Effect of otilonium bromide and ibodutant on the internalization of the NK2 receptor in human colon

Neurogastroenterology and Motility

Volumn 23, Issue 1, 2011, Pages 96-

  Cipriani, G ^a   Santicioli, P ^b   Evangelista, S ^b   Maggi, C A ^b   Riccadonna, S ^a   Ringressi, M N ^a   Bechi, P ^a   Faussone Pellegrini, M S ^a   Vannucchi, M G ^a  

^a UNIVERSITY OF FLORENCE   (Italy)

^b Menarini Ricerche SpA   (Italy)

Author keywords

Human colon; Ibodutant; Immunohisto chemistry; Neurokinin 2 (NK2) receptor; Otilonium bromide

Indexed keywords

IBODUTANT; NEUROKININ 2 RECEPTOR; NEUROKININ 2 RECEPTOR ANTAGONIST; OTILONIUM BROMIDE; UNCLASSIFIED DRUG;

ADULT; AGED; ARTICLE; CELL COUNT; CLINICAL ARTICLE; COLON; DRUG EFFECT; FEMALE; HUMAN; HUMAN TISSUE; IMMUNOHISTOCHEMISTRY; INTERNALIZATION; MALE; PRIORITY JOURNAL; QUANTITATIVE ANALYSIS; SMOOTH MUSCLE FIBER;

ADULT; AGED; AGED, 80 AND OVER; ANIMALS; COLON; DIPEPTIDES; FEMALE; GASTROINTESTINAL AGENTS; HUMANS; IMMUNOHISTOCHEMISTRY; MALE; MIDDLE AGED; QUATERNARY AMMONIUM COMPOUNDS; RECEPTORS, NEUROKININ-2; THIOPHENES;

EID: 78650147208     PISSN: 13501925     EISSN: 13652982     Source Type: Journal    
DOI: 10.1111/j.1365-2982.2010.01594.x     Document Type: Article

References (30)

1. 2 receptors in human. Auton Neurosci 2006; 126-127: 232-49.
2. Shimizu Y, Matsuyama H, Shiina T, Takewaki T, Furness JB. Tachykinin and their functions in the gastrointestinal tract. Cell Mol Life Sci 2008; 65: 295-311.
3. 2 receptor antagonist in the guinea-pig and human colon. Naunyn-Schmied Arch Pharmacol 1997; 356: 678-88.
4. 2 receptor antagonist prevents motility-stimulating effects of neurokinin A in small intestine. Br J Pharmacol 2001; 134: 215-23.
5. Renzi D, Pellegrini B, Tonelli F, Surrenti C, Calabrò A. Substance P (neurokinin-1) and neurokinin A (neurokinin-2) receptor gene and protein expression in the healthy and inflamed human intestine. Am J Pathol 2000; 157: 1511-22.
6. 2 receptors in human colon: involvement in the regulation of intestinal motility. J Comp Neurol 2007; 503: 381-91.
7. Warner FJ, Liu L, Lubowski DZ, Burcher E. Circular muscle contraction, messenger signalling and localization of binding sites for neurokinin A in human sigmoid colon. Clin Exp Pharmacol Physiol 2000; 27: 928-33.
8. 2 receptors in chemically defined human colonic neuronal pathways. J Comp Neurol 2008; 507: 1542-58.
9. Koenig JA, Edwardson JM. Endocytosis and recycling of G protein-coupled receptors. Trends Pharmacol Sci 1997; 18: 276-87.
10. Southwell BR, Seybold VS, Woodman HL, Jenkinson KM, Furness JB. Quantitation of neurokinin 1 receptor internalization and recycling in guinea-pig myenteric neurons. Neuroscience 1998; 87: 925-31.
11. Evangelista S. Quaternary ammonium derivatives as spasmolytics for irritable bowel syndrome. Curr Pharm Des 2004; 10: 3561-8.
12. Lesbros-Pantoflickova D, Michetti P, Fried M, Beglinger C, Blum AL. Meta-analysis: the treatment of irritable bowel syndrome. Aliment Pharmacol Ther 2004; 20: 1253-69.
13. 2 receptor antagonist actions of otilonium bromide in the circular muscle of guinea-pig colon. Naunyn-Schmied Arch Pharmacol 1999; 359: 420-7.
14. 2 receptor antagonist. Eur J Pharmacol 2006; 549: 140-8.
15. Mann PT, Southwell BR, Furness JB. Internalization of the neurokinin 1 rceptor in rat myenteric neurons. Neuroscience 1999; 91: 353-62.
16. Harrington AM, Hutson JM, Southwell BR. Immunohistochemical localization of substance P NK1 receptor in guinea pig distal colon. Neurogastroenterol Motil 2005; 17: 727-37.
17. 2 rceptors modulate resting tone in the rat isolated small intestine. Br J Pharmacol 1996; 118: 1262-8.
18. Zagorodnyuk V, Gregory S, Costa M, Tramontana M, Giuliani S, Maggi CA. Spontaneous release of acetylcholine from autonomic nerves in the bladder. Br J Pharmacol 2009; 157: 607-19.
19. Kanazawa M, Palsson OS, Thiwan SI et al. Contributions of pain sensitivity and colonic motility to IBS symptom severity and predominant bowel habits. Am J Gastroenterol 2008; 103: 2550-61.
20. Giachetti A. Pharmacological studies on otilonium bromide. Ital J Gastroenterol 1991; 23(Suppl. 1): 56-9.
21. Strege PR, Evangelista S, Lyford GL, Sarr MG, Farrugia G. Otilonium bromide inhibits calcium entry through L-type calcium channels in human intestinal smooth muscle. Neurogastroenterol Motil 2004; 16: 167-74.
22. Evangelista S, Giachetti A, Chapelain B, Neliat G, Maggi CA. Receptor binding profile of otilonium bromide. Pharmacol Res 1998; 38: 111-7.
23. 14C-Otilonium bromide in the rat: evidence for selective tropism for the large intestine after oral administration. Drug Metab Dispos 2000; 28: 643-7.
24. Narducci F, Bassotti G, Granata MT, Pelli MA, Palumbo R, Morelli A. Colonic motility and gastric emptying in patients with the irritable colon syndrome. Effect of pretreatment with octylonium bromide. Dig Dis Sci 1986; 31: 241-6.
25. Gallego D, Aulí M, Aleu J et al. Effect of otilonium bromide on contractile patterns in the human sigmoid colon. Neurogastroenterol Motil 2010; 22: e180-91.
26. Strege PR, Sha L, Beyden A et al. T-type Ca2+ channel modulation by otilonium bromide. Am J Physiol Gastrointest Liver Physiol 2010; 298: G706-13.
27. 2 receptor stably expressed in chinese hamster ovary cells. Biochem Pharmacol 1999; 57: 899-906.
28. Meini S, Bellucci F, Catalani C et al. Multifaceted approach to determine the antagonist molecular mechanism and interaction of ibodutant ([1-(2-phenyl-1R-[[1-(tetrahydropyran-4-ylmethyl)-piperidin-4-ylmethyl]-carbamoyl]-ethylcarbamoyl)-cyclopentyl]-amide) at the human tachykinin NK2 receptor. J Pharmacol Exp Ther 2009; 329: 486-95.
29. Lecci A, Maggi CA. Pheripheral tachykinin receptors as potential therapeutic targets in visceral disease. Expert Opin Ther Targets 2003; 7: 343-62.
30. Quartara L, Altamura M, Evangelista S, Maggi CA. Tachykinin receptor antagonists in clinical trials. Expert Opin Investig Drugs 2009; 18: 1843-64.