Reference

Effects of spasmolytics on potassium-induced contraction of rat intestine in vivo

Effects of spasmolytics on potassium-induced contraction of rat intestine in vivo. Subissi, Alessandro; Brunori, Paola; Bachi, Moreno (Dep. Pharmacol., Lab. Guidotti S.p.A., Pisa 56010, Italy). Eur. J. Pharmacol., 96(3-4), 295-301 (English) 1983. CODEN: EJPHAZ. ISSN: 0014-2999. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Eight spasmolytic drugs commonly used in the treatment of the irritable bowel syndrome were compared to verapamil [52-53-9] with respect to their effects (all drugs injected i.v.) on the contraction of duodenum, ileum, and colon induced by high-K+ topical application in the anesthetized rat. Verapamil > rociverine citrate [89026-32-4] > papaverine [58-74-2] > mebeverine [3625-06-7] > dicyclomine [77-19-0] antagonized dose-dependently the contraction of duodenum and colon, the activity on duodenum being from 2- (rociverine) to 10-fold (verapamil) higher. Verapamil and rociverine, but not the other drugs, were also active on ileum. N-Butylscopolammonium bromide [149-64-4], phloroglucinol [108-73-6] and trimebutine maleate [34140-59-5] were inactive against the contraction of the 3 intestinal regions, and prifinium bromide [4630-95-9] was inactive on duodenum and ileum, while having remarkable activity on colon (unrelated to its antimuscarinic activity). The results are discussed briefly with ref. to the pharmacol. therapy of the irritable bowel syndrome.

Effects of trimebutine maleate (TM-906) on the spontaneous contraction of isolated guinea pig colon

Effects of trimebutine maleate (TM-906) on the spontaneous contraction of isolated guinea pig colon. Takenaga, Hideyuki; Magaribuchi, Tetsuo; Tamaki, Hajime (Pharmacol. Res. Lab., Tanabe Seiyaku Co., Ltd., Toda 335, Japan). Jpn. J. Pharmacol., 34(2), 177-81 (English) 1984. CODEN: JJPAAZ. ISSN: 0021-5198. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Effects of TM-906 (I) [34140-59-5] on the spontaneous contraction of the isolated guinea pig colon were investigated. TM-906, at 10-6 and 10-5 g/mL increased the tone without affecting the amplitude of the spontaneous contraction in prepns. with low tone, whereas it decreased the tone and the amplitude of the spontaneous contraction in prepns. with high tone. At 10-4 g/mL, TM-906 decreased the tone and finally abolished the spontaneous contraction in all prepns. The increase in tone induced by TM-906 was prevented by diltiazem and exposure to Ca++-free soln., but not by tetrodotoxin, atropine, phentolamine or propranolol, and depended on the extracellular concn. of CaCl2. The decrease in tone and amplitude of the spontaneous contraction produced by TM-906 were not prevented by tetrodotoxin, phentolamine or propranolol. TM-906 further increased the tone increased by 10 mM KCl, while it decreased the tone increased by 30 mM KCl. Apparently, TM-906 possesses both a relaxing and an excitatory effect which seem due to its direct action on the smooth muscle.