Dual effects of trimebutine on electrical responses of gastric smooth muscles in the rat

Effects of DQ-2511 a Novel Prokînetic Agent, on Electrical Activities of Smooth Muscle in the Guinea Pig Stomach

“…How ever, the concentrations of DQ-2511 which effectively enhance gastric motility appear to be limited to a narrow range, and in vitro the most effective concentration is found to be around 10~8 rnol/1. This property of DQ-2511 differs from that of other prokinctics such as cisapride or trimebutine in that for the latter drugs the effectiveness increases with increas ing concentrations and reveals inhibitory ac tion only at higher concentrations (mostly over 10-5 mol/l) [24,25]. The present experi ments showed that this was also the case for DQ-2511, as higher concentrations of DQ-25 11 inhibited the slow waves and cholinergic transmission.…”

“…For example, cisapride in creases the gastrointestinal motility by en hancing the release of ACh from cholinergic nerves through inhibition of the prejunctional inhibitory serotonin receptors [9], and these effects of cisapride could be detected as the increase in amplitude of the e.j.p. [24], T rimebutine increases the gastric motility by accel erating the frequency of slow wave generation and reduces the enhanced activity by inhib iting the release of ACh [25]. On the other hand, the action of DQ-2511 involves an acti vation of peripheral reflux nervous system [8], and this is an important difference from the other prokinetic agents such as cisapride [6].…”

Effects of trimebutine maleate on colonic motility through Ca2+-activated K+ channels and L-type Ca2+ channels

“…TM inhibits smooth muscle contractions in intestinal hyperkinesis, but TM may depolarize the resting membrane potential in hypomotility to normalize the movement (Xue et al, 1995;Delvaux and Wingate, 1997). The effect of TM is not only influenced by the state of the gut, but also by the concentration of TM.…”

“…This dish was filled with Krebs saline, which was constantly bubbled with carbogen at 37 o C. The mucosa was carefully cut off under a microscope. Conventional intracellular microelectrode techniques were applied to record the action and membrane potentials using glass microelectrodes filled with 3 M KCl (resistance: 40-60 MΩ; Xue et al,1995). Spontaneous activities were recorded by an AXON 700B amplifier (Molecular Devices) using the current clamp (I = 0) in gap-free mode.…”

Determination of trimebutine in pharmaceuticals by differential pulse voltammetry at a glassy carbon electrode

“…They are clinically used in the treatment of various digestive tract-disorders including dyspepsia, irritable bowel syndrome and post-operative ileus [1][2][3]. The inhibitory and excitatory actions of trimebutine on gastric muscles are due to inhibition of Ca 2+ and depolarization of the membrane, respectively [4]. Trimebutine (TMB) exhibits weak opioid properties [5][6][7][8] and has been shown to influence the activity of visceral afferent nerves in the rat [9].…”