Investigations into the binding affinities of different human 5-HT 4 receptor splice variants

Pharmacology

Volumn 85, Issue 4, 2010, Pages 224-233

  Irving, Helen R ^a   Tochon Danguy, Nathalie ^a   Chinkwo, Kenneth A ^a   Li, Jian G ^a   Grabbe, Carmen ^a   Shapiro, Marina ^a   Pouton, Colin W ^a   Coupar, Ian M ^a  

^a MONASH UNIVERSITY   (Australia)

Author keywords

5 HT4 receptor agonists; 5 HT4 receptor splice variants; Prucalopride; Tegaserod; Zacopride

Indexed keywords

1 (4 AMINO 5 CHLORO 2 METHOXYPHENYL) 3 (1 BUTYL 4 PIPERIDINYL) 1 PROPANONE; 1 METHYL 3 INDOLECARBOXYLIC ACID [1 [2 (METHYLSULFONYLAMINO)ETHYL] 4 PIPERIDINYLMETHYL] ESTER; 3 ETHYL 2,3 DIHYDRO 2 OXO 1 BENZIMIDAZOLECARBOXYLIC ACID 3ALPHA TROPANYLAMIDE; 4 AMINO N [1 [3 (BENZYLSULFONYL)PROPYL] 4 PIPERIDINYLMETHYL] 5 CHLORO 2 METHOXYBENZAMIDE; BENZAMIDE; BENZIMIDAZOLE DERIVATIVE; DAU 6236; ENDO 8 METHYL 8 AZABICYCLO(3.2.1)OCT 3 YL 2,3 DIHYDRO 3 ETHYL 2 OXO 1H BENZIMIDAZOLE 1 CARBOXYLATE HYDROCHLORIDE; PRUCALOPRIDE; RENZAPRIDE; SEROTONIN 4 AGONIST; SEROTONIN 4 RECEPTOR; SEROTONIN 4A RECEPTOR; SEROTONIN 4B RECEPTOR; SEROTONIN 4C RECEPTOR; SEROTONIN 4D RECEPTOR; SEROTONIN 4G RECEPTOR; SEROTONIN CREATININE SULFATE; TEGASEROD; UNCLASSIFIED DRUG; ZACOPRIDE;

AGONIST; ANIMAL CELL; ARTICLE; BINDING AFFINITY; CONSTIPATION; CONTROLLED STUDY; DRUG BINDING SITE; DRUG RECEPTOR BINDING; HUMAN; IRRITABLE COLON; LIGAND BINDING; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN VARIANT; RECEPTOR AFFINITY;

ANILINE COMPOUNDS; ANIMALS; BENZAMIDES; BENZIMIDAZOLES; BENZOFURANS; BICYCLO COMPOUNDS, HETEROCYCLIC; BINDING SITES; BINDING, COMPETITIVE; CERCOPITHECUS AETHIOPS; COS CELLS; CYCLIC AMP; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; INDOLES; KINETICS; LIGANDS; PIPERIDINES; PROTEIN ISOFORMS; RECEPTORS, SEROTONIN, 5-HT4; SEROTONIN ANTAGONISTS;

EID: 77951475671     PISSN: 00317012     EISSN: None     Source Type: Journal    
DOI: 10.1159/000280418     Document Type: Article

References (28)

1. Blondel O, Vandecasteele G, Gastineau M, Leclerc S, Dahmoune Y, Langlois M, Fischmeister R: Molecular and functional characterisation of a 5-HT 4 receptor cloned from human atrium. FEBS Lett 1997; 412: 465-474.
2. Blondel O, Gastineau M, Dahmoune Y, Langlois M, Fischmeister R: Cloning, expression, and pharmacology of four human 5- hydroxytryptamine 4 receptor isoforms produced by alternative splicing in the carboxyl terminus. J Neurochem 1998; 70: 2252-2261.
3. Van den Wyngaert I, Gommeren W, Verhasselt P, Jurzak M, Leysen J, Luyten W, Bender E: Cloning and expression of a human serotonin 5-HT 4 receptor cDNA. J Neurochem 1997; 69: 1810-1819.
4. Bender E, Pindon A, van Oers I, Zhang Y-B, Gommeren W, Verhasselt P, Jurzak M, Leysen J, Luyten W: Structure of the human serotonin 5-HT 4 receptor gene and cloning of a novel 5-HT 4 spice variant. J Neurochem 2000; 74: 478-489.
5. Claeysen S, Sebben M, Becamel C, Bockaert J, Dumuis A: Novel brain-specific 5-HT 4 receptor splice variants show marked constitutive activity: role of the C-terminal intracellular domain. Mol Pharmacol 1999; 55: 910-920.
6. Mialet J, Berque-Bestel I, Eftekhari P, Gastineau M, Giner M, Dahmoune Y, Donz eau- Gouge P, Hoebeke J, Langlois M, Sicsic S, Fischmeister R, Lezoualc'h F: Isolation of the serotoninergic 5-HT 4(e) receptor from human heart and comparative analysis of its pharmacological profile in C6-glial and CHO cell lines. Br J Pharmacol 2000; 129: 771-781. (Pubitemid 30153861)
7. Langlois M, Fischmeister R: 5-HT 4 receptor ligands: applications and new prospects. J Med Chem 2003; 46: 319-344. (Pubitemid 36139783)
8. Brattelid T, Kvingedal AM, Krobert KA, Andressen KW, Bach T, Hystad ME, Kaumann AJ, Levy FO: Cloning, pharmacological characterisation and tissue distribution of a novel 5-HT 4 receptor splice variant, 5-HT 4(i) . Naunyn Schmiedeberg's Arch Pharmacol 2004; 369: 616-628. (Pubitemid 38823994)
9. Vilaró MT, Doménech T, Palacios JM, Mengod G: Cloning and characterization of a novel human 5-HT 4 receptor variant that lacks the alternatively spliced carboxy terminal exon: RT-PCR distribution in human brain and periphery of multiple 5-HT 4 receptor variants. Neuropharmacol 2002; 42: 60-73. (Pubitemid 34062822)
10. Coupar IM, Desmond PV, Irving HR: Human 5-HT 4 and 5-HT 7 receptor splice variants: are they important? Curr Neuropharmacol 2007; 5: 224-231.
11. Mialet J, Berque-Bestel I, Sicsic S, Langlois M, Fischmeister R, Lezoualc'h F: Pharmacological characterization of the human 5-HT 4(d) receptor splice variant stably expressed in Chinese hamster ovary cells. Br J Pharmacol 2000; 131: 827-835.
12. Pindon A, Van Hecke G, Van Gompel P, Lesage AS, Leysen JE, Jurzak M: Differences in signal transduction of two 5-HT 4 receptor splice variants: compound specificity and dual coupling with G -s- and G -i/o-proteins. Mol Pharmacol 2002; 61: 85-96. (Pubitemid 34049515)
13. De Maeyer JH, Lefebvre RA, Schuurkes JAJ: 5-HT 4 receptor agonists: similar but not the same. Neurogastroenterol Motil 2008; 20: 99-112.
14. Bradford MM: A rapid and sensitive method for quantitation of microgram quantities of protein utilizing the principle of protein-dye binding. Anal Biochem 1976; 72: 248-254.
15. Beattie DT, Smith JAM, Marquess D, Vickery RG, Armstrong SR, Pulido-Rios T, Mc- Cullough JL, Sandlund C, Richardson C, Mai N, Humphrey PPA: The 5-HT 4 receptor agonist, tegaserod, is a potent 5-HT 2B receptor antagonist in vitro and in vivo. Br J Pharmacol 2004; 143: 549-560. (Pubitemid 39524272)
16. Tack J, Middleton SJ, Horne MC, Piessevaux H, Bloor JS, Meyers NL, Palmer RM: Pilot study of the efficacy of renzapride on gastrointestinal motility and symptoms in patients with constipation-predominant irritable bowel syndrome. Aliment Pharmacol Ther 2006; 23: 1655-1665. (Pubitemid 43727476)
17. Krobert KA, Brattelid T, Levy FO, Kaumann AJ: Prucalopride is a partial agonist through human and porcine atrial 5-HT 4 receptors: comparison with recombinant human 5-HT 4 splice variants. Naunyn Schmiedeberg's Arch Pharmacol 2005; 371: 473-479. (Pubitemid 41218967)
18. FDA, US Food and Drug Administration. 2007, last update 30 April 2009. http://www. fda.gov/Drugs/DrugSafety/PublicHealthAdvisories/ucm051284.html (retrieved 5 August 2009).
19. Müller-Lissner SA, Fumagalli I, Bardhan KD, Pace F, Pecher E, Nault B, Rüegg P: Tegaserod, a 5-HT 4 receptor partial agonist, relieves symptoms in irritable bowel syndrome patients with abdominal pain, bloating and constipation. Aliment Pharmacol Ther 2001; 15: 1655-1666.
20. Mikami T, Sugimoto H, Naganeo R, Ohmo T, Saito T, Eda H: Contribution of active and inactive states of the human 5-HT 4d receptor to the functional activites of the 5-HT 4 -receptor agonists. J Pharmacol Sci 2008; 107: 251-259.
21. Vickery RG, Mai N, Kaufman E, Beattie DT, Pulido-Rios T, O'Keefe M, Humphrey PPA, Smith JAM: A comparison of the pharmacological properties of guinea-pig and human recombinant 5-HT 4 receptors. Br J Pharmacol 2007; 150: 782-791.
22. Eglen RM, Bonhaus DW, Johnson LG, Leung E, Clark RD: Pharmacological characterization of two novel and potent 5-HT 4 receptor agonists, RS 67333 and RS 67506, in vitro and in vivo. Br J Pharmacol 1995; 115: 1387-1392.
23. Sonda S, Katayama K, Kawahara T, Sato N, Asano K: Synthesis and pharmacological properties of benzamide derivatives as selective serotonin 4 receptor agonists. Bioorg Med Chem 2004; 12: 2737-2747.
24. McLean PG, Coupar IM: Further investigation into the signal transduction mechanism of the 5-HT 4 -like receptor in the smooth muscle of human colon. Br J Pharmacol 1996; 118: 1058-1064.
25. McLean PG, Coupar IM, Molenaar P: A comparative study of functional 5-HT 4 receptors in human colon, rat ileum and rat oesophagus. Br J Pharmacol 1995; 115: 47-56.
26. Irving HR, Tan YY, Tochon-Danguy N, Liu H, Chetty N, Desmond PV, Pouton CW, Coupar IM: Comparison of 5-HT 4 and 5-HT 7 receptor expression and function in the circular muscle of the human colon. Life Sci 2007; 80: 1198-1205.
27. Chetty N, Coupar IM, Tan YY, Desmond PV, Irving HR: Distribution of serotonin receptors and interacting proteins in the human sigmoid colon. Neurogastroenterol Motil 2009; 21:551-558.e15.
28. Bach T, Syversveen T, Kvingedal AM, Krobert KA, Brattelid T, Kaumann AJ, Levy FO: 5-HT 4(a) and 5-HT 4(b) receptors have nearly identical pharmacology and are both expressed in human atrium and ventricle. Naunyn Schmiedeberg's Arch Pharmacol 2001; 363: 146-160.