Neurogastroenterology of tegaserod (HTF 919) in the submucosal division of the guinea-pig and human enteric nervous system

Neurogastroenterology and Motility

Volumn 20, Issue 1, 2008, Pages 80-93

  Fang, X ^a,d   Liu, S ^a   Wang, X Y ^a   Gao, N ^a   Hu, H Z ^a   Wang, G D ^a   Cook, C H ^a   Needleman, B J ^a   Mikami, D J ^a   Xia, Y ^a   Fei, G J ^a   Hicks, G A ^b   Wood, J D ^a,c  

^a THE OHIO STATE UNIVERSITY COLLEGE OF MEDICINE   (United States)

^b NOVARTIS PHARMA AG   (Switzerland)

^c OHIO STATE UNIVERSITY   (United States)

^d PEKING UNION MEDICAL COLLEGE HOSPITAL   (China)

Author keywords

5 HT4 serotonergic receptors; Enteric nervous system; Intestine; Secretion

Indexed keywords

CHOLINE ACETYLTRANSFERASE; SEROTONIN 2B RECEPTOR; SEROTONIN 4 RECEPTOR; TEGASEROD; VESICULAR ACETYLCHOLINE TRANSPORTER;

ANIMAL CELL; ANIMAL TISSUE; ARTICLE; AUTONOMIC NERVOUS SYSTEM; CONTROLLED STUDY; DRUG MECHANISM; ELECTRONEUROLOGY; FLUORESCENCE; GUINEA PIG; HUMAN; HUMAN CELL; HUMAN TISSUE; IMMUNOHISTOCHEMISTRY; IMMUNOREACTIVITY; INTESTINE INNERVATION; INTESTINE SECRETION; NEUROBIOLOGY; NEUROMODULATION; NEUROPHYSIOLOGY; NONHUMAN; PERIKARYON; PERIMETER; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN LOCALIZATION; RECEPTOR BLOCKING; SMALL INTESTINE;

ANIMALS; ELECTROPHYSIOLOGY; ENTERIC NERVOUS SYSTEM; GASTRIC MUCOSA; GASTROINTESTINAL AGENTS; GUINEA PIGS; HUMANS; INDOLES; INTESTINE, SMALL; NEURONS; RECEPTORS, SEROTONIN; SEROTONIN;

EID: 37249068113     PISSN: 13501925     EISSN: 13652982     Source Type: Journal    
DOI: 10.1111/j.1365-2982.2007.00983.x     Document Type: Article

References (46)

1. Hoyer D, Clarke DE, Fozard JR et al. International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin). Pharmacol Rev 1994 46 : 157 203.
2. Pindon A, Van Hecke G, Josson K et al. Internalization of human 5-HT4a and 5-HT4b receptors is splice variant dependent. Biosci Rep 2004 24 : 215 23.
3. Degen L, Matzinger D, Merz M et al. Tegaserod, a 5-HT4 receptor partial agonist, accelerates gastric emptying and gastrointestinal transit in healthy male subjects. Aliment Pharmacol Ther 2001 15 : 1745 51.
4. Kellow J, Lee OY, Chang FY et al. An Asia-Pacific, double blind, placebo controlled, randomised study to evaluate the efficacy, safety, and tolerability of tegaserod in patients with irritable bowel syndrome. Gut 2003 52 : 671 6.
5. Johanson JF, Wald A, Tougas G et al. Effect of tegaserod in chronic constipation: a randomized, double-blind, controlled trial. Clin Gastroenterol Hepatol 2004 2 : 796 805.
6. Tack J, Muller-Lissner S, Bytzer P et al. A randomised controlled trial assessing the efficacy and safety of repeated tegaserod therapy in women with irritable bowel syndrome with constipation (IBS-C). Gut 2005 54 : 1707 13.
7. Jin JG, Foxx-Orenstein AE, Grider JR. Propulsion in guinea pig colon induced by 5-hydroxytryptamine (HT) via 5-HT4 and 5-HT3 receptors. J Pharmacol Exp Ther 1999 288 : 93 7.
8. Cooke HJ, Carey HV. Pharmacological analysis of 5-hydroxytryptamine actions on guinea-pig ileal mucosa. Eur J Pharmacol 1985 111 : 329 37.
9. Cooke HJ, Wang YZ, Frieling T, Wood JD. Neural 5-hydroxytryptamine receptors regulate chloride secretion in guinea pig distal colon. Am J Physiol 1991 1 : G833 40.
10. Leung E, Blissard D, Jett MF, Eglen RM. Investigation of the 5-hydroxytryptamine receptor mediating the "transient" short-circuit current response in guinea-pig ileal mucosa. Naunyn Schmiedebergs Arch Pharmacol 1995 351 : 596 602.
11. Scott CM, Bunce KT, Spraggs CF. Investigation of the 5-hydroxytryptamine receptor mediating the 'maintained' short-circuit current response in guinea-pig ileal mucosa. Br J Pharmacol 1992 106 : 877 82.
12. Borman RA, Burleigh DE. Evidence for the involvement of a 5-HT4 receptor in the secretory response of human small intestine to 5-HT. Br J Pharmacol 1993 110 : 927 8.
13. Burleigh DE, Borman RA. Short-circuit current responses to 5-hydroxytryptamine in human ileal mucosa are mediated by a 5-HT4 receptor. Eur J Pharmacol 1993 241 : 125 8.
14. Liu M, Geddis MS, Wen Y, Setlik W, Gershon MD. Expression and function of 5-HT4 receptors in the mouse enteric nervous system. Am J Physiol Gastrointest Liver Physiol 2005 289 : G1148 63.
15. Galligan JJ, Pan H, Messori E. Signalling mechanism coupled to 5-hydroxytryptamine4 receptor-mediated facilitation of fast synaptic transmission in the guinea-pig ileum myenteric plexus. Neurogastroenterol Motil 2003 15 : 523 9.
16. LePard KJ, Ren J, Galligan JJ. Presynaptic modulation of cholinergic and non-cholinergic fast synaptic transmission in the myenteric plexus of guinea pig ileum. Neurogastroenterol Motil 2004 16 : 355 64.
17. Grider JR. Neurotransmitters mediating the intestinal peristaltic reflex in the mouse. J Pharmacol Exp Ther 2003 307 : 460 7.
18. Hu H-Z, Fang X, Liu S et al. Actions of tegaserod in the enteric nervous system of guinea-pig small intestine. Neurogastroenterol Motil 2005 17 : 614.
19. 4 receptor in the small intestine and enteric nervous system of guinea pig and human. Neurogastroenterol Motil 2005 17 : 614.
20. Hu HZ, Gao N, Zhu MX et al. Slow excitatory synaptic transmission mediated by P2Y1 receptors in the guinea-pig enteric nervous system. J Physiol 2003 2 : 493 504.
21. Hanani M, Ermilov LG, Schmalz PF et al. The three-dimensional structure of myenteric neurons in the guinea-pig ileum. J Auton Nerv Syst 1998 71 : 1 9.
22. Weihe E, Tao-Cheng JH, Schafer MK, Erickson JD, Eiden LE. Visualization of the vesicular acetylcholine transporter in cholinergic nerve terminals and its targeting to a specific population of small synaptic vesicles. Proc Natl Acad Sci U S A 1996 93 : 3547 52.
23. Bornstein JC, Furness JB, Kunze WA. Electrophysiological characterization of myenteric neurons: how do classification schemes relate? J Auton Nerv Syst 1994 48 : 1 15.
24. Wood JD. Application of classification schemes to the enteric nervous system. J Auton Nerv Syst 1994 48 : 17 29.
25. Beattie DT, Smith JA, Marquess D et al. The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo. Br J Pharmacol 2004 143 : 549 60.
26. Bender E, Pindon A, van Oers I et al. Structure of the human serotonin 5-HT4 receptor gene and cloning of a novel 5-HT4 splice variant. J Neurochem 2000 74 : 478 89.
27. Ji SW, Park H, Chung JP, Lee SI, Lee YH. Effects of tegaserod on ileal peristalsis of guinea pig in vitro. J Pharmacol Sci 2004 94 : 144 52.
28. Hu HZ, Gao N, Liu S et al. Action of bradykinin in the submucosal plexus of guinea pig small intestine. J Pharmacol Exp Ther 2004 309 : 320 7.
29. Hu HZ, Gao N, Lin Z et al. P2X(7) receptors in the enteric nervous system of guinea-pig small intestine. J Comp Neurol 2001 440 : 299 310.
30. Liu S, Gao X, Gao N et al. Expression of type 1 corticotropin-releasing factor receptor in the guinea pig enteric nervous system. J Comp Neurol 2005 481 : 284 98.
31. Schafer MK, Weihe E, Erickson JD, Eiden LE. Human and monkey cholinergic neurons visualized in paraffin-embedded tissues by immunoreactivity for VAChT, the vesicular acetylcholine transporter. J Mol Neurosci 1995 6 : 225 35.
32. Tonini M, Galligan JJ, North RA. Effects of cisapride on cholinergic neurotransmission and propulsive motility in the guinea pig ileum. Gastroenterology 1989 1 : 1257 64.
33. Tack JF, Janssens W, Janssens J, Vantrappen G, Wood JD. Effect of cisapride on myenteric neurons in the guinea-pig gastric antrum. Neurogastroenterol Motil 1991 3 : A203.
34. Mawe GM. The role of cholecystokinin in ganglionic transmission in the guinea-pig gall-bladder. J Physiol 1991 439 : 89 102.
35. Buchheit KH, Gamse R, Giger R et al. The serotonin 5-HT4 receptor. 1. Design of a new class of agonists and receptor map of the agonist recognition site. J Med Chem 1995 38 : 2326 30.
36. Drolet B, Khalifa M, Daleau P, Hamelin BA, Turgeon J. Block of the rapid component of the delayed rectifier potassium current by the prokinetic agent cisapride underlies drug-related lengthening of the QT interval. Circulation 1998 97 : 204 10.
37. Lin J, Guo J, Gang H, Wojciechowski P, Wigle JT, Zhang S. Intracellular K+ is required for the inactivation-induced high-affinity binding of cisapride to HERG channels. Mol Pharmacol 2005 68 : 855 65.
38. Cooke HJ, Christofi FL. Enteric neural regulation of mucosal secretion. In : Johnson LR, Barrett KE, Ghishan FK, Merchant JL, Said HM, Wood JD, eds. Physiology of the Gastrointestinal Tract, 4th edn. San Diego : Elsevier, 2006 : 737 62.
39. North RA, Surprenant A. Inhibitory synaptic potentials resulting from alpha 2-adrenoceptor activation in guinea-pig submucous plexus neurones. J Physiol 1985 358 : 17 33.
40. Monro RL, Bertrand PP, Bornstein JC. ATP participates in three excitatory postsynaptic potentials in the submucous plexus of the guinea pig ileum. J Physiol 2004 2 : 571 84.
41. Bornstein JC, Furness JB. Correlated electrophysiological and histochemical studies of submucous neurons and their contribution to understanding enteric neural circuits. J Auton Nerv Syst 1988 25 : 1 13.
42. Weber D, Bernhard M, Pfannkuche H-J. The 5-HT4 receptor agonist, tegaserod, stimulates electrolyte/water secretion in the rat colon. Gastroenterology 2004 126 : A147.
43. - efflux from rat colonocytes. Gastroenterology 1999 116 : A648.
44. Carey HV, Cooke HJ. Tonic activity of submucosal neurons influences basal ion transport. Life Sci 1989 44 : 1083 8.
45. McCullough JL, Armstrong SR, Hegde SS, Beattie DT. The 5-HT2B antagonist and 5-HT4 agonist activities of tegaserod in the anaesthetized rat. Pharmacol Res 2006 53 : 353 8.
46. Greenwood-Van Meerveld B, Campbell-Dittmeyer K, Johnson AC, Hicks GA. 5-HT2B receptors do not modulate sensitivity to colonic distension in rats with acute colorectal hypersensitivity. Neurogastroenterol Motil 2006 18 : 343 5.