• 1
    Hoyer D, Hannon JP, Martin GR. Molecular, pharmacological and functional diversity of 5-HT receptors. Pharmacol Biochem Behav 2002; 71: 53354.
  • 2
    Gershon MD. Review article: serotonin receptors and transporters -- roles in normal and abnormal gastrointestinal motility. Aliment Pharmacol Ther 2004; 20(Suppl 7): 314.
  • 3
    Gershon MD, Tack J. The serotonin signaling system: from basic understanding to drug development for functional GI disorders. Gastroenterology 2007; 132: 397414.
  • 4
    Jones BJ, Blackburn TP. The medical benefit of 5-HT research. Pharmacol Biochem Behav 2002; 71: 55568.
  • 5
    Dumuis A, Bouhelal R, Sebben M, Cory R, Bockaert J. A nonclassical 5-hydroxytryptamine receptor positively coupled with adenylate cyclase in the central nervous system. Mol Pharmacol 1988; 34: 8807.
  • 6
    Dumuis A, Sebben M, Bockaert J. The gastrointestinal prokinetic benzamide derivatives are agonists at the non-classical 5-HT receptor (5-HT4) positively coupled to adenylate cyclase in neurons. Naunyn Schmiedebergs Arch Pharmacol 1989; 340: 40310.
  • 7
    Dumuis A, Sebben M, Bockaert J. BRL 24924: a potent agonist at a non-classical 5-HT receptor positively coupled with adenylate cyclase in colliculi neurons. Eur J Pharmacol 1989; 162: 3814.
  • 8
    Bockaert J, Sebben M, Dumuis A. Pharmacological characterization of 5-hydroxytryptamine 4 (5-HT4) receptors positively coupled to adenylate cyclase in adult guinea pig hippocampal membranes: effect of substituted benzamide derivatives. Mol Pharmacol 1990; 37: 40811.
  • 9
    Langlois M, Fischmeister R. 5-HT4 receptor ligands: applications and new prospects. J Med Chem 2003; 46: 31944.
  • 10
    Bockaert J, Claeysen S, Compan V, Dumuis A. 5-HT4 receptors. Curr Drug Targets CNS Neurol Disord 2004; 3: 3951.
  • 11
    Cash BD, Chey WD. Review article: The role of serotonergic agents in the treatment of patients with primary chronic constipation. Aliment Pharmacol Ther 2005; 22: 104760.
  • 12
    Tonini M, Pace F. Drugs acting on serotonin receptors for the treatment of functional GI disorders. Dig Dis 2006; 24: 5969.
  • 13
    Schworer H, Ramadori G. Autoreceptors can modulate 5-hydroxytryptamine release from porcine and human small intestine in vitro. Naunyn Schmiedebergs Arch Pharmacol 1998; 357: 54852.
  • 14
    Grider JR, Kuemmerle JF, Jin JG. 5-HT released by mucosal stimuli initiates peristalsis by activating 5-HT4/5-HT1p receptors on sensory CGRP neurons. Am J Physiol 1996; 270: G77882.
  • 15
    Grider JR, Foxx-Orenstein AE, Jin JG. 5-Hydroxytryptamine4 receptor agonists initiate the peristaltic reflex in human, rat, and guinea pig intestine. Gastroenterology 1998; 115: 37080.
  • 16
    Grider JR. Neurotransmitters mediating the intestinal peristaltic reflex in the mouse. J Pharmacol Exp Ther 2003; 307: 4607.
  • 17
    Foxx-Orenstein AE, Kuemmerle JF, Grider JR. Distinct 5-HT receptors mediate the peristaltic reflex induced by mucosal stimuli in human and guinea pig intestine. Gastroenterology 1996; 111: 128190.
  • 18
    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: G114863.
  • 19
    Briejer MR, Schuurkes JA. 5-HT3 and 5-HT4 receptors and cholinergic and tachykininergic neurotransmission in the guinea-pig proximal colon. Eur J Pharmacol 1996; 308: 17380.
  • 20
    Leclere PG, Lefebvre RA. Presynaptic modulation of cholinergic neurotransmission in the human proximal stomach. Br J Pharmacol 2002; 135: 13542.
  • 21
    De Maeyer JH, Prins NH, Schuurkes JA, Lefebvre RA. Differential effects of 5-hydroxytryptamine4 receptor agonists at gastric versus cardiac receptors: an operational framework to explain and quantify organ-specific behavior. J Pharmacol Exp Ther 2006; 317: 95564.
  • 22
    Prins NH, Van Der Grijn A, Lefebvre RA, Akkermans LM, Schuurkes JA. 5-HT(4) receptors mediating enhancement of contractility in canine stomach; an in vitro and in vivo study. Br J Pharmacol 2001; 132: 19417.
  • 23
    Amemiya N, Hatta S, Takemura H, Ohshika H. Characterization of the contractile response induced by 5-methoxytryptamine in rat stomach fundus strips. Eur J Pharmacol 1996; 318: 4039.
  • 24
    James AN, Ryan JP, Crowell MD, Parkman HP. Regional gastric contractility alterations in a diabetic gastroparesis mouse model: effects of cholinergic and serotoninergic stimulation. Am J Physiol Gastrointest Liver Physiol 2004; 287: G6129.
  • 25
    Takada K, Sakurai-Yamashita Y, Yamashita K et al. Regional difference in correlation of 5-HT4 receptor distribution with cholinergic transmission in the guinea pig stomach. Eur J Pharmacol 1999; 374: 48994.
  • 26
    Takemura K, Takada K, Mameya S, Kaibara M, Taniyama K. Regional and functional differences of 5-hydroxytryptamine-receptor subtypes in guinea pig stomach. Jpn J Pharmacol 1999; 79: 419.
  • 27
    Takeda M, Tsukamoto K, Mizutani Y, Suzuki T, Taniyama K. Identification of SK-951, a novel benzofuran derivative, as an agonist to 5-HT4 receptors. Jpn J Pharmacol 1999; 79: 20312.
  • 28
    Prins NH, Akkermans LM, Lefebvre RA, Schuurkes JA. 5-HT(4) receptors on cholinergic nerves involved in contractility of canine and human large intestine longitudinal muscle. Br J Pharmacol 2000; 131: 92732.
  • 29
    Leclere PG, Prins NH, Schuurkes JA, Lefebvre RA. 5-HT4 receptors located on cholinergic nerves in human colon circular muscle. Neurogastroenterol Motil 2005; 17: 36675.
  • 30
    Briejer MR, Bosmans JP, Van Daele P et al. The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound. Eur J Pharmacol 2001; 423: 7183.
  • 31
    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: 35564.
  • 32
    Xue L, Camilleri M, Locke GR, 3rd, et al. Serotonergic modulation of murine fundic tone. Am J Physiol Gastrointest Liver Physiol 2006; 291: G11806.
  • 33
    Briejer MR, Veen GJ, Akkermans LM, Lefebvre RA, Schuurkes JA. Cisapride and structural analogs selectively enhance 5-hydroxytryptamine (5-HT)-induced purinergic neurotransmission in the guinea pig proximal colon. J Pharmacol Exp Ther 1995; 274: 6418.
  • 34
    Cellek S, John AK, Thangiah R et al. 5-HT4 receptor agonists enhance both cholinergic and nitrergic activities in human isolated colon circular muscle. Neurogastroenterol Motil 2006; 18: 85361.
  • 35
    Baxter GS, Craig DA, Clarke DE. 5-Hydroxytryptamine4 receptors mediate relaxation of the rat oesophageal tunica muscularis mucosae. Naunyn Schmiedebergs Arch Pharmacol 1991; 343: 43946.
  • 36
    Komada T, Yano S. Pharmacological characterization of 5-Hydroxytryptamine-receptor subtypes in circular muscle from the rat stomach. Biol Pharm Bull 2007; 30: 50813.
  • 37
    Tuladhar BR, Costall B, Naylor RJ. Pharmacological characterization of the 5-hydroxytryptamine receptor mediating relaxation in the rat isolated ileum. Br J Pharmacol 1996; 119: 30310.
  • 38
    McLean PG, Coupar IM. Stimulation of cyclic AMP formation in the circular smooth muscle of human colon by activation of 5-HT4-like receptors. Br J Pharmacol 1996; 117: 2389.
  • 39
    Prins NH, Van Haselen JF, Lefebvre RA, Briejer MR, Akkermans LM, Schuurkes JA. Pharmacological characterization of 5-HT4 receptors mediating relaxation of canine isolated rectum circular smooth muscle. Br J Pharmacol 1999; 127: 14317.
  • 40
    Smith AJ, Chappell AE, Buret AG, Barrett KE, Dong H. 5-Hydroxytryptamine contributes significantly to a reflex pathway by which the duodenal mucosa protects itself from gastric acid injury. FASEB J 2006; 20: 248695.
  • 41
    Tuo BG, Sellers Z, Paulus P, Barrett KE, Isenberg JI. 5-HT induces duodenal mucosal bicarbonate secretion via cAMP- and Ca2+ -dependent signaling pathways and 5-HT4 receptors in mice. Am J Physiol Gastrointest Liver Physiol 2004; 286: G44451.
  • 42
    Safsten B, Sjoblom M, Flemstrom G. Serotonin increases protective duodenal bicarbonate secretion via enteric ganglia and a 5-HT4-dependent pathway. Scand J Gastroenterol 2006; 41: 127989.
  • 43
    Kellum JM, Albuquerque FC, Stoner MC, Harris RP. Stroking human jejunal mucosa induces 5-HT release and Cl- secretion via afferent neurons and 5-HT4 receptors. Am J Physiol 1999; 277: G51520.
  • 44
    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: 1258.
  • 45
    Budhoo MR, Harris RP, Kellum JM. The role of the 5-HT4 receptor in Cl- secretion in human jejunal mucosa. Eur J Pharmacol 1996; 314: 10914.
  • 46
    Hansen MB. ICS 205-930 reduces 5-methoxytryptamine-induced short-circuit current in stripped pig jejunum. Can J Physiol Pharmacol 1994; 72: 22732.
  • 47
    Borman RA, Burleigh DE. Human colonic mucosa possesses a mixed population of 5-HT receptors. Eur J Pharmacol 1996; 309: 2714.
  • 48
    Budhoo MR, Harris RP, Kellum JM. 5-Hydroxytryptamine-induced Cl- transport is mediated by 5-HT3 and 5-HT4 receptors in the rat distal colon. Eur J Pharmacol 1996; 298: 13744.
  • 49
    Talley NJ. New and emerging treatments for irritable bowel syndrome and functional dyspepsia. Expert Opin Emerg Drugs 2002; 7: 918.
  • 50
    Galligan JJ, Vanner S. Basic and clinical pharmacology of new motility promoting agents. Neurogastroenterol Motil 2005; 17: 64353.
  • 51
    Schiller LR. New and emerging treatment options for chronic constipation. Rev Gastroenterol Disord 2004; 4(Suppl 2): S4351.
  • 52
    Buchheit KH, Gamse R, Giger R et al. The serotonin 5-HT4 receptor. 2. Structure-activity studies of the indole carbazimidamide class of agonists. J Med Chem 1995; 38: 23318.
  • 53
    Wallenborn J, Gelbrich G, Bulst D et al. Prevention of postoperative nausea and vomiting by metoclopramide combined with dexamethasone: randomised double blind multicentre trial. BMJ 2006; 333: 324.
  • 54
    Valenzuela JE, Dooley CP. Dopamine antagonists in the upper gastrointestinal tract. Scand J Gastroenterol Suppl 1984; 96: 12736.
  • 55
    Parra A, Barron J, Sinibaldi J, Coria I, Espinosa de los Monteros A. Differences in the metoclopramide-induced prolactin release related to age at first full-term pregnancy or nulliparity. Hum Reprod 1997; 12: 2149.
  • 56
    Ohno K, Miyazawa S, Hashiguchi M et al. Establishing a comprehensive questionnaire for detecting drug-induced extrapyramidal symptoms. Yakugaku Zasshi 2003; 123: 8816.
  • 57
    Walkembach J, Bruss M, Urban BW, Barann M. Interactions of metoclopramide and ergotamine with human 5-HT(3A) receptors and human 5-HT reuptake carriers. Br J Pharmacol 2005; 146: 54352.
  • 58
    Talley NJ. Review article: 5-hydroxytryptamine agonists and antagonists in the modulation of gastrointestinal motility and sensation: clinical implications. Aliment Pharmacol Ther 1992; 6: 27389.
  • 59
    Chey WD, Cash BD. Cilansetron: a new serotonergic agent for the irritable bowel syndrome with diarrhoea. Expert Opin Investig Drugs 2005; 14: 18593.
  • 60
    Chang L, Chey WD, Harris L, Olden K, Surawicz C, Schoenfeld P. Incidence of ischemic colitis and serious complications of constipation among patients using alosetron: systematic review of clinical trials and post-marketing surveillance data. Am J Gastroenterol 2006; 101: 106979.
    Direct Link:
  • 61
    Mohammad S, Zhou Z, Gong Q, January CT. Blockage of the HERG human cardiac K+ channel by the gastrointestinal prokinetic agent cisapride. Am J Physiol 1997; 273: H25348.
  • 62
    Rampe D, Roy ML, Dennis A, Brown AM. A mechanism for the proarrhythmic effects of cisapride (Propulsid): high affinity blockade of the human cardiac potassium channel HERG. FEBS Lett 1997; 417: 2832.
  • 63
    Potet F, Bouyssou T, Escande D, Baro I. Gastrointestinal prokinetic drugs have different affinity for the human cardiac human ether-a-gogo K+ channel. J Pharmacol Exp Ther 2001; 299: 100712.
  • 64
    Busti AJ, Murillo JRJ, Cryer B. Tegaserod-induced myocardial infarction: case report and hypothesis. Pharmacotherapy 2004; 24: 52631.
  • 65
    Tack J, Vanden Berghe P, Coulie B, Janssens J. Sumatriptan is an agonist at 5-HT receptors on myenteric neurones in the guinea-pig gastric antrum. Neurogastroenterol Motil 2007; 19: 3946.
  • 66
    Gidener S, Apaydin S, Kupelioglu A, Guven H, Gelal A, Gure A. Serotonin causes acute gastric mucosal injury in rats, probably via 5HT1D receptors. Int J Exp Pathol 1995; 76: 23740.
  • 67
    Kaumann AJ, Parsons AA, Brown AM. Human arterial constrictor serotonin receptors. Cardiovasc Res 1993; 27: 2094103.
  • 68
    Thompson CA. Novartis suspends tegaserod sales at FDA’s request. Am J Health Syst Pharm 2007; 64: 1020.
  • 69
    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: 54960.
  • 70
    Janssen P, Prins NH, Meulemans AL, Lefebvre RA. Smooth muscle 5-HT2A receptors mediating contraction of porcine isolated proximal stomach strips. Br J Pharmacol 2002; 137: 121724.
  • 71
    Glusa E, Pertz HH. Further evidence that 5-HT-induced relaxation of pig pulmonary artery is mediated by endothelial 5-HT(2B) receptors. Br J Pharmacol 2000; 130: 6928.
  • 72
    Ishida T, Kawashima S, Hirata K, Yokoyama M. Nitric oxide is produced via 5-HT1B and 5-HT2B receptor activation in human coronary artery endothelial cells. Kobe J Med Sci 1998; 44: 5163.
  • 73
    Ismair MG, Kullak-Ublick GA, Blakely RD, Fried M, Vavricka SR. Tegaserod inhibits the serotonin transporter SERT. Digestion 2007; 75: 905.
  • 74
    Briejer MR, Prins NH, Schuurkes JA. Effects of the enterokinetic prucalopride (R093877) on colonic motility in fasted dogs. Neurogastroenterol Motil 2001; 13: 46572.
  • 75
    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: 232630.
  • 76
    Claeysen S, Joubert L, Sebben M, Bockaert J, Dumuis A. A single mutation in the 5-HT4 receptor (5-HT4-R D100(3.32)A) generates a Gs-coupled receptor activated exclusively by synthetic ligands (RASSL). J Biol Chem 2003; 278: 699702.
  • 77
    Lopez-Rodriguez ML, Benhamu B, Morcillo MJ et al. 5-HT(4) receptor antagonists: structure-affinity relationships and ligand-receptor interactions. Curr Top Med Chem 2002; 2: 62541.
  • 78
    Kenakin T. Collateral efficacy in new drug discovery. Trends Pharmacol Sci 2007; 28: 35961.
  • 79
    Kenakin T. Collateral efficacy in drug discovery: taking advantage of the good (allosteric) nature of 7TM receptors. Trends Pharmacol Sci 2007; 28: 40715.
  • 80
    Claeysen S, Sebben M, Becamel C, Parmentier ML, Dumuis A, Bockaert J. Constitutively active mutants of 5-HT4 receptors are they in unique active states? EMBO Rep 2001; 2: 617.
  • 81
    Joubert L, Claeysen S, Sebben M et al. A 5-HT4 receptor transmembrane network implicated in the activity of inverse agonists but not agonists. J Biol Chem 2002; 277: 2550211.
  • 82
    Baneres JL, Mesnier D, Martin A, Joubert L, Dumuis A, Bockaert J. Molecular characterization of a purified 5-HT4 receptor: a structural basis for drug efficacy. J Biol Chem 2005; 280: 2025360.
  • 83
    Pindon A, Van Hecke G, Van Gompel P, Lesage AS, Leysen JE, Jurzak M. Differences in signal transduction of two 5-HT4 receptor splice variants: compound specificity and dual coupling with Galphas- and Galphai/o-proteins. Mol Pharmacol 2002; 61: 8596.
  • 84
    Barthet G, Framery B, Gaven F et al. 5-hydroxytryptamine 4 receptor activation of the extracellular signal-regulated kinase pathway depends on Src activation but not on G protein or beta-arrestin signaling. Mol Biol Cell 2007; 18: 197991.
  • 85
    Norum JH, Hart K, Levy FO. Ras-dependent ERK activation by the human G(s)-coupled serotonin receptors 5-HT4(b) and 5-HT7(a). J Biol Chem 2003; 278: 3098104.
  • 86
    Maillet M, Robert SJ, Cacquevel M et al. Crosstalk between Rap1 and Rac regulates secretion of sAPPalpha. Nat Cell Biol 2003; 5: 6339.
  • 87
    Robert S, Maillet M, Morel E et al. Regulation of the amyloid precursor protein ectodomain shedding by the 5-HT4 receptor and Epac. FEBS Lett 2005; 579: 113642.
  • 88
    Talley NJ. Drug therapy options for patients with irritable bowel syndrome. Am J Manag Care 2001; 7: S2617.
  • 89
    De Giorgio R, Barbara G, Furness JB, Tonini M. Novel therapeutic targets for enteric nervous system disorders. Trends Pharmacol Sci 2007; 28: 47381.
  • 90
    Black JW, Shankley NP. Interpretation of agonist affinity estimations: the question of distributed receptor states. Proc R Soc Lond B Biol Sci 1990; 240: 50318.
  • 91
    Medhurst AD, Kaumann AJ. Characterization of the 5-HT4 receptor mediating tachycardia in piglet isolated right atrium. Br J Pharmacol 1993; 110: 102330.
  • 92
    De Maeyer JH, Straetemans R, Schuurkes JA, Lefebvre RA. Porcine left atrial and sinoatrial 5-HT4 receptor-induced responses: fading of the response and influence of development. Br J Pharmacol 2006; 147: 14057.
  • 93
    Kaumann AJ, Sanders L, Brown AM, Murray KJ, Brown MJ. A 5-HT4-like receptor in human right atrium. Naunyn Schmiedebergs Arch Pharmacol 1991; 344: 1509.
  • 94
    Pau D, Workman AJ, Kane KA, Rankin AC. Electrophysiological effects of prucalopride, a novel enterokinetic agent, on isolated atrial myocytes from patients treated with beta-adrenoceptor antagonists. J Pharmacol Exp Ther 2005; 313: 14653.
  • 95
    Kaumann AJ, Lynham JA, Brown AM. Labelling with [125I]-SB 207710 of a small 5-HT4 receptor population in piglet right atrium: functional relevance. Br J Pharmacol 1995; 115: 9336.
  • 96
    Krobert KA, Brattelid T, Levy FO, Kaumann AJ. Prucalopride is a partial agonist through human and porcine atrial 5-HT4 receptors: comparison with recombinant human 5-HT4 splice variants. Naunyn Schmiedebergs Arch Pharmacol 2005; 371: 4739.
  • 97
    Villalon CM, Den Boer MO, Heiligers JP, Saxena PR. Mediation of 5-hydroxytryptamine-induced tachycardia in the pig by the putative 5-HT4 receptor. Br J Pharmacol 1990; 100: 6657.
  • 98
    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: 937.
  • 99
    Vickery RG, Mai N, Kaufman E et al. A comparison of the pharmacological properties of guinea-pig and human recombinant 5-HT4 receptors. Br J Pharmacol 2007; 150: 78291.
  • 100
    Ansanay H, Sebben M, Bockaert J, Dumuis A. Characterization of homologous 5-hydroxytryptamine4 receptor desensitization in colliculi neurons. Mol Pharmacol 1992; 42: 80816.
  • 101
    Ronde P, Ansanay H, Dumuis A, Miller R, Bockaert J. Homologous desensitization of 5-hydroxytryptamine4 receptors in rat esophagus: functional and second messenger studies. J Pharmacol Exp Ther 1995; 272: 97783.
  • 102
    Camilleri M. Review article: tegaserod. Aliment Pharmacol Ther 2001; 15: 27789.
  • 103
    Pittman RN, Reynolds EE, Molinoff PB. Relationship between intrinsic activities of agonists in normal and desensitized tissue and agonist-induced loss of beta adrenergic receptors. J Pharmacol Exp Ther 1984; 230: 6148.
  • 104
    Roettger BF, Ghanekar D, Rao R et al. Antagonist-stimulated internalization of the G protein-coupled cholecystokinin receptor. Mol Pharmacol 1997; 51: 35762.
  • 105
    Thielemans L, Depoortere I, Perret J et al. Desensitization of the human motilin receptor by motilides. J Pharmacol Exp Ther 2005; 313: 1397405.
  • 106
    Barthet G, Gaven F, Framery B et al. Uncoupling and endocytosis of 5-hydroxytryptamine 4 receptors. Distinct molecular events with different GRK2 requirements. J Biol Chem 2005; 280: 2792434.
  • 107
    Mialet J, Fischmeister R, Lezoualc’h F. Characterization of human 5-HT4(d) receptor desensitization in CHO cells. Br J Pharmacol 2003; 138: 44552.
  • 108
    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: 21523.
  • 109
    Ellidokuz E, Kaya D. The effect of metoclopramide on QT dynamicity: double-blind, placebo-controlled, cross-over study in healthy male volunteers. Aliment Pharmacol Ther 2003; 18: 1515.
  • 110
    Kaumann AJ, Lynham JA, Brown AM. Comparison of the densities of 5-HT4 receptors, beta 1- and beta 2-adrenoceptors in human atrium: functional implications. Naunyn Schmiedebergs Arch Pharmacol 1996; 353: 5925.
  • 111
    Sanders L, Lynham JA, Bond B, Del Monte F, Harding SE, Kaumann AJ. Sensitization of human atrial 5-HT4 receptors by chronic beta-blocker treatment. Circulation 1995; 92: 252639.
  • 112
    Pau D, Workman AJ, Kane KA, Rankin AC. Electrophysiological effects of 5-hydroxytryptamine on isolated human atrial myocytes, and the influence of chronic beta-adrenoceptor blockade. Br J Pharmacol 2003; 140: 143441.
  • 113
    Grammer JB, Zeng X, Bosch RF, Kuhlkamp V. Atrial L-type Ca2+ -channel, beta-adrenorecptor, and 5-hydroxytryptamine type 4 receptor mRNAs in human atrial fibrillation. Basic Res Cardiol 2001; 96: 8290.
  • 114
    Brattelid T, Qvigstad E, Lynham JA et al. Functional serotonin 5-HT4 receptors in porcine and human ventricular myocardium with increased 5-HT4 mRNA in heart failure. Naunyn Schmiedebergs Arch Pharmacol 2004; 370: 15766.
  • 115
    Qvigstad E, Brattelid T, Sjaastad I et al. Appearance of a ventricular 5-HT4 receptor-mediated inotropic response to serotonin in heart failure. Cardiovasc Res 2005; 65: 86978.
  • 116
    Qvigstad E, Sjaastad I, Brattelid T et al. Dual serotonergic regulation of ventricular contractile force through 5-HT2A and 5-HT4 receptors induced in the acute failing heart. Circ Res 2005; 97: 26876.
  • 117
    Lezoualc’h F, Steplewski K, Sartiani L, Mugelli A, Fischmeister R, Bril A. Quantitative mRNA analysis of serotonin 5-HT4 receptor isoforms, calcium handling proteins and ion channels in human atrial fibrillation. Biochem Biophys Res Commun 2007; 357: 21824.
  • 118
    Mine Y, Yoshikawa T, Oku S, Nagai R, Yoshida N, Hosoki K. Comparison of effect of mosapride citrate and existing 5-HT4 receptor agonists on gastrointestinal motility in vivo and in vitro. J Pharmacol Exp Ther 1997; 283: 10008.
  • 119
    Talley NJ. Serotoninergic neuroenteric modulators. Lancet 2001; 358: 20618.
  • 120
    Krevsky B, Malmud LS, Maurer AH, Somers MB, Siegel JA, Fisher RS. The effect of oral cisapride on colonic transit. Aliment Pharmacol Ther 1987; 1: 293304.
  • 121
    Bouras EP, Camilleri M, Burton DD, McKinzie S. Selective stimulation of colonic transit by the benzofuran 5HT4 agonist, prucalopride, in healthy humans. Gut 1999; 44: 6826.
  • 122
    Nguyen A, Camilleri M, Kost LJ et al. SDZ HTF 919 stimulates canine colonic motility and transit in vivo. J Pharmacol Exp Ther 1997; 280: 12706.
  • 123
    Tonini M. 5-Hydroxytryptamine effects in the gut: the 3, 4, and 7 receptors. Neurogastroenterol Motil 2005; 17: 63742.