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Chemical Compound Review

Spasmomen     diethyl-methyl-[2-[4-[(2...

Synonyms: Octylonium, SP63, SureCN109554, AG-E-81199, CHEMBL2103773, ...
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Disease relevance of diethyl-methyl-[2-[4-[(2-octoxybenzoyl)amino]benzoyl]oxyethyl]ammonium


Psychiatry related information on diethyl-methyl-[2-[4-[(2-octoxybenzoyl)amino]benzoyl]oxyethyl]ammonium

  • Notably the administration of otilonium bromide in rats receiving morphine together with naloxone decreased the intensity of certain withdrawal symptoms, such as excretion of faeces, wet dog shake behaviour, and elevated the nociceptive threshold values [4].
  • Treatment of IBS patients with octylonium bromide (80 mg, qid, per os) for 5-7 days reduced their colonic response to eating to a very short increase in colonic motor activity limited to the first 30 min [5].
  • CONCLUSION: These data suggest that otilonium bromide enhances sensory thresholds to recto-sigmoideal distention [6].
  • In contrast to placebo, octylonium bromide significantly reduced pain and bloating, and significantly increased (p < 0.02) the pain threshold throughout the treatment period [7].
  • Combining otilonium bromide with benzodiazepines, such as diazepam, may improve the efficacy of the agent with respect to GI symptoms, while also treating underlying anxiety disorders [2].

High impact information on diethyl-methyl-[2-[4-[(2-octoxybenzoyl)amino]benzoyl]oxyethyl]ammonium


Biological context of diethyl-methyl-[2-[4-[(2-octoxybenzoyl)amino]benzoyl]oxyethyl]ammonium


Anatomical context of diethyl-methyl-[2-[4-[(2-octoxybenzoyl)amino]benzoyl]oxyethyl]ammonium

  • The radioactivity in large intestine walls was measurable at otilonium bromide concentrations in the range of micromole equivalents/kg, from 4 to 8 h after drug administration [12].
  • We describe here the effects of otilonium bromide (an anticholinergic agent widely used as an intestinal spasmolytic) on whole-cell currents through Ca2+ channels (IBa) and catecholamine secretion in rat adrenal glands and isolated rat chromaffin cells [16].
  • In radioligand binding experiments otilonium bromide produced a concentration-dependent inhibition of the binding of both an agonist ([125I]neurokinin A, Ki 7.2 microM) and an antagonist ([3H]SR 48968, Ki 2.2 microM) to membranes of Chinese hamster ovary cells transfected with the human tachykinin NK2 receptor [13].
  • The competitive antagonism toward BaCl2-induced contraction of rat ileum and aorta suggested that octylonium bromide interferes with Ca++ mobilization [17].
  • Sigmoid motility during distension was significantly reduced after octylonium bromide (p < 0.05), but it did not change after placebo [7].

Associations of diethyl-methyl-[2-[4-[(2-octoxybenzoyl)amino]benzoyl]oxyethyl]ammonium with other chemical compounds


Gene context of diethyl-methyl-[2-[4-[(2-octoxybenzoyl)amino]benzoyl]oxyethyl]ammonium

  • Antimuscarinic, calcium channel blocker and tachykinin NK2 receptor antagonist actions of otilonium bromide in the circular muscle of guinea-pig colon [13].
  • Otilonium bromide eliminated the APs superimposed on the depolarization induced by the tachykinin NK1 receptor agonist, [Sar9]substance P-sulphone and suppressed the corresponding contraction (IC50 43 microM) but had little effect on the sustained membrane depolarization induced by this agonist [13].

Analytical, diagnostic and therapeutic context of diethyl-methyl-[2-[4-[(2-octoxybenzoyl)amino]benzoyl]oxyethyl]ammonium


  1. Otilonium bromide in irritable bowel syndrome: a double-blind, placebo-controlled, 15-week study. Battaglia, G., Morselli-Labate, A.M., Camarri, E., Francavilla, A., De Marco, F., Mastropaolo, G., Naccarato, R. Aliment. Pharmacol. Ther. (1998) [Pubmed]
  2. Irritable bowel syndrome. Spinelli, A. Clinical drug investigation (2007) [Pubmed]
  3. Assessment of potential selectivity of antispasmodics for the various sections of the gastrointestinal tract of the rat as a guideline for their clinical use. Maggi, C.A., Meli, A. Archives internationales de pharmacodynamie et de thérapie. (1983) [Pubmed]
  4. Effects exerted by otilonium bromide administration on precipitated opioid withdrawal syndrome in rats. Pinelli, A., Trivulzio, S., Vignati, S. Toxicology (1997) [Pubmed]
  5. Colonic motility and gastric emptying in patients with irritable bowel syndrome. Effect of pretreatment with octylonium bromide. Narducci, F., Bassotti, G., Granata, M.T., Pelli, M.A., Gaburri, M., Palumbo, R., Morelli, A. Dig. Dis. Sci. (1986) [Pubmed]
  6. Otilonium bromide enhances sensory thresholds of volume and pressure in patients with irritable bowel syndrome. Czimmer, J., Süto, G., Király, A., Mózsik, G. J. Physiol. Paris (2001) [Pubmed]
  7. Octylonium bromide in the treatment of the irritable bowel syndrome: a clinical-functional study. Baldi, F., Longanesi, A., Blasi, A., Monello, S., Cestari, R., Missale, G., Corazziari, E., Badiali, G., Marzio, L., Di Felice, F. Hepatogastroenterology (1992) [Pubmed]
  8. Meta-analysis: The treatment of irritable bowel syndrome. Lesbros-Pantoflickova, D., Michetti, P., Fried, M., Beglinger, C., Blum, A.L. Aliment. Pharmacol. Ther. (2004) [Pubmed]
  9. The colon-selective spasmolytic otilonium bromide inhibits muscarinic M(3) receptor-coupled calcium signals in isolated human colonic crypts. Lindqvist, S., Hernon, J., Sharp, P., Johns, N., Addison, S., Watson, M., Tighe, R., Greer, S., Mackay, J., Rhodes, M., Lewis, M., Stebbings, W., Speakman, C., Evangelista, S., Johnson, I., Williams, M. Br. J. Pharmacol. (2002) [Pubmed]
  10. Platelet-activating factor regulates chloride transport in colonic epithelial cell monolayers. Claud, E.C., Li, D., Xiao, Y., Caplan, M.S., Jilling, T. Pediatr. Res. (2002) [Pubmed]
  11. Otilonium bromide inhibits muscle contractions via L-type calcium channels in the rat colon. Martin, M.T., Hove-Madsen, L., Jimenez, M. Neurogastroenterol. Motil. (2004) [Pubmed]
  12. A distribution study with (14)C-otilonium bromide in the rat: evidence for selective tropism for large intestine after oral administration. Evangelista, S., Cochet, P., Bromet, N., Criscuoli, M., Maggi, C.A. Drug Metab. Dispos. (2000) [Pubmed]
  13. Antimuscarinic, calcium channel blocker and tachykinin NK2 receptor antagonist actions of otilonium bromide in the circular muscle of guinea-pig colon. Santicioli, P., Zagorodnyuk, V., Renzetti, A.R., Maggi, C.A. Naunyn Schmiedebergs Arch. Pharmacol. (1999) [Pubmed]
  14. The clinical pharmacology of single doses of otilonium bromide in healthy volunteers. Sutton, J.A., Kilminster, S.G., Mould, G.P. Eur. J. Clin. Pharmacol. (1997) [Pubmed]
  15. Receptor binding profile of Otilonium bromide. Evangelista, S., Giachetti, A., Chapelain, B., Neliat, G., Maggi, C.A. Pharmacol. Res. (1998) [Pubmed]
  16. Blocking effects of otilonium on Ca2+ channels and secretion in rat chromaffin cells. Gandía, L., López, M.G., Villarroya, M., Gilabert, J.A., Cárdenas, A., García, A.G., Borges, R. Eur. J. Pharmacol. (1996) [Pubmed]
  17. Octylonium bromide: a smooth muscle relaxant which interferes with calcium ions mobilization. Maggi, C.A., Manzini, S., Meli, A. Archives internationales de pharmacodynamie et de thérapie. (1983) [Pubmed]
  18. High-performance liquid chromatographic method for assay of otilonium bromide, diazepam, and related compounds in finished pharmaceutical forms. Mannucci, C., Bertini, J., Cocchini, A., Perico, A., Salvagnini, F., Triolo, A. Journal of pharmaceutical sciences. (1993) [Pubmed]
  19. Stability-indicating methods for determining omeprazole and octylonium bromide in the presence of their degradation products. el-Kousy, N.M., Bebawy, L.I. Journal of AOAC International. (1999) [Pubmed]
  20. Clinical and functional evaluation of the efficacy of otilonium bromide: a multicenter study in Italy. Baldi, F., Longanesi, A., Blasi, A., Monello, S., Cestari, R., Missale, G., Corazziari, E., Badiali, G., Pescatori, M., Anastasio, G. The Italian journal of gastroenterology. (1991) [Pubmed]
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