reduce the propelling time. In a stress model, the small and large intestine motilities were significantly decreased. The reduction of intestine motility was restored to a normal level and the restoring effect was more pronounced in the combined treatment with trimebutine plus mosapride than treatment with trimebutine or mosapride alone. Furthermore, treatment with trimebutine plus mosapride significantly decreased acute visceral pain which was not controlled by trimebutine or mosapride alone. These data suggest that combination therapy with trimebutine plus mosapride has a synergic effect on small and large intestine motility and visceral pain control in gastrointestinal disorders.

Effect of Herb Medicine Treatment for Functional Dyspepsia: A Randomized Placebo-Controlled and Compared Standard Treatment Trial (기능성 소화불량증 환자에 대한 한약복합제의 치료 효과: 무작위배정 표준치료제 위약 대조군 연구)

  • Kim, Yeon-Mi;Park, Yang-Chun;Jo, Jeong-Hyo;Kang, Wee-Chang;Son, Mi-Won;Hong, Kwon-Eui
    • The Journal of Korean Medicine
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    • v.31 no.1
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    • pp.1-13
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    • 2010
  • Objective: Functional dyspepsia is a prevalent disease. It impedes subjective quality of life. The purpose of this study was to examine the equivalent effect of herb medicine treatment (DA-9701) for functional dyspepsia. Methods: In this randomized, single-blinded, placebo-controlled study, we compared a herb medicine (DA-9701) with standard treatment (mosapride) and placebo for the treatment of functional dyspepsia. 42 volunteers who satisfied the requirements were enrolled in study. Severity of dyspepsia was measured by Nepean Dyspepsia Index (NDI) and Functional Dyspepsia Quality of Life (FD-QOL) before and after treatments. Results: 1. In the DA-9701 group, total key symptoms score was significantly lower and improve rate of key symptoms was higher than in the mosapride and placebo groups, but there were no statistically significant differences between three groups. 2. In the DA-9701 and mosapride groups, "nausea" and "bad breath" were significantly lower compared with the placebo group. 3. In the DA-9701 group, NDI Quality of Life scores were significantly higher, but there were no [other] statistically significant differences between the three groups. 4. In the DA-9701 and mosapride groups, FD-QOL scores were higher compared with the placebo group, but there were no statistically significant differences between the three groups. Conclusion: Herb medicine treatment (DA-9701) is effective to improve the symptoms and quality of life in patients with functional dyspepsia.

Symmetrical Drug-Related Intertriginous and Flexural Exanthema: Two Cases and Brief Literature Review

  • Seok, Joon;Kim, Jae Min;Park, Kui Young;Seo, Seong Jun
    • Annals of dermatology
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    • v.30 no.5
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    • pp.606-609
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    • 2018
  • It has been reported that there are a range of causative drugs related to symmetrical drug-related intertriginous and flexural exanthema (SDRIFE). The causative drugs reported so far include the following: antibiotics, intravenous immunoglobulin, chemotherapeutic agents, and biologics. In this study, we report two cases of SDRIFE and a review of the previous literature. We believe that our study makes a significant contribution to the literature because it demonstrates that intradermal injection of the Chinese herbal ball, and not its topical application, elicited a reaction that predicted the occurrence of SDRIFE. This finding is important for the diagnosis of SDRIFE in future studies. Our findings also provide evidence for a SDRIFE reaction after exposure to ranitidine and mosapride.

Measurement of Human Cytochrome P450 Enzyme Induction Based on Mesalazine and Mosapride Citrate Treatments Using a Luminescent Assay

  • Kim, Young-Hoon;Bae, Young-Ji;Kim, Hyung Soo;Cha, Hey-Jin;Yun, Jae-Suk;Shin, Ji-Soon;Seong, Won-Keun;Lee, Yong-Moon;Han, Kyoung-Moon
    • Biomolecules & Therapeutics
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    • v.23 no.5
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    • pp.486-492
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    • 2015
  • Drug metabolism mostly occurs in the liver. Cytochrome P450 (CYP) is a drug-metabolizing enzyme that is responsible for many important drug metabolism reactions. Recently, the US FDA and EU EMA have suggested that CYP enzyme induction can be measured by both enzymatic activity and mRNA expression. However, these experiments are time-consuming and their interassay variability can lead to misinterpretations of the results. To resolve these problems and establish a more powerful method to measure CYP induction, we determined CYP induction by using luminescent assay. Luminescent CYP assays link CYP enzyme activity to firefly luciferase luminescence technology. In this study, we measured the induction of CYP isozymes (1A2, 2B6, 2C9, and 3A4) in cryopreserved human hepatocytes (HMC424, 478, and 493) using a luminometer. We then examined the potential induction abilities (unknown so far) of mesalazine, a drug for colitis, and mosapride citrate, which is used as an antispasmodic drug. The results showed that mesalazine promotes CYP2B6 and 3A4 activities, while mosapride citrate promotes CYP1A2, 2B6, and 3A4 activities. Luminescent CYP assays offer rapid and safe advantages over LC-MS/MS and qRT-PCR methods. Furthermore, luminescent CYP assays decrease the interference between the optical properties of the test compound and the CYP substrates. Therefore, luminescent CYP assays are less labor intensive, rapid, and can be used as robust tools for high-throughput CYP screening during early drug discovery.

Measurement of Gastric Contractility of Awake Rats by Bowel Sounds Recorded through an Electronic Stethoscope in a Sound Insulation Box (차음상자와 전자청진기로 기록된 장음에 의해서 깨어 있는 흰쥐의 위수축력 측정)

  • Yoon, Sang-Hyub
    • The Journal of Internal Korean Medicine
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    • v.35 no.4
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    • pp.439-447
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    • 2014
  • Objectives: The aim of this study was to investigate whether 1) variation of bowel sounds recorded stably through an electronic stethoscope in a sound insulation box can be related with that of gastric contraction and 2) if they are thus useful tool in the measurement of the gastric contractility in awake rats or not. Methods: Electrical potentials of both electronic stethoscope of bowel sound and force transducer were recorded simultaneously and continuously in the sound insulation box for the starting 30 min of basal state, and then 30 min of 0.2 ml normal saline administration, finally 30 min of 0.2 ml mosapride citrate solution (100 mg/Kg) in rats. Each motility index of normal saline or mosapride citrate treatment was presented with ratio against the basal state by using integrated electrical potentials. Results: A pattern of significance of gastric contractility between bowel sound and force transducer was showed analogously. Conclusions: The amplitude of bowel sounds recorded by the electronic stethoscope related with the intensity of gastric contractions. This confirms that a sound insulation box and electronic stethoscope are useful tools in the measurement of the gastric contractility of awake rats.

Esophageal Dysmotility in a Young Adult Dog (식도운동성 저하에 대한 진단 및 치료)

  • Kim, Jae-Hoon;Park, Hyung-Jin;Song, Kun-Ho;Choi, Ho-Jung;Seo, Kyoung-Won
    • Journal of Veterinary Clinics
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    • v.30 no.3
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    • pp.193-195
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    • 2013
  • An 18-month-old intact male Cocker Spaniel dog weighing 7.7 kg was referred with a 2-week history of severe regurgitation. Based on the screening examination and fluoroscopy, this patient was diagnosed as having esophageal dysmotility. Treatment with mosapride and feeding small amounts of canned food frequently in an elevated position resulted in a successful outcome. The severe regurgitation improved, and the esophageal transit time improved from 18 sec to 8 sec. This is the first case report describing the diagnosis and clinical management of esophageal dysmotility in a young dog in Korea.

Characteristics of 5-Hydroxytryptamine Receptors Involved in Contraction of Feline Ileal Longitudinal Smooth Muscle

  • Wang, Yiyi;Park, Sun-Young;Oh, Kyung-Hoon;Min, Young-Sil;Lee, Yun-Jeong;Lee, Seok-Yong;Sohn, Uy-Dong
    • The Korean Journal of Physiology and Pharmacology
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    • v.15 no.5
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    • pp.267-272
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    • 2011
  • A number of studies have demonstrated that 5-hydroxytryptamine (5-HT) can induce muscle contraction or relaxation response and enhance secretion in the gastrointestinal tract via a multiplicity of 5-HT receptor subtypes. In the present study, we investigated the pharmacological characterization of the 5-HT-induced contractile response in longitudinal smooth muscle isolated from the feline ileum. Addition of 5-HT into muscle chambers enhanced the basal tone and spontaneous activity in a concentration-dependent manner. The neurotoxin tetrodotoxin did not alter the 5-HT-induced contraction of the longitudinal muscles. Neither atropine nor guanethidine affected the contraction. The 5-HT agonists, 5-methylserotonin hydrochloride and mosapride, also evoked concentration-dependent contractions. The 5-HT-induced contraction was enhanced by the $5HT_2$ receptor antagonist ketanserin and the $5-HT_3$ receptor antagonist ondansetron but was inhibited by the 5-$HT_1$ receptor antagonist methysergide and 5-$HT_4$ receptor antagonist GR113808. These results indicate that 5-$HT_1$ and 5-$HT_4$ receptors may mediate the contraction of the 5-HT-induced response and 5-$HT_2$ and 5-$HT_3$ receptors may mediate 5-HT-induced relaxation in feline ileal longitudinal smooth muscles.

The Improvement Effect of MMSC (DL-Methionine Methylsulfonium Chloride) in Functional Dyspepsia Animal Models (동물모델을 이용한 MMSC(DL-Methionine Methylsulfonium Chloride)의 기능성소화불량증 개선효과)

  • Kim, Jae Min;Cha, Myoung Hee;Lee, Don Haeng;Lee, Woon Kyu
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.42 no.12
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    • pp.2076-2081
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    • 2013
  • The objective of this study is to investigate the gastric emptying and gastrointestinal transit improvement effect of DL-methionine methylsulfonium chloride (MMSC) in functional dyspepsia animal models. Cisplatin causes nausea, vomiting, and inhibition of gastric emptying. Rats were divided into four groups: G1 (normal group), G2 (gastric emptying induced by cisplatin), G3 (gastric emptying induced by cisplatin with itopride 30 mg/kg pretreatment), and G4 (gastric emptying induced by cisplatin with MMSC 4 mg/kg pretreatment). Immediately after an oral administration of a liquid meal (phenol red), delayed gastric emptying was induced by cisplatin (10 mg/kg (i.p.)). After 20 min in the cisplatin administration, the animals were sacrificed. In rats treated with cisplatin, the gastric emptying rate was significantly reduced. On the other hand, MMSC reversed the reduction of gastric emptying induced by cisplatin. And also, MMSC caused to travel FITC-dextran more significantly longer distance than the control, which is based on the values of the mean geometric center in the atropine driven delayed gastrointestinal transit animal models. Furthermore, MMSC drastically increased the gastrointestinal transit in rats, considerably increased the values of the mean geometric center (MGC), compared to the control, which was comparable to that of mosapride. These results suggest that MMSC could be an effective component for the treatment of functional dyspepsia.