Effects of TAK-480, a novel tachykinin NK2-receptor antagonist, on visceral hypersensitivity in rabbits and ricinoleic acid-induced defecation in guinea pigs

Journal of Pharmacological Sciences

Volumn 120, Issue 1, 2012, Pages 15-25

  Tanaka, Takahiro ^a   Tanaka, Akiko ^a   Nakamura, Akihiro ^a   Matsushita, Kozo ^a   Imanishi, Akio ^a   Matsumoto Okano, Shiho ^a   Inatomi, Nobuhiro ^a   Miura, Kasei ^a   Toyoda, Masao ^b   Mizojiri, Gaku ^b   Tsukimi, Yasuhiro ^a  

^a TAKEDA PHARMACEUTICAL COMPANY LIMITED   (Japan)

^b SAISEIKAI NAKATSU HOSPITAL   (Japan)

Author keywords

Irritable bowel syndrome; Stimulated defecation; TAK 480; Visceral hypersensitivity

Indexed keywords

4 (DIFLUOROMETHOXY) N [2 [[4 (METHOXYMETHYL) 2,3,3A,4,5,9B HEXAHYDRO 1H PYRROLO[3,2 C]QUINOLIN 1 YL]CARBONYL]CYCLOHEXYL]BENZAMIDE; ALOSETRON; NEUROKININ 2 RECEPTOR ANTAGONIST; RICINOLEIC ACID; TAK 480; UNCLASSIFIED DRUG; ZYMOSAN;

ADULT; AGED; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BINDING AFFINITY; COLON DILATATION; CONTROLLED STUDY; DEFECATION; DRUG ACTIVITY; DRUG EFFICACY; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG SAFETY; DRUG STRUCTURE; FEMALE; GUINEA PIG; HUMAN; HUMAN TISSUE; HYPERSENSITIVITY; INTESTINE FUNCTION; IRRITABLE COLON; MALE; NONHUMAN; RABBIT; VISCERAL HYPERSENSITIVITY;

EID: 84866557634     PISSN: 13478613     EISSN: 13478648     Source Type: Journal    
DOI: 10.1254/jphs.12085FP     Document Type: Article

References (36)

1. Longstreth GF, Thompson WG, Chey WD, Houghton LA, Mearin F, Spiller RC. Functional bowel disorders. Gastroenterology. 2006;130:1480-1491.
2. Ritchie J. Pain from distension of the pelvic colon by inflating a balloon in the irritable colon syndrome. Gut. 1973;14:125-132.
3. Sagami Y, Shimada Y, Tayama J, Nomura T, Satake M, Endo Y, et al. Effect of a corticotropin releasing hormone receptor antagonist on colonic sensory and motor function in patients with irritable bowel syndrome. Gut. 2004;53:958-964.
4. Fukudo S, Kanazawa M, Kano M, Sagami Y, Endo Y, Utsumi A, et al. Exaggerated motility of the descending colon with repetitive distention of the sigmoid colon in patients with irritable bowel syndrome. J Gastroenterol. 2002;37 Suppl 14:145-150.
5. Hillila MT, Farkkila MA. Prevalence of irritable bowel syndrome according to different diagnostic criteria in a non-selected adult population. Aliment Pharmacol Ther. 2004;20:339-345.
6. Boyce PM, Koloski NA, Talley NJ. Irritable bowel syndrome according to varying diagnostic criteria: are the new Rome II criteria unnecessarily restrictive for research and practice? Am J Gastroenterol. 2000;95:3176-3183.
7. Crowell MD. Role of serotonin in the pathophysiology of the irritable bowel syndrome. Br J Pharmacol. 2004;141:1285-1293.
8. Holzer P, Holzer-Petsche U. Tachykinins in the gut. Part I. Expression, release and motor function. Pharmacol Ther. 1997;73: 173-217.
9. Lecci A, Capriati A, Maggi CA. Tachykinin NK2 receptor antagonists for the treatment of irritable bowel syndrome. Br J Pharmacol. 2004;141:1249-1263.
10. Shimizu Y, Matsuyama H, Shiina T, Takewaki T, Furness JB. Tachykinins and their functions in the gastrointestinal tract. Cell Mol Life Sci. 2008;65:295-311.
11. Maggi CA. The mammalian tachykinin receptors. Gen Pharmacol. 1995;26:911-944.
12. 2 receptors in human. Auton Neurosci. 2006;126-127:232-249.
13. 2 receptors. J Pharmacol Sci. 2011;117:106-115.
14. 2+ channels in dorsal root ganglia neurons of the adult rat. J Neurophysiol. 2003;90:21-31.
15. 2 receptors in normal and altered rectal sensitivity in rats. Br J Pharmacol. 2000;129:193-199.
16. Kamp EH, Beck DR, Gebhart GF. Combinations of neurokinin receptor antagonists reduce visceral hyperalgesia. J Pharmacol Exp Ther. 2001;299:105-113.
17. 2 receptor antagonist prevents motility- stimulating effects of neurokinin A in small intestine. Br J Pharmacol. 2001;134:215-223.
18. Maggi CA, Giuliani S, Patacchini R, Quartara L, Rovero P, Renzetti AR, et al. Heterogeneity of tachykinin NK-2 receptors in rabbit, guinea-pig and human smooth muscles. Neuropeptides. 1992;23:181-186.
19. 1 receptor antagonists on the viscerosensory response caused by colorectal distention in rabbits. J Pharmacol Exp Ther. 2002; 300:925-931.
20. Awouters F, Megens A, Verlinden M, Schuurkes J, Niemegeers C, Janssen PA. Loperamide. Survey of studies on mechanism of its antidiarrheal activity. Dig Dis Sci. 1993;38:977-995.
21. Emonds-Alt X, Vilain P, Goulaouic P, Proietto V, Van Broeck D, Advenier C, et al. A potent and selective non-peptide antagonist of the neurokinin A (NK2) receptor. Life Sci. 1992;50:PL101-PL106.
22. Cialdai C, Tramontana M, Patacchini R, Lecci A, Catalani C, Catalioto RM, et al. MEN15596, a novel nonpeptide tachykinin NK2 receptor antagonist. Eur J Pharmacol. 2006;549:140-148.
23. Tanaka T, Matsumoto-Okano S, Inatomi N, Fujioka Y, Kamiguchi H, Yamaguchi M, et al. Establishment and validation of a rabbit model for in vivo pharmacodynamic screening of tachykinin NK2 antagonists. J Pharmacol Sci. 2012;118:487-495.
24. Jones RC 3rd, Otsuka E, Wagstrom E, Jensen CS, Price MP, Gebhart GF. Short-term sensitization of colon mechanoreceptors is associated with long-term hypersensitivity to colon distention in the mouse. Gastroenterology. 2007;133:184-194.
25. 2X receptor contributions to colon mechanosensitivity and hypersensitivity in the mouse. Gastroenterology. 2009;137:2096-2104.
26. 2 receptors. Eur J Pharmacol. 1997;337:279-282.
27. Delvaux M, Louvel D, Mamet JP, Campos-Oriola R, Frexinos J. Effect of alosetron on responses to colonic distension in patients with irritable bowel syndrome. Aliment Pharmacol Ther. 1998; 12:849-855.
28. Capasso F, Mascolo N, Autore G, Duraccio MR. Influence of ricinoleic acid on the contractions elicited by PGE2 on the guineapig ileum. J Pharm Pharmacol. 1984;36:64-65.
29. Croci T, Landi M, Emonds-Alt X, Le Fur G, Maffrand JP, Manara L. Role of tachykinins in castor oil diarrhoea in rats. Br J Pharmacol. 1997;121:375-380.
30. 2 receptor antagonist. Neuropeptides. 1997;31:449-458.
31. Camilleri M, Chey WY, Mayer EA, Northcutt AR, Heath A, Dukes GE, et al. A randomized controlled clinical trial of the serotonin type 3 receptor antagonist alosetron in women with diarrhea- predominant irritable bowel syndrome. Arch Intern Med. 2001;161:1733-1740.
32. Lembo T, Wright RA, Bagby B, Decker C, Gordon S, Jhingran P, et al; Lotronex Investigator Team. Alosetron controls bowel urgency and provides global symptom improvement in women with diarrhea-predominant irritable bowel syndrome. Am J Gastroenterol. 2001;96:2662-2670.
33. 3 receptor antagonists on stress-induced colonic hyperalgesia and diarrhoea in rats: a comparative study with opioid receptor agonists, a muscarinic receptor antagonist and a synthetic polymer. Neurogastroenterol Motil. 2008;20:557-565.
34. Chang L, Drossman DA. Rome foundation endpoints and outcomes conference 2009: optimizing clinical trials in FGID. Am J Gastroenterol. 2010;105:722-730.
35. Holzer P, Holzer-Petsche U. Tachykinins in the gut. Part II. Roles in neural excitation, secretion and inflammation. Pharmacol Ther. 1997;73:219-263.
36. Al-Saffar A, Hellström PM. Contractile responses to natural tachykinins and selective tachykinin analogs in normal and inflamed ileal and colonic muscle. Scand J Gastroenterol. 2001;36:485-493.