Synergistic effect between 5-HT4 receptor agonist and phosphodiesterase 4-inhibitor in releasing acetylcholine in pig gastric circular muscle in vitro

European Journal of Pharmacology

Volumn 781, Issue , 2016, Pages 76-82

  Lefebvre, Romain A ^a   Van Colen, Inge ^a   Pauwelyn, Vicky ^a   De Maeyer, Joris H ^b  

^a GHENT UNIVERSITY   (Belgium)

^b Movetis NV   (Belgium)

Author keywords

5 HT4 receptor; Acetylcholine release; Phosphodiesterase 4; Prucalopride; Stomach; Velusetrag

Indexed keywords

ACETYLCHOLINE; CHOLINE; PHOSPHODIESTERASE IV; PHOSPHODIESTERASE IV INHIBITOR; PRUCALOPRIDE; ROFLUMILAST; ROLIPRAM; SEROTONIN 4 AGONIST; SEROTONIN 4 RECEPTOR; TRITIUM; VELUSETRAG; AMINOPYRIDINE DERIVATIVE; AZABICYCLO DERIVATIVE; BENZAMIDE DERIVATIVE; BENZOFURAN DERIVATIVE; CYCLOPROPANE DERIVATIVE; TD-5108;

ACETYLCHOLINE RELEASE; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CHOLINERGIC NERVE CELL; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG EFFECT; DRUG POTENTIATION; GASTROPROKINETIC EFFECT; IN VITRO STUDY; MALE; NONHUMAN; PIG; PRIORITY JOURNAL; STOMACH MUSCLE; ANIMAL; DOSE RESPONSE; DRUG EFFECTS; GASTROINTESTINAL MOTILITY; METABOLISM; MUSCLE CONTRACTION; PHYSIOLOGY; SECRETION (PROCESS); SMOOTH MUSCLE; STOMACH;

ACETYLCHOLINE; AMINOPYRIDINES; ANIMALS; AZABICYCLO COMPOUNDS; BENZAMIDES; BENZOFURANS; CYCLIC NUCLEOTIDE PHOSPHODIESTERASES, TYPE 4; CYCLOPROPANES; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG SYNERGISM; GASTROINTESTINAL MOTILITY; MALE; MUSCLE CONTRACTION; MUSCLE, SMOOTH; PHOSPHODIESTERASE 4 INHIBITORS; RECEPTORS, SEROTONIN, 5-HT4; SEROTONIN 5-HT4 RECEPTOR AGONISTS; STOMACH; SUS SCROFA;

EID: 84963588818     PISSN: 00142999     EISSN: 18790712     Source Type: Journal    
DOI: 10.1016/j.ejphar.2016.04.003     Document Type: Article

References (42)

1. 4-elicited positive inotropic response is mediated by cAMP and regulated by PDE3 in failing rat and human cardiac ventricles Br. J. Pharmacol. 155 2008 1005 1044
2. A. Ahn, C. Barnes, D. Shaywitz, M. Grimaldi, and D.M. Canafax Velusetrag improves gastric emptying time in subjects with diabetic or idiopathic gastroparesis Gastroenterol 148 4 2015 Suppl. 1, S-507
3. J.T. Barbey, R. Lazzara, and D.P. Zipes Spontaneous adverse event reports of serious ventricular arrhythmias, QT prolongation, syncope, and sudden death in patients treated with cisapride J. Cardiovasc. Pharmacol. Ther. 7 2002 65 76
4. 4 receptor agonist with gastrointestinal prokinetic properties Front. Pharmacol. 2 2011 1 13 Article 25
5. J. Broad, V.W.S. Kung, G. Boundouki, Q. Aziz, J.H. De Maeyer, C.H. Knowles, and G.J. Sanger Cholinergic interactions between donepezil and prucalopride in human colon: potential to treat severe intestinal dysmotility Br. J. Pharmacol. 170 2013 1253 1261
6. D.S. Bundschuh, M. Eltze, J. Barsig, L. Wollin, A. Hatzelmann, and R. Beume In vivo efficacy in airway disease models of roflumilast, a novel orally active PDE4 inhibitor J. Pharmacol. Exp. Ther. 297 2001 280 290
7. 4 receptor agonist Neurogastroenterol. Motil. 21 2009 1197 1203
8. D.A. Craig, and D.E. Clarke Pharmacological characterization of a neuronal receptor for 5-hydroxytryptamine in guinea pig ileum with properties similar to the 5-hydroxytryptamine4 receptor J. Pharmacol. Exp. Ther. 252 1990 1378 1386
9. 4 receptor agonists: similar but not the same Neurogastroenterol. Motil. 20 2008 99 112
10. 4 receptor-induced responses: fading of the response and influence of development Br. J. Pharmacol. 147 2006 140 147
11. A. Emmanuel, M. Cools, L. Vandeplassche, and R. Kerstens Prucalopride improves bowel function and colonic transit time in patients with chronic constipation: an integrated analysis Am. J. Gastroenterol. 109 2014 887 894
12. 4 receptors Br. J. Pharmacol. 156 2009 237 249
13. J.J. Galligan, and S. Vanner Basic and clinical pharmacology of new motility promoting agents Neurogastroenterol. Motil. 17 2005 643 653
14. 4 agonist with high intrinsic activity, in chronic idiopathic constipation - a 4-week, randomized double-blind, placebo-controlled, dose-response study Aliment. Pharmacol. Ther. 32 2010 1102 1112
15. M. Katsura, T. Hashimoto, and K. Kuriyama Effect of 1,3-di-n-butyl-7-(2-oxopropyl)-xanthine (denbufylline) on metabolism and function of cerebral cholinergic neurons Jpn. J. Pharmacol. 55 1991 233 240
16. G.M. Keating Prucalopride: a review of its use in the management of chronic constipation Drugs 73 2013 1935 1950
17. 4 splice variants Naunyn-Schmied. Arch. Pharmacol. 371 2005 473 479
18. P.G. Leclere, and R.A. Lefebvre Influence of nitric oxide donors and of the alpha(2)-agonist UK-14,304 on acetylcholine release in the pig gastric fundus Neuropharmacology 40 2001 270 278
19. 4 receptors located on cholinergic nerves in human colon circular muscle Neurogastroenterol. Motil. 17 2005 366 375
20. 4 receptor agonist that has achieved proof-of-concept in patients with chronic idiopathic constipation Bioorg. Med. Chem. Lett. 22 2012 6048 6052
21. 4 receptor agonist: clinical compound TD-2749 Bioorg. Med. Chem. Lett. 22 2012 4849 4853
22. M.L. Manini, M. Camilleri, M. Goldberg, S. Sweetser, S. Mckinzie, D. Burton, S. Wong, M.M. Kitt, Y.-P. Li, and A.R. Zinsmeister Effects of velusetrag (TD-5108) on gastrointestinal transit and bowel function in health and pharmacokinetics in health and constipation Neurogastroenterol. Motil. 22 2010 42-e8
23. P.G. McLean, and I.M. Coupar Further investigation into the signal transduction mechanism of the 5-HT4-like receptor in the circular smooth muscle of human colon Br. J. Pharmacol. 118 1996 1058 1064
24. J.M. Michalski, G. Golden, J. Ikari, and S.I. Rennard PDE4: a novel target in the treatment of chronic obstructive pulmonary disease Clin. Pharmacol. Ther. 91 2012 134 142
25. 4 receptors by SB203186 Naunyn-Schmied. Arch. Pharmacol. 353 1995 28 35
26. 4 receptor facilitated cholinergic contractility in pig descending colon Eur. J. Pharmacol. 705 2013 156 163
27. 4 receptors in circular smooth muscle of pig descending colon Eur. J. Pharmacol. 667 2011 365 374
28. E. Priem, I. Van Colen, J.H. De Maeyer, and R.A. Lefebvre The facilitating effect of prucalopride on cholinergic neurotransmission in pig gastric circular muscle is regulated by phosphodiesterase 4 Neuropharmacol 62 2012 2126 2135
29. 4 receptors on cholinergic nerves involved in contractility of canine and human large intestine longitudinal muscle Br. J. Pharmacol. 131 2000 927 932
30. 4 receptors mediating enhancement of contractlity in canine stomach; an in vitro and in vivo study Br. J. Pharmacol. 132 2001 1941 1947
31. K.F. Rabe Update on roflumilast, a phosphodiesterase 4 inhibitor for the treatment of chronic obstructive pulmonary disease Br. J. Pharmacol. 163 2011 53 67
32. 4 receptor activation facilitates recovery from synaptic rundown and increases transmitter release from single varicosities of myenteric neurons Am. J. Physiol. 294 2008 G1376 G1383
33. 4 receptor agonist with high intrinsic activity Naunyn-Schmiede. Arch. Pharmacol. 378 2008 125 137
34. 4 agonists developed for gastrointestinal disorders Aliment. Pharmacol. Ther. 35 2012 745 767
35. C.J. Tralau-Stewart, R.A. Williamson, A.T. Nials, M. Gascoigne, J. Dawson, G.J. Hart, A.D.R. Angell, Y.E. Solanke, F.S. Lucas, J. Wiseman, P. Ward, L.E. Ranshaw, and R.G. Knowles GSK256066, an exceptionally high-affinity and selective inhibitor of phosphodiesterase 4 suitable for administration: in vitro, kinetic and in vivo characterization J. Pharmacol. Exp. Ther. 337 2011 145 154
36. Y. Wan, S.X. Sun, S. Corman, X. Huang, X. Gao, and A.F. Shorr A longitudinal, retrospective cohort study on the impact of roflumilast on exacerbations and economic burden among chronic obstructive disease patients in the real world Int. J. Chron. Obstr. Pulm. Dis. 10 2015 2127 2136
37. 4 receptor-mediated contractions Br. J. Pharmacol. 110 1993 1593 1599
38. 4 receptor activation via phosphodiesterases and its cross-talk with C-type natriuretic peptide in porcine left atrium Naunyn-Schmiede. Arch. Pharmacol. 385 2012 565 577
39. J. Wiley, and C. Owyang Somatostatin inhibits cAMP-mediated cholinergic transmission in the myenteric plexus Am. J. Physiol. 253 1987 G607 G612
40. L.R. Wiseman, and D. Faulds Cisapride. An updated review of its pharmacology and therapeutic efficacy as a prokinetic agent in gastrointestinal motility disorders Drugs 47 1994 116 152
41. A. Wohlsen, A. Hirrle, H. Tenor, D. Marx, and R. Beume Effect of cyclic AMP-elevating agents on airway ciliary beat frequency in central and lateral airways in rat precision-cut lung slices Eur. J. Pharmacol. 635 2010 177 183
42. W.M. Yau, J. Dorsett, and M.L. Youther Stimulation of acetylcholine release from myenteric neurons of guinea pig small intestine by forskolin and cyclic AMP J. Pharmacol. Exp. Ther. 243 1987 507 510