EM574, an erythromycin derivative, is a motilin receptor agonist in the rabbit

European Journal of Pharmacology

Volumn 322, Issue 1, 1997, Pages 63-71

  Sato, Fumihiko ^a   Sekiguchi, Masahiro ^a   Marui, Shogo ^a   Inatomi, Nobuhiro ^a   Shino, Akio ^a   Itoh, Zen ^b   Omura, Satoshi ^c  

^a TAKEDA PHARMACEUTICAL COMPANY LIMITED   (Japan)

^b GUNMA UNIVERSITY   (Japan)

^c KITASATO INSTITUTE   (Japan)

Author keywords

EM574; Erythromycin; Motilin; Rabbit; Receptor binding

Indexed keywords

8,9 ANHYDRO N ISOPROPYLNORERYTHROMYCIN A 6,9 HEMIACETAL; ERYTHROMYCIN; ERYTHROMYCIN DERIVATIVE; MOTILIN; UNCLASSIFIED DRUG;

ANIMAL TISSUE; ARTICLE; AUTORADIOGRAPHY; BINDING SITE; CONTROLLED STUDY; GUINEA PIG; IN VITRO STUDY; INTESTINE; INTESTINE CONTRACTION; MALE; NONHUMAN; PRIORITY JOURNAL; RABBIT; RAT; RECEPTOR BINDING; SPECIES DIFFERENCE; STOMACH ANTRUM;

ANIMALS; AUTORADIOGRAPHY; ERYTHROMYCIN; FEMALE; GASTROINTESTINAL AGENTS; GUINEA PIGS; IODINE RADIOISOTOPES; MALE; MUSCLE CONTRACTION; MUSCLE, SMOOTH; PYLORIC ANTRUM; RABBITS; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, GASTROINTESTINAL HORMONE; RECEPTORS, NEUROPEPTIDE; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0030996626     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0014-2999(96)00983-1     Document Type: Article

References (42)

1. Adachi, H., N. Toda, S. Hayashi, M. Noguchi, K. Suzuki, K. Torizuka, H. Yajima and K. Koyama, 1981, Mechanism of the excitatory action of motilin on isolated rabbit intestine, Gastroenterology 80, 783.
2. Annese, V., J. Janssens, G. Vantrappen, J. Tack, T.L. Peeters, P. Willemse and V. Cutem, 1992, Erythromycin accelerates gastric emptying by inducing antral contractions and improved gastroduodenal coordination, Gastroenterology 102, 823.
3. Bormans, V., T.L. Peeters and G. Vantrappen, 1986, Motilin receptors in rabbit stomach and small intestine, Regul. Pept. 15, 143.
4. Brown, J.C., M.A. Cook and J.R. Dryburgh, 1973, Motilin, a gastric motor activity stimulating polypeptide: the complete amino acid sequence, Can. J. Biochem. 51, 533.
5. 3H-mepyramine, J. Pharmacol. Exp. Ther. 209, 437.
6. Depoortere, I., T.L. Peeters, G. Matthijs, T. Cachet, J. Hoogmartens and G. Vantrappen, 1989, Structure-activity relation of erythromycin-related macrolides in inducing contractions and in displacing bound motilin in rabbit duodenum, J. Gastrointest. Motil. 1, 150.
7. Depoortere, I., T.L. Peeters and G. Vantrappen, 1990, The erythromycin derivative EM-523 is a potent motilin agonist in man and in rabbit, Peptides 11, 515.
8. Depoortere, I., T.L. Peeters and G. Vantrappen, 1993, Distribution and characterization of motilin receptors in the cat, Peptides 14, 1153.
9. Fox, J.E.T., E.E. Daniel, J. Jury, A.E. Fox and S.M. Collins, 1983, Sites and mechanisms of action of neuropeptides in canine gastric motility differ in vivo and in vitro, Life Sci. 33, 817.
10. Fox, J.E.T., E.E. Daniel, J. Jury and H. Robotham, 1984, The mechanism of motilin excitation of the canine small intestine, Life Sci. 34, 1001.
11. Green, W.E.R., H. Ruppin, D.L. Wingate, E. Domschke, E. Wunsch, L. Demling and H.D. Ritchie, 1976, Effects of 13-nle-motilin on the electrical and mechanical activity of the isolated perfused canine stomach and duodenum, Gut 17, 362.
12. Holzer, P., W. Schluet and C.A. Maggi, 1995, Substance P stimulates and inhibits intestinal peristalsis via distinct receptors, J. Pharmacol. Exp. Ther. 274, 322.
13. Inatomi, N., H. Satoh, Y. Maki, N. Hashimoto, Z. Itoh and S. Ōmura, 1989, An erythromycin derivative, EM-523, induced motilin-like gastrointestinal motility in dogs, J. Pharmacol. Exp. Ther. 251, 707.
14. Inatomi, N., F. Sato, S. Marui, Z. Itoh and S. Ōmura, 1996, Vagus-dependent and vagus-independent mechanisms of action of the erythromycin derivative EM574 and motilin in dogs, Jpn. J. Pharmacol. 71, 29.
15. Itoh, Z., S. Takeuchi, I. Aizawa, K. Mori, T. Taminato, Y. Seino, H. Imura and N. Yanaihara, 1978, Changes in plasma motilin concentration and gastrointestinal contractile activity in conscious dogs, Am. J. Dig. Dis. 23, 929.
16. Itoh, Z., M. Nakaya, T. Suzuki, H. Arai and K. Wakabayashi, 1984a, Erythromycin mimics exogenous motilin in gastrointestinal contractile activity in the dog, Am. J. Physiol. 247, G688.
17. Itoh, Z., T. Suzuki, M. Nakaya, M. Inoue and S. Mitsuhashi, 1984b, Gastrointestinal motor-stimulating activity of macrolide antibiotics and analysis of their side effects on the canine gut, Antimicrob. Agents Chemother. 26, 863.
18. Itoh, Z., T. Suzuki, M. Nakaya, M. Inoue, H. Arai and K. Wakabayashi, 1985, Structure-activity relation among macrolide antibiotics in initiation of interdigestive migrating contractions in the canine gastrointestinal tract, Am. J. Physiol. 248, G320.
19. Janssens, J., T.L. Peeters, G. Vantrappen, J. Tack, J.L. Urbain, M. De Roo, E. Muls and R. Bouillon, 1990, Improvement of gastric emptying in diabetic gastroparesis by erythromycin, New Engl. J. Med. 322, 1028.
20. Jennewein, H.M., H. Hummelt, R. Siewert and F. Waldeck, 1975, The motor-stimulating effect of natural motilin on the lower esophageal sphincter, fundus, antrum and duodenum in dogs, Digestion 13, 246.
21. 13-motilin (KW-5139)-evoked release of acetylcholine from enteric neurons in the rabbit duodenum, Br. J. Pharmacol. 109, 94.
22. 125I-motilin to duodenal muscle, Biochem. Biophys. Res. Commun. 150, 877.
23. Lowry, O.H., N.J. Rosebrough, A.L. Farr and R.J. Randall, 1951, Protein measurement with the Folin phenol reagent, J. Biol. Chem. 193, 265.
24. 13]porcine motilin fragments, Peptides 13, 565.
25. Maliakkal, B.J., G. Polidori, C. Gordon, L. Davis and T.K. Desai, 1991, Severe gastroparesis following cancer chemotherapy and prokinetic response to erythromycin [abstract], Gastroenterology 100, A466.
26. Matthijs, G., T.L. Peeters and G. Vantrappen, 1988, Effect of different calcium modulators on motilin-induced contractions of the rabbit duodenum. Comparison with acetylcholine, Regul. Pept. 21, 321.
27. Mozwecz, H., D. Pavel, D. Pitrak, P. Orellana, P.K. Schlesinger and T.J. Layden, 1990, Erythromycin stearate as prokinetic agent in postvagotomy gastroparesis, Dig. Dis. Sci. 33, 902.
28. Ōmura, S., K. Tsuzuki, T. Sunazuka, S. Marui, H. Toyoda, N. Inatomi and Z. Itoh, 1987, Macrolides with gastrointestinal motor stimulating activity, J. Med. Chem. 30, 1941.
29. Parkman, H.P., A.P. Pagano, M.A. Vozzelli and J.P. Ryan, 1995, Gastrokinetic effects of erythromycin: myogenic and neurogenic mechanisms of action in rabbit stomach, Am. J. Physiol. 269, G418.
30. Peeters, T.L., G. Vantrappen and J. Janssens, 1980, Fasting motilin levels are related to the interdigestive motility complex, Gastroenterology 79, 716.
31. Peeters, T.L., V. Bormans and G. Vantrappen, 1988, Comparison of motilin binding to crude homogenates of human and canine gastrointestinal smooth muscle tissue, Regul. Pept. 23, 171.
32. Peeters, T.L., G. Matthijs, I. Depoortere, T. Cachet, J. Hoogmartens and G. Vantrappen, 1989, Erythromycin is a motilin receptor agonist, Am. J. Physiol. 257, G470.
33. 2+ dependence of motilide-induced contractions in rabbit duodenal muscle strips in vitro, Naunyn-Schmiedeberg's Arch. Pharmacol. 343, 202.
34. Richards, R.D., K.G. Davenport, K.D. Hurm, W.R. Wimbish and R.W. McCallum, 1990, Acute and chronic treatment of gastroparesis with erythromycin [abstract], Gastroenterology 98, A385.
35. Sakai, T., M. Satoh, K. Sonobe, M. Nakajima, Y. Shiba and Z. Itoh, 1994, Autoradiographic study of motilin binding sites in the rabbit gastrointestinal tract, Regul. Pept. 53, 249.
36. Satoh, T., N. Inatomi, H. Satoh, S. Marui, Z. Itoh and S. Ōmura, 1990, EM-523, an erythromycin derivative, and motilin show similar contractile activity in isolated rabbit intestine, J. Pharmacol. Exp. Ther. 254, 940.
37. Satoh, M., T. Sakai, I. Sano, K. Fujikura, H. Koyama, K. Oshima, Z. Itoh and S. Ōmura, 1994, EM-574, an erythromycin derivative, is a potent motilin receptor agonist in human gastric antrum, J. Pharmacol. Exp. Ther. 271, 574.
38. Scatchard, G., 1949, The attraction of proteins for small molecules and ions, Ann. NY Acad. Sci. 51, 660.
39. Sheikh, S.P., E. Roach, J. Fuhlendorff and J.A. Williams, 1991, Localization of Y1 receptors for NPY and PYY on vascular smooth muscle cells in rat pancreas, Am. J. Physiol. 260, G250.
40. Sunazuka, T., K. Tsuzuki, S. Marui, H. Toyoda, S. Ōmura, N. Inatomi and Z. Itoh, 1989, Motilides, macrolides with gastrointestinal motor stimulating activity. II. Quaternary N-substituted derivatives of 8,9-anhydro-erythromycin A 6,9-hemiacetal and 9,9-dihydroerythromycin A 6,9-epoxide, Chem. Pharm. Bull. 37, 2701.
41. Tsuzuki, K., T. Sunazuka, S. Marui, H. Toyoda, S. Ōmura, N. Inatomi and Z. Itoh, 1989, Motilides, macrolides with gastrointestinal motor stimulating activity. I. O-Substituted and tertiary N-substituted derivatives of 8,9-anhydroerythromycin A 6,9-hemiacetal, Chem. Pharm. Bull. 37, 2687.
42. Xynos, E., A. Mantides, A. Papageorgiou, A. Fountos, G. Pechlivanides and J.S. Vassilakis, 1992, Erythromycin accelerates delayed gastric emplying of solids in patients after truncal vagotomy and pyloroplasty, Eur. J. Surg. 158, 407.