Metabolic Kinetics of 5-Hydroxytryptamine and the Research Targets of Functional Gastrointestinal Disorders

Digestive Diseases and Sciences

Volumn 59, Issue 11, 2014, Pages 2642-2648

  Jing, Fuchun ^a,b   Zhang, Jun ^a  

^a XI'AN JIAOTONG UNIVERSITY   (China)

^b Department of Clinical Laboratory   (China)

Author keywords

5 Hydroxytryptamine; Functional gastrointestinal disorders; Metabolic kinetics; Research targets

Indexed keywords

SEROTONIN; SEROTONIN RECEPTOR; SEROTONIN TRANSPORTER; SEROTONIN UPTAKE INHIBITOR; SLC6A4 PROTEIN, HUMAN;

BLOOD BRAIN BARRIER; CENTRAL NERVOUS SYSTEM; DIGESTIVE SYSTEM FUNCTION DISORDER; HUMAN; KINETICS; MEDICAL RESEARCH; METABOLIC KINETICS; METABOLIC REGULATION; NONHUMAN; PRIORITY JOURNAL; REVIEW; SEROTONIN RELEASE; SEROTONINERGIC NERVE CELL; CLASSIFICATION; GASTROINTESTINAL DISEASE; GASTROINTESTINAL MOTILITY; METABOLISM;

GASTROINTESTINAL DISEASES; GASTROINTESTINAL MOTILITY; HUMANS; RECEPTORS, SEROTONIN; SEROTONIN; SEROTONIN PLASMA MEMBRANE TRANSPORT PROTEINS; SEROTONIN UPTAKE INHIBITORS;

EID: 84922394415     PISSN: 01632116     EISSN: 15732568     Source Type: Journal    
DOI: 10.1007/s10620-014-3244-x     Document Type: Review

References (84)

1. Drossman DA. The functional gastrointestinal disorders and the Rome III process. Gastroenterology. 2006;130:1377–1390.
2. Mayer EA, Gebhart GF. Basic and clinical aspects of visceral hyperalgesia. Gastroenterology. 1994;107:271–293.
3. Cervero F, Laird JM. Visceral pain. Lancet. 1999;353:2145–2148.
4. Gershon MD, Tack J. The serotonin signaling system: from basic understanding to drug development for functional GI disorders. Gastroenterology. 2007;132:397–414.
5. Tosic-Golubovic S, Miljkovic S, Nagorni A, et al. Irritable bowel syndrome, anxiety, depression and personality characteristics. Psychiatria Danubina. 2010;22:418–424.
6. Locke GR, Weaver AL, Melton LJ, Talley NJ. Psychosocial factors are linked to functional gastrointestinal disorders: a population based nested case–control study. Am J Gastroenterol. 2004;99:350–357.
7. Miwa H, Nakajima K, Yamaguchi K, et al. Generation of dyspeptic symptoms by direct acid infusion into the stomach of healthy Japanese subjects. Aliment Pharmacol Ther. 2007;26:257–264.
8. Moayyedi P, Deeks J, Talley NJ, Delaney B, Forman D. An update of the Cochrane systematic review of Helicobacter pylori eradication therapy in nonulcer dyspepsia: resolving the discrepancy between systematic reviews. Am J Gastroenterol. 2003;98:2621–2626.
9. Gathaiya N, Locke GR, Camilleri M, Schleck CD, Zinsmeister AR, Talley NJ. Novel associations with dyspepsia: a community-based study of familial aggregation, sleep dysfunction and somatization. Neurogastroenterol Motil. 2009;21:922-e69.
10. Feinle-Bisset C, Azpiroz F. Dietary and lifestyle factors in functional dyspepsia. Nat Rev Gastroenterol Hepatol. 2013;10:150–157.
11. Mahadeva S, Yadav H, Rampal S, Goh KL. Risk factors associated with dyspepsia in a rural Asian population and its impact on quality of life. Am J Gastroenterol. 2010;105:904–912.
12. Erspamer V. Historical introduction: the Italian contribution to the discovery of 5-hydroxytryptamine (enteramine, serotonin). J Hypertens Suppl. 1986;4:S3–S5.
13. Rapport MM, Green AA, Page IH. Serum vasoconstrictor, serotonin; isolation and characterization. J Biol Chem. 1948;176:1243–1251.
14. Nichols DE, Nichols CD. Serotonin receptors. Chem Rev. 2008;108:1614–1641.
15. Berger M, Gray JA, Roth BL. The expanded biology of serotonin. Annu Rev Med. 2009;60:355–366.
16. Feijó FM, Bertoluci MC, Reis C. Serotonin and hypothalamic control of hunger: a review. Rev Assoc Med Bras. 2011;57:74–77.
17. Camilleri M. Serotonin in the gastrointestinal tract. Curr Opin Endocrinol Diabetes Obes. 2009;16:53–59.
18. Manocha M, Khan W. Serotonin and GI disorders: an update on clinical and experimental studies. Clin Transl Gastroenterol. 2012;3:1–6.
19. Walther DJ, Peter JU, Bashammakh S, et al. Synthesis of serotonin by a second tryptophan hydroxylase isoform. Science. 2003;299:76.
20. Cote F, Thevenot E, Fligny C, et al. Disruption of the nonneuronal tph1 gene demonstrates the importance of peripheral serotonin in cardiac function. Proc Natl Acad Sci USA. 2003;100:13525–13530.
21. Walther DJ, Bader M. A unique central tryptophan hydroxylase isoform. Biochem Pharmacol. 2003;66:1673–1680.
22. Schafermeyer A, Gratzl M, Rad R, et al. Isolation and receptor profiling of ileal enterochromaffin cells. Acta Physiol Scand. 2004;182:53–62.
23. Fujimiya M, Okumiya K, Kuwahara A. Immunoelectron microscopic study of the luminal release of serotonin from rat enterochromaffin cells induced by high intraluminal pressure. Histochem Cell Biol. 1997;108:105–113.
24. Wade PR, Chen J, Jaffe B, et al. Localization and function of a 5-HT transporter in crypt epithelia of the gastrointestinal tract. J Neurosci. 1996;16:2352–2364.
25. Houghton LA, Atkinson W, Whitaker RP, Whorwell PJ, Rimmer MJ. Increased platelet depleted plasma 5-hydroxytryptamine concentration following meal ingestion in symptomatic female subjects with diarrhoea predominant irritable bowel syndrome. Gut. 2003;52:663–670.
26. Dunlop SP, Coleman NS, Blackshaw E, et al. Abnormalities of 5-hydroxytryptamine metabolism in irritable bowel syndrome. Clin Gastroenterol Hepatol. 2005;3:349–357.
27. Atkinson W, Lockhart S, Whorwell PJ, Keevil B, Houghton LA. Altered 5-hydroxytryptamine signaling in patients with constipation- and diarrhea-predominant irritable bowel syndrome. Gastroenterology. 2006;130:34–43.
28. Brown PM, Drossman DA, Wood AJ, et al. The tryptophan hydroxylase inhibitor LX1031 is effective for patients with nonconstipating irritable bowel syndrome. Gastroenterology. 2011;141:507–516.
29. Wang H, Steeds J, Motomura Y, et al. CD4+ T cell-mediated immunological control of enterochromaffin cell hyperplasia and 5-hydroxytryptamine production in enteric infection. Gut. 2007;56:949–957.
30. Nakamura K, Sato T, Ohashi A, et al. Role of a serotonin precursor in development of gut microvilli. Am J Pathol. 2008;172:333–344.
31. Muller T, Durk T, Blumenthal B, et al. 5-hydroxytryptamine modulates migration, cytokine and chemokine release and T-cell priming capacity of dendritic cells in vitro and in vivo. PLoS One. 2009;4:e6453.
32. Haub S, Ritze Y, Bergheim I, et al. Enhancement of intestinal inflammation in mice lacking interleukin 10 by deletion of the serotonin reuptake transporter. Neurogastroenterol Motil. 2010;22:826–834.
33. Cloez-Tayarani I, Changeux JP. Nicotine and serotonin in immune regulation and inflammatory processes: a perspective. J Leukoc Biol. 2007;81:599–606.
34. Kushnir-Sukhov NM, Brown JM, Wu Y, et al. Human mast cells are capable of serotonin synthesis and release. J Allergy Clin Immunol. 2007;119:498–499.
35. O’Connell PJ, Wang X, Leon-Ponte M, et al. A novel form of immune signaling revealed by transmission of the inflammatory mediator serotonin between dendritic cells and T cells. Blood. 2006;107:1010–1017.
36. Foley S, Garsed K, Singh G, et al. Impaired uptake of serotonin by platelets from patients with irritable bowel syndrome correlates with duodenal immune activation. Gastroenterology. 2011;140:1434–1443.
37. Bearcroft CP, Perrett D, Farthing MJ. 5-hydroxytryptamine release into human jejunum by cholera toxin. Gut. 1996;39:528–531.
38. Fukumoto S, Tatewaki M, Yamada T, et al. Short-chain fatty acids stimulate colonic transit via intraluminal 5-HT release in rats. Am J Physiol Regul Integr Comp Physiol. 2003;284:R1269–R1276.
39. Kim M, Cooke HJ, Javed NH, et al. d-Glucose releases 5-hydroxytryptamine from human BON cells as a model of enterochromaffin cells. Gastroenterology. 2001;121:1400–1406.
40. O’Mahony L, McCarthy J, Kelly P, et al. Lactobacillus and bifidobacterium in irritable bowel syndrome: symptom responses and relationship to cytokine profiles. Gastroenterology. 2005;128:541–551.
41. Whorwell PJ, Altringer L, Morel J, et al. Efficacy of an encapsulated probiotic Bifidobacterium infantis 35624 in women with irritable bowel syndrome. Am J Gastroenterol. 2006;101:1581–1590.
42. Brenner DM, Moeller MJ, Chey WD, Schoenfeld PS. The utility of probiotics in the treatment of irritable bowel syndrome: a systematic review. Am J Gastroenterol. 2009;104:1033–1049.
43. Moayyedi P, Ford AC, Talley NJ, et al. The efficacy of probiotics in the treatment of irritable bowel syndrome: a systematic review. Gut. 2010;59:325–332.
44. Masand PS, Gupta S, Schwartz TL, et al. Paroxetine in patients with irritable bowel syndrome: a pilot open-label study. Prim Care Companion J Clin Psychiatry. 2002;4:12–16.
45. Masand PS, Gupta S, Schwartz TL, Virk S, Hameed A, Kaplan DS. Open-label treatment with citalopram in patients with irritable bowel syndrome: a pilot study. Prim Care Companion J Clin Psychiatry. 2005;7:162–166.
46. Creed F, Fernandes L, Guthrie E, et al. North of England IBS Research Group. The cost-effectiveness of psychotherapy and paroxetine for severe irritable bowel syndrome. Gastroenterology. 2003;124:303–317.
47. Kuiken SD, Tytgat GN, Boeckxstaens GE. The selective serotonin reuptake inhibitor fluoxetine does not change rectal sensitivity and symptoms in patients with irritable bowel syndrome: a double blind, randomized, placebo-controlled study. Clin Gastroenterol Hepatol. 2003;1:219–228.
48. Tack J, Broekaert D, Corsetti M, Fischler B, Janssens J. Influence of acute serotonin reuptake inhibition on colonic sensorimotor function in man. Aliment Pharmacol Ther. 2006;23:265–274.
49. Broekaert D, Fischler B, Sifrim D, Janssens J, Tack J. Influence of citalopram, a selective serotonin reuptake inhibitor, on oesophageal hypersensitivity: a double-blind, placebo-controlled study. Aliment Pharmacol Ther. 2006;23:365–370.
50. Tabas G, Beaves M, Wang J, et al. Paroxetine to treat irritable bowel syndrome not responding to high-fiber diet: a double-blind, placebo-controlled trial. Am J Gastroenterol. 2004;99:914–920.
51. Vahedi H, Merat S, Rashidioon A, Ghoddoosi A, Malekzadeh R. The effects of fluoxetine in patients with pain and constipation-predominant irritable bowel syndrome: a doubleblind randomized-controlled study. Aliment Pharmacol Ther. 2005;22:381–385.
52. Barkin RL, Barkin SJ. Antidepressants for the management of pain in geriatric patients. Anesth Today. 2004;15:23–26.
53. Bradley RH, Barkin RL, Jerome J, DeYoung K, Dodge CW. Efficacy of venlafaxine for the long term treatment of chronic pain with associated major depressive disorder. Am J Ther. 2003;10:318–323.
54. Mayer EA, Tillisch K, Bradesi S. Review article: modulation of the brain-gut axis as a therapeutic approach in gastrointestinal disease. Aliment Pharmacol Ther. 2006;24:919–933.
55. Kim DY, Camilleri M. Serotonin: a mediator of the brain–gut connection. Am J Gastroenterol. 2000;95:2698–2709.
56. Hoyer D, Hannon JP, Martin GR. Molecular, pharmacological and functional diversity of 5-HT receptors. Pharmacol Biochem Behav. 2002;71:533–554.
57. Briejer MR, Mathis C, Schuurkes JA. 5-HT receptor types in the rat ileum longitudinal muscle: focus on 5-HT2 receptors mediating contraction. Neurogastroenterol Motil. 1997;9:231–237.
58. Gershon MD. 5-HT (serotonin) physiology and related drugs. Curr Opin Gastroenterol. 2000;16:113–120.
59. Coulie B, Tack J, Maes B, Geypens B, De Roo M, Janssens J. Sumatriptan, a selective 5-HT1 receptor agonist, induces a lag phase for gastric emptying of liquids in humans. Am J Physiol. 1997;272:G902–G908.
60. Tuladhar BR, Ge L, Naylor RJ. 5-HT(7) receptors mediate the inhibitory effect of 5-HT on peristalsis in the isolated guinea-pig ileum. Br J Pharmacol. 2003;138:1210–1214.
61. Prause A, Stoffel M, Portier C, Mevissen M. Expression and function of 5-HT7 receptors in smooth muscle preparations from equine duodenum, ileum, and pelvic flexure. Res Vet Sci. 2009;87:292–299.
62. Tack J, Piessevaux H, Coulie B, et al. A placebo-controlled trial of buspirone, a fundus-relaxing drug, in functional dyspepsia: effect on symptoms and gastric sensory and motor function. Gastroenterology. 1999;116:A325.
63. Chial HJ, Camilleri M, Ferber I, et al. Effects of venlafaxine, buspirone, and placebo on colonic sensorimotor functions in healthy humans. Clin Gastroenterol Hepatol. 2003;1:211–218.
64. O’Mahony SM, Bulmer DC, Coelho AM, et al. 5-HT(2B) receptors modulate visceral hypersensitivity in a stress-sensitive animal model of brain–gut axis dysfunction. Neurogastroenterol Motil. 2010;22:573–578.
65. Kim S-K, Li Y, Abrol R, et al. Predicted structures and dynamics for agonists and antagonists bound to serotonin 5-HT2B and 5-HT2C receptors. J Chem Inf Model. 2011;51:420–433.
66. Aapro MS. 5-HT3 receptor antagonists. An overview of their present status and future potential in cancer therapy-induced emesis. Drugs. 1991;42:551–568.
67. 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.
68. Bearcroft CP, Andre EA, Farthing MJ. In vivo effects of the 5-HT3 antagonist alosetron on basal and cholera toxin-induced secretion in the human jejunum: a segmental perfusion study. Aliment Pharmacol Ther. 1997;11:1109–1114.
69. Talley NJ, Phillips SF, Haddad A, et al. GR38032F (ondansetron), a selective 5-HT3 receptor antagonist, slows colonic transit in healthy human. Dig Dis Sci. 1990;35:477–480.
70. Horton R. Lotronex and the FDA: a fatal erosion of integrity. Lancet. 2001;357:1544–1545.
71. Friedel D, Thomas R, Fisher RS. Ischemic colitis during treatment with alosetron. Gastroenterology. 2001;120:557–560.
72. Asagarasu A, Matsui T, Hayashi H, et al. Discovery of a novel 5-HT(3) antagonist/5-HT(1A) agonist 3-amino-5,6,7,8-tetrahydro-2-{4-[4-(quinolin-2-yl) piperazin-1-yl]butyl} quinazolin-4 (3H)-one (TZB-30878) as an orally bioavailable agent for irritable bowel syndrome. J Med Chem. 2010;53:7549–7563.
73. Hee Sun KIM. 5-Hydroxytryptamine4 receptor agonists and colonic motility. J Smooth Muscle Res. 2009;45:25–29.
74. Lewin MB, Bryant RM, Fenrich AL, Grifka RG. Cisapride-induced long QT interval. J Pediatr. 1996;128:279–281.
75. Emmanuel AV, Kamm MA, Roy AJ, Kerstens R, Vandeplassche L. Randomised clinical trial: the efficacy of prucalopride in patients with chronic intestinal pseudo-obstruction—a double-blind, placebo-controlled, cross-over, multiple n = 1 study. Aliment Pharmacol Ther. 2012;35:48–55.
76. Goldberg M, Li YP, Johanson JF, et al. Clinical trial: the efficacy and tolerability of velusetrag, a selective 5-HT4 agonist with high intrinsic activity, in chronic idiopathic constipation—a 4-week, randomized, double-blind, placebo-controlled, dose-response study. Aliment Pharmacol Ther. 2010;32:1102–1112.
77. Camilleri M, Vazquez-Roque MI, Burton D, et al. Pharmacodynamic effects of a novel prokinetic 5-HT receptor agonist, ATI-7505, in humans. Neurogastroenterol Motil. 2007;19:30–38.
78. 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.
79. Prins NH, Briejer MR, Van Bergen PJ, Akkermans LM, Schuurkes JA. Evidence for 5-HT7 receptors mediating relaxation of human colonic circular smooth muscle. Br J Pharmacol. 1999;128:849–852.
80. Dahlstrom A, Fuxe K. Localization of monoamines in the lower brain stem. Experientia. 1964;20:398–399.
81. Charnay Y, Leger L. Brain serotonergic circuitries. Dialogues Clin Neurosci. 2010;12:471–487.
82. Lydiard RB. Irritable bowel syndrome, anxiety, and depression: what are the links? J Clin Psychiatry. 2001;62:38–45.
83. Dekel R, Drossman DA, Sperber AD. The use of psychotropic drugs in irritable bowel syndrome. Expert Opin Investig Drugs. 2013;22:329–339.
84. Grover M, Camilleri M. Effects on gastrointestinal functions and symptoms of serotonergic psychoactive agents used in functional gastrointestinal diseases. J Gastroenterol. 2013;48:177–181.