生物活性

• 描述Trimebutine is a drug with antimuscarinic and weak mu opioid agonist effects. Trimebutine has low affinity to opioid receptors, possesses mu-receptor selective properties rather than those of kappa-opioid receptor in the peripheral tissues and in the central brain homogenate^[3]. Trimebutine accelerates gastric emptying, induces premature phase III of the migrating motor complex in the intestine and modulates the contractile activity of the colon^[4]. Trimebutine attenuated colonic motility mainly through the inhibition of L-type Ca(2+) channels at higher concentrations, whereas, at lower concentrations, it depolarized membrane potentials by reducing BK(ca) currents, resulting in the enhancement of the muscle contractions^[5]. In addition, trimebutine may exert its suppressive effect on the HMGB1(high mobility group box 1)-RAGE inflammatory signal pathways by strongly blocking the recruitment of ERK1/2 (extracellular signal-regulated kinase 1 and 2) to the intracellular tail domain of RAGE in addition to its weak inhibition of the extracellular interaction of HMGB1 with RAGE(receptor for advanced glycation end-products)^[6].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT01926444	Pain Cancer ... more >> Colonic Diseases Collapse <<	Phase 2	Completed	-	United States, Arizona ... more >> Mayo Clinic Scottsdale, Arizona, United States, 85259 United States, California Anaheim Clinical Trials Anaheim, California, United States, 92801 Precision Research Institute Chula Vista, California, United States, 91910 Precision Research Institute San Diego, California, United States, 92114 United States, Florida Avail Clinical Research LLC Deland, Florida, United States, 32720 The Center for GI Disorders Hollywood, Florida, United States, 33021 United States, Maryland Mid-Atlantic Medical Research Centers Hollywood, Maryland, United States, 20636 United States, Minnesota Mayo Clinic Rochester Rochester, Minnesota, United States, 55910 United States, New Jersey PharmaTrials Hillsborough, New Jersey, United States, 08844 United States, New York Montefiore Medical Center Bronx, New York, United States, 10467 United States, South Carolina Gastroenterology Associates of Orangeburg Orangeburg, South Carolina, United States, 29118 Canada, British Columbia GIRI (GI Research Institute) Vancouver, British Columbia, Canada, V6Z 2K5 Canada, Ontario Toronto Digestive Disease Associates Toronto, Ontario, Canada, L4L4Y7 Canada, Quebec Clinique 1037 Montreal, Quebec, Canada, H2X3H9 Spécialistes MD Specialists Montreal, Quebec, Canada, H3Z 2P9 Collapse <<
  NCT02276768	Pain Cancer ... more >> Colonic Disease Collapse <<	Phase 1	Completed	-	Canada, Quebec ... more >> Algorithme Pharma Inc. Montreal, Quebec, Canada, H3P-3P1 Collapse <<
  NCT01507922	Irritable Bowel Syndrome	Phase 4	Completed	-	Korea, Republic of ... more >> Korea University Ansan Hospital Ansan, Korea, Republic of Hallym University Sacred Heart Hospital Anyang, Korea, Republic of Kangwon National University Hospital Chuncheon, Korea, Republic of Gachon University Gil Hospital Incheon, Korea, Republic of Inje University Seoul Paik Hospital Seoul, Korea, Republic of Korea University Anam Hospital Seoul, Korea, Republic of Korea University Guro Hospital Seoul, Korea, Republic of Collapse <<

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• 参考文献

• [1] Roman FJ, Lanet S, et al. Pharmacological properties of trimebutine and N-monodesmethyltrimebutine. J Pharmacol Exp Ther. 1999 Jun;289(3):1391-7.

  [2] Kaneto H, Takahashi M, et al. The opioid receptor selectivity for trimebutine in isolated tissues experiments and receptor binding studies. J Pharmacobiodyn. 1990 Jul;13(7):448-53.

  [3] Kaneto H, Takahashi M, Watanabe J. The opioid receptor selectivity for trimebutine in isolated tissues experiments and receptor binding studies. J Pharmacobiodyn. 1990 Jul;13(7):448-53

  [4] Delvaux M, Wingate D. Trimebutine: mechanism of action, effects on gastrointestinal function and clinical results. J Int Med Res. 1997 Sep-Oct;25(5):225-46

  [5] Lee HT, Kim BJ. Trimebutine as a modulator of gastrointestinal motility. Arch Pharm Res. 2011 Jun;34(6):861-4

  [6] Nakajima S, Ogawa N, Yokoue N, Tachibana H, Tamada K, Okazawa M, Sato A, Oyama T, Abe H, Kamiya T, Yoshimori A, Yoshizawa K, Inoue S, Yokomizo T, Uchiumi F, Abe T, Tanuma SI. Trimebutine attenuates high mobility group box 1-receptor for advanced glycation end-products inflammatory signaling pathways. Biochem Biophys Res Commun. 2020 Dec 17;533(4):1155-1161

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