The β3-Adrenoceptor Agonist GW427353 (Solabegron) Decreases Excitability of Human Enteric Neurons via Release of Somatostatin

Gastroenterology

Volumn 138, Issue 1, 2010, Pages 266-274

  Schemann, Michael ^a   Hafsi, Nadia ^a   Michel, Klaus ^a   Kober, Olivia I ^b,c   Wollmann, Jutta ^a   Li, Qin ^a   Zeller, Florian ^d   Langer, Rupert ^a   Lee, Kevin ^b   Cellek, Selim ^b  

^a TECHNICAL UNIVERSITY OF MUNICH   (Germany)

^b GLAXOSMITHKLINE   (United Kingdom)

^c UNIVERSITY OF BRISTOL   (United Kingdom)

^d Clinical Centre Freising   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

1 (2 ETHYLPHENOXY) 3 (1,2,3,4 TETRAHYDRO 1 NAPHTHYLAMINO) 2 PROPANOL OXALATE; ADIPONECTIN; BETA 3 ADRENERGIC RECEPTOR; GENE PRODUCT; OCTREOTIDE; PROTEIN GENE PRODUCT 9.5; SOLABEGRON; SOMATOSTATIN; SOMATOSTATIN RECEPTOR 2; TYROSINE 3 MONOOXYGENASE; UNCLASSIFIED DRUG; 3' ((2 ((2 (3 CHLOROPHENYL) 2 HYDROXYETHYL)AMINO)ETHYL)AMINO) (1,1' BIPHENYL) 3 CARBOXYLIC ACID; 3'-((2-((2-(3-CHLOROPHENYL)-2-HYDROXYETHYL)AMINO)ETHYL)AMINO)-(1,1'-BIPHENYL)-3-CARBOXYLIC ACID; ANILINE DERIVATIVE; BENZOIC ACID DERIVATIVE; GANGLION STIMULATING AGENT; NICOTINE; PROPANOLAMINE DERIVATIVE;

ADIPOCYTE; AGED; ARTICLE; CONTROLLED STUDY; DRUG MECHANISM; ENZYME LINKED IMMUNOSORBENT ASSAY; FEMALE; HUMAN; HUMAN TISSUE; IMMUNOHISTOCHEMISTRY; IRRITABLE COLON; MAJOR CLINICAL STUDY; MALE; NERVE CELL; NERVE EXCITABILITY; POSTSYNAPTIC POTENTIAL; PRIORITY JOURNAL; SYNAPTIC MEMBRANE; TISSUE PERFUSION; ACTION POTENTIAL; AUTONOMIC NERVOUS SYSTEM; CYTOLOGY; DOSE RESPONSE; DRUG ANTAGONISM; DRUG EFFECT; DRUG INTERACTION; DRUG POTENTIATION; ELECTROSTIMULATION; IN VITRO STUDY; INNERVATION; INTESTINE; METABOLISM; MIDDLE AGED; MYENTERIC PLEXUS; PHYSIOLOGY;

ACTION POTENTIALS; ADIPOCYTES; AGED; ANILINE COMPOUNDS; BENZOIC ACIDS; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG INTERACTIONS; ELECTRIC STIMULATION; FEMALE; GANGLIONIC STIMULANTS; HUMANS; INTESTINES; MALE; MIDDLE AGED; MYENTERIC PLEXUS; NEURONS; NICOTINE; PROPANOLAMINES; RECEPTORS, ADRENERGIC, BETA-3; SOMATOSTATIN; SUBMUCOUS PLEXUS;

EID: 72249102564     PISSN: 00165085     EISSN: None     Source Type: Journal    
DOI: 10.1053/j.gastro.2009.09.046     Document Type: Article

References (27)

1. Jänig W. Integration of gut function by sympathetic reflexes. Baillieres Clin Gastroenterol 2 (1988) 45-62
2. Hirst G.D., and McKirdy H.C. Presynaptic inhibition at mammalian peripheral synapse?. Nature 250 (1974) 430-431
3. Surprenant A., and North R.A. Mechanism of synaptic inhibition by noradrenaline acting at alpha 2-adrenoceptors. Proc R Soc Lond B Biol Sci 234 (1988) 85-114
4. Dobreva G., Neunlist M., Frieling T., et al. Post- and presynaptic effects of norepinephrine in guinea-pig colonic submucous plexus. Neurogastroenterol Motil 10 (1998) 123-130
5. de Ponti F., Gibelli G., Croci T., et al. Functional evidence of atypical β3-adrenoceptors in the human colon using the β3-selective adrenoceptor antagonist, SR 59230A. Br J Pharmacol 117 (1996) 1374-1376
6. Bardou M., Dousset B., Deneux-Tharaux C., et al. In vitro inhibition of human colonic motility with SR 59119A and SR 59104A: evidence of a β3-adrenoceptor-mediated effect. Eur J Pharmacol 353 (1998) 281-287
7. Cellek S., Thangiah R., Bassil A.K., et al. Demonstration of functional neuronal beta3-adrenoceptors within the enteric nervous system. Gastroenterology 133 (2007) 175-183
8. Berkowitz D.E., Nardone N.A., Smiley R.M., et al. Distribution of β-3-adrenoceptor mRNA in human tissues. Eur J Pharmacol 289 (1995) 223-228
9. Seboek D., Linscheid P., Zulewski H., et al. Somatostatin is expressed and secreted by human adipose tissue upon infection and inflammation. J Clin Endocrinol Metab 89 (2004) 4833-4839
10. Kelleher D.L., Hicks K.J., Cox D.S., et al. Randomized, double-blind, placebo (PLA)-controlled, crossover study to evaluate efficacy and safety of the beta 3-adrenergic receptor agonist solabegron (SOL) in patients with irritable bowel syndrome (IBS). Neurogastroenterol Motil 20 Suppl 2 (2008) 131-132 (abstract)
11. Grudell A.B., Camilleri M., Jensen K.L., et al. Dose-response effect of a beta3-adrenergic receptor agonist, solabegron, on gastrointestinal transit, bowel function, and somatostatin levels in health. Am J Physiol 294 (2008) G1114-G1119
12. Schicho R., Krueger D., Zeller F., et al. Hydrogen sulfide is a novel prosecretory neuromodulator in the guinea-pig and human colon. Gastroenterology 131 (2006) 1542-1552
13. Neunlist M., Peters S., and Schemann M. Multisite optical recording of excitability in the enteric nervous system. Neurogastroenterol Motil 11 (1999) 393-402
14. Michel K., Zeller F., Langer R., et al. Serotonin excites neurons in the human submucous plexus via 5-HT3 receptors. Gastroenterology 128 (2005) 1317-1326
15. Schemann M., Michel K., Peters S., et al. Cutting-edge technology; III, imaging and the gastrointestinal tract: mapping the human enteric nervous system. Am J Physiol 282 (2002) G919-G925
16. Breunig E., Michel K., Zeller F., et al. Histamine excites neurones in the human submucous plexus through activation of H1, H2, H3 and H4 receptors. J Physiol 583 (2007) 731-742
17. Thompson R.J., Doran J.F., Jackson P., Dhillon A.P., and Rode J. PGP 9.5-a new marker for vertebrate neurons and neuroendocrine cells. Brain Res 278 (1983) 224-228
18. Geffen L.B., and Hughes C.C. Degeneration of sympathetic nerves in vitro and development of smooth muscle supersensitivity to noradrenaline. J Physiol 221 (1972) 71-84
19. Mihara S., North R.A., and Surprenant A. Somatostatin increases an inwardly rectifying potassium conductance in guinea-pig submucous plexus neurones. J Physiol 390 (1987) 335-355
20. Anthony A., Sim R., Guillaume J.L., et al. Beta(beta)3-adrenergic receptors in human pancreatic islet and duodenal somatostatin neuroendocrine cells. Aliment Pharmacol Ther 14 (2000) 579-585
21. Martin C.A., Naline E., Manara L., and Advenier C. Effects of two beta 3-adrenoceptor agonists, SR 58611A and BRL 37344, and of salbutamol on cholinergic and NANC neural contraction in guinea-pig main bronchi in vitro. Br J Pharmacol 110 (1993) 1311-1316
22. Liu M., Seino S., and Kirchgessner A.L. Identification and characterization of glucoresponsive neurons in the enteric nervous system. Neuroscience 19 (1999) 10305-10317
23. Rehn M., Hübschle T., and Diener M. TNF-alpha hyperpolarizes membrane potential and potentiates the response to nicotinic receptor stimulation in cultured rat myenteric neurones. Acta Physiol Scand 181 (2004) 13-22
24. Umekawa T., Yoshida T., Sakane N., et al. Effect of CL316,243, a highly specific beta(3)-adrenoceptor agonist, on lipolysis of epididymal, mesenteric and subcutaneous adipocytes in rats. Endocr J 44 (1997) 181-185
25. Hanani M., Nissan A., and Freund H.R. Innervation of submucosal adipocytes in the human colon. Neurosci Lett 428 (2007) 7-10
26. Booth C.E., Kirkup A.J., Hicks G.A., et al. Somatostatin sst(2) receptor-mediated inhibition of mesenteric afferent nerves of the jejunum in the anesthetized rat. Gastroenterology 121 (2001) 358-369
27. Vasina V., Abu-Gharbieh E., Barbara G., et al. The beta(3)-adrenoceptor agonist SR58611A ameliorates experimental colitis in rats. Neurogastroenterol Motil 20 (2008) 1030-1041