Gershon MD, Tack J. The serotonin signaling system: from basic understanding to drug development for functional GI disorders. Gastroenterology. 2007;132:397–414.
Article
PubMed
CAS
Google Scholar
Beattie DT, Smith JAM. Serotonin pharmacology in the gastrointestinal tract: a review. Naunyn-Schmiedeberg’s Arch Pharmacol. 2008;377:181–203.
Article
CAS
Google Scholar
McLean PG, Borman RA, Lee K. 5-HT in the enteric nervous system: gut function and neuropharmacology. Trends Neurosci. 2007;30:9–13.
Article
PubMed
CAS
Google Scholar
Degen L, Matzinger D, Merz M, Appel-Dingemanse S, Osborne S, Luchinger S, Bertold R, Maecke H, Beglinger C. Tegaserod, a 5-HT4 receptor partial agonist, accelerates gastric emptying and gastrointestinal transit in healthy male subjects. Aliment Pharmacol Ther. 2001;15:1745–51.
Article
PubMed
CAS
Google Scholar
Prather CM, Camilleri M, Zinsmeister AR, McKinzie S, Thomforde G. Tegaserod accelerates orocecal transit in patients with constipation-predominant irritable bowel syndrome. Gastroenterology. 2000;118:463–8.
Article
PubMed
CAS
Google Scholar
De Maeyer JH, Lefebvre RA, Schuurkes JAJ. 5-HT4 receptor agonists: similar but not the same. Neurogastroenterol Motil. 2008;20:99–112.
Article
PubMed
CAS
Google Scholar
Coffin B, Farmachidi JP, Rueegg P, Bastie A, Bouhassira D. Tegaserod, a 5-HT4 receptor partial agonist, decreases sensitivity to rectal distension in healthy subjects. Aliment Pharmacol Ther. 2003;17:577–85.
Article
PubMed
CAS
Google Scholar
Greenwood-Van Meerveld B, Venkova K, Hicks G, Dennis E, Crowell MD. Activation of peripheral 5-HT4 receptors attenuates colonic sensitivity to intraluminal distension. Neurogastroenterol Motil. 2006;18:76–86.
Article
PubMed
CAS
Google Scholar
Grider JR, Foxx-Orenstein AE, Jin JG. 5-Hydroxytryptamine4 receptor agonists initiate the peristaltic reflex in human, rat, and guinea pig intestine. Gastroenterology. 1998;115:370–80.
Article
PubMed
CAS
Google Scholar
Hoffman JM, Tyler K, MacEachern SJ, Balemba OB, Johnson AC, Brooks EM, Zhao H, Swain GM, Moses PL, Galligan JJ, et al. Activation of colonic mucosal 5-HT4 receptors accelerates propulsive motility and inhibits visceral hypersensitivity. Gastroenterology. 2012;142(844–54):e4.
Google Scholar
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;94:142–52.
Article
Google Scholar
McGuire C, Boundouki G, Hockley JRF, Reed D, Cibert-Goton V, Peiris M, Kung V, Broad J, Aziz Q, Chan C, et al. Ex vivo study of human visceral nociceptors. Gut. 2017;67:86–96.
Article
Google Scholar
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.
Article
PubMed
CAS
Google Scholar
Grider JR. Desensitization of the peristaltic reflex induced by mucosal stimulation with the selective 5-HT4 agonist tegaserod. Am J Physiol. 2006;290:319–27.
Google Scholar
Nedi T, White PJ, Coupar IM, Irving HR. Tissue dependent differences in G-protein coupled receptor kinases associated with 5-HT4 receptor desensitization in the rat gastro-intestinal tract. Biochem Pharmacol. 2011;81:123–33.
Article
PubMed
CAS
Google Scholar
Ansanay H, Sebben M, Bockaert J, Dumuis A. Characterization of homologous 5-hydroxytryptamine4 receptor desensitization in colliculi neurons. Mol Pharmacol. 1992;42:808–16.
PubMed
CAS
Google Scholar
Rondé 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;272:977–83.
PubMed
Google Scholar
Barthet G, Carrat G, Cassier E, Barker B, Gaven F, Pillot M, Framery B, Pellissier LP, Augier J, Kang DS, et al. Β-arrestin1 phosphorylation by GRK5 regulates G protein-independent 5-HT4 receptor signalling. EMBO J. 2009;28:2706–18.
Article
PubMed
PubMed Central
CAS
Google Scholar
Barthet G, Gaven F, Framery B, Shinjo K, Nakamura T, Claeysen S, Bockaert J, Dumuis A. Uncoupling and endocytosis of 5-hydroxytryptamine 4 receptors: distinct molecular events with different GRK2 requirements. J Biol Chem. 2005;280:27924–34.
Article
PubMed
CAS
Google Scholar
Mnie-Filali O, Amraei MG, Benmbarek S, Archer-Lahlou E, Peñas-Cazorla R, Vilaró MT, Boye SM, Piñeyro G. Serotonin 4 receptor (5-HT4R) internalization is isoform-specific: effects of 5-HT and RS67333 on isoforms A and B. Cell Signal. 2010;22:501–9.
Article
PubMed
CAS
Google Scholar
Ahmed MR, Gurevich V, Dalby KN, Benovic JL, Gurevich EV. Haloperidol and clozapine differentially affect the expression of arrestins, receptor kinases, and extracellular signal-regulated kinase activation. J Pharmacol Exp Ther. 2008;325:276–83.
Article
PubMed
PubMed Central
CAS
Google Scholar
Fan X, Zhang J, Zhang X, Yue W, Ma L. Acute and chronic morphine treatments and morphine withdrawal differentially regulate GRK2 and GRK5 gene expression in rat brain. Neuropharmacol. 2002;43:809–16.
Article
CAS
Google Scholar
Miralles A, Asensio VJ, Garcia-Sevilla JA. Acute treatment with the cyclic antidepressant desipramine, but not fluoxetine, increases membrane-associated G protein-coupled receptor kinases 2/3 in rat brain. Neuropharmacol. 2002;443:1249–57.
Article
Google Scholar
Diaz A, Pazos A, Florez J, Ayesta FJ, Santana V, Hurle MA. Regulation of mu-opioid receptors, G-protein-coupled receptor kinases and beta-arrestin 2 in the rat brain after chronic opioid receptor antagonism. Neuroosci. 2002;112:345–53.
Article
CAS
Google Scholar
Hurle MA. Changes in the expression of G protein-coupled receptor kinases and beta-arrestin 2 in rat brain during opioid tolerance and supersensitivity. J Neurochem. 2001;77:486–92.
Article
PubMed
CAS
Google Scholar
Gainetdinov RR, Premont RT, Bohn LM, Lefkowitz RJ, Caron MG. Desensitization of G protein-coupled receptors and neuronal functions. Annu Rev Neurosci. 2004;27:107–44.
Article
PubMed
CAS
Google Scholar
Armstrong SR, McCullough JL, Beattie DT. Measurement of 5-HT4 receptor-mediated esophageal responses by digital sonomicrometry in the anesthetized rat. J Pharmacol Toxicol Meth. 2006;53:198–205.
Article
CAS
Google Scholar
Beattie DT, Armstrong SR, Shaw JP, Marquess D, Sandlund C, Smith JA, Taylor JA, Humphrey PP. The in vivo gastrointestinal activity of TD-5108, a selective 5-HT(4) receptor agonist with high intrinsic activity. Naunyn-Schmiedeberg’s Arch Pharmacol. 2008;378:139–47.
Article
CAS
Google Scholar
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.
Article
PubMed
CAS
Google Scholar
Beattie DT, Smith JA, Marquess D, Vickery RG, Armstrong SR, Pulido-Rios T, McCullough JL, Sandlund C, Richardson C, Mai N, Humphrey PP. 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.
Article
PubMed
PubMed Central
CAS
Google Scholar
Baxter GS, Craig DA, Clarke DE. 5-Hydroxytryptamine4 receptors mediate relaxation of the rat oesophageal tunica muscularis mucosae. Naunyn-Schmiedeberg’s Arch Pharmacol. 1991;343:439–46.
Article
CAS
Google Scholar
Poole DP, Xu B, Koh SL, Hunne B, Coupar IM, Irving HR, Shinjo K, Furness JB. Identification of neurons that express 5-hydroxytryptamine-4 receptors in the intestine. Cell Tissue Res. 2006;325:413–22.
Article
PubMed
CAS
Google Scholar
Premont RT, Gainetdinov RR. Physiological roles of G protein-coupled receptor kinases and arrestins. Annu Rev Physiol. 2007;69:511–34.
Article
PubMed
CAS
Google Scholar
Bahouth SW, Nooh MM. Barcoding of GPCR trafficking and signaling through the various trafficking roadmaps by compartmentalized signaling networks. Cell Signal. 2017;36:42–55.
Article
PubMed
CAS
PubMed Central
Google Scholar
Clark RB, Knoll BJ, Barber R. Partial agonists and G protein-coupled receptor desensitization. Trends Pharmacol Sci. 1999;20:279–86.
Article
PubMed
CAS
Google Scholar
Burgos-Ramos E, Puebla-Jimenez L, Arilla-Ferreiro E. Minocycline provides protection against beta-amyloid(25-35)-induced alterations of the somatostatin signaling pathway in the rat temporal cortex. Neurooscience. 2008;154:1458–66.
Article
CAS
Google Scholar
Matuzany-Ruban A, Golan M, Miroshnik N, Schreiber G, Avissar S. Normalization of GRK2 protein and mRNA measures in patients with depression predict response to antidepressants. Int J Neuropsychopharmacol. 2009;2009:1–9.
Google Scholar
Wu H, Wei W, Song L, Zhang L, Chen Y, Hu X. Paeoniflorin induced immune tolerance of mesenteric lymph node lymphocytes via enhancing beta 2-adrenergic receptor desensitization in rats with adjuvant arthritis. Int Immunopharmacol. 2007;7:662–73.
Article
PubMed
CAS
Google Scholar
Dzimiri N, Muiya P, Andres E, Al-Halees Z. Differential functional expression of human myocardial G protein receptor kinases in left ventricular cardiac diseases. Eur J Pharmacol. 2004;489:162–77.
Article
CAS
Google Scholar
Grange-Midroit M, Garcia-Sevilla JA, Ferrer-Alcon M, La Harpe R, Walzer C, Guimon J. G protein-coupled receptor kinases, beta-arrestin-2 and associated regulatory proteins in the human brain: postmortem changes, effect of age and subcellular distribution. Brain Res Mol Brain Res. 2002;101:39–51.
Article
PubMed
CAS
Google Scholar