Effects of a κ-opioid agonist, asimadoline, on satiation and GI motor and sensory functions in humans

American Journal of Physiology - Gastrointestinal and Liver Physiology

Volumn 284, Issue 4 47-4, 2003, Pages

  Delgado Aros, Silvia ^a   Chial, Heather J ^a   Camilleri, Michael ^a   Szarka, Lawrence A ^a   Weber, Frank T ^b   Jacob, Jutta ^b   Ferber, Irene ^a   McKinzie, Sanna ^a   Burton, Duane D ^a   Zinsmeister, Alan R ^a  

^a MAYO CLINIC   (United States)

^b MERCK KGAA   (Germany)

Author keywords

Barostat; Colon; Sensation; Stomach; Visceral

Indexed keywords

ASIMADOLINE; KAPPA OPIATE RECEPTOR AGONIST;

ABDOMINAL DISEASE; ADULT; ANOREXIA; ARTICLE; BAROSTAT; CENTRAL NERVOUS SYSTEM DISEASE; CLINICAL TRIAL; COLON DILATATION; CONSTIPATION; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DOSE RESPONSE; DOUBLE BLIND PROCEDURE; DRUG EFFECT; DRUG EFFICACY; FEMALE; GASTROINTESTINAL MOTILITY; GASTROINTESTINAL SYMPTOM; HEADACHE; HEARTBURN; HEPATOBILIARY DISEASE; HUMAN; HUMAN EXPERIMENT; INTESTINE TRANSIT TIME; MALE; MENTAL DISEASE; MUSCULOSKELETAL DISEASE; NAUSEA; NORMAL HUMAN; NUTRIENT; PAIN ASSESSMENT; PERIPHERAL NEUROPATHY; PHASE 1 CLINICAL TRIAL; POSTPRANDIAL STATE; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; RESPIRATORY TRACT DISEASE; SATIETY; SCINTIGRAPHY; SENSORY SYSTEM; VERTIGO; VISCERAL PAIN; VISUAL DISORDER;

ACETAMIDES; ADOLESCENT; ADULT; COLON; COMPLIANCE; DOUBLE-BLIND METHOD; FEMALE; FLATULENCE; GASTROINTESTINAL MOTILITY; HUMANS; MALE; MIDDLE AGED; PAIN; POSTPRANDIAL PERIOD; PYRROLIDINES; RECEPTORS, OPIOID, KAPPA; SATIATION; SENSATION; STOMACH; VISCERAL AFFERENTS;

EID: 0037378287     PISSN: 01931857     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (61)

1. Allescher HD, Storr M, Piller C, Brantl V, and Schusdziarra V. Effect of opioid active therapeutics on the ascending reflex pathway in the rat ileum. Neuropeptides 34: 181-186, 2000.
2. Anonymous. Asimadoline (EMD 61753). Darmstadt, Germany: Merck, 2001.
3. Barber A, Bartoszyk GD, Bender HM, Gottschlich R, Greiner HE, Harting J, Mauler F, Minck KO, Murray RD, and Simon M. A pharmacological profile of the novel, peripherally-selective κ-opioid receptor agonist, EMD 61753. Br J Pharmacol 113: 1317-1327, 1994.
4. Bender HM and Dasenbrock J. Brain concentrations of asimadoline in mice: the influence of coadministration of various P-glycoprotein substrates. Int J Clin Pharmacol Ther 36: 76-79, 1998.
5. 4 receptor antagonist SB-207266 on gastrointestinal motor and sensory function in humans. Gut 47: 667-674, 2000.
6. Bharucha AE, Camilleri M, Zinsmeister AR, and Hanson RB. Adrenergic modulation of human colonic motor and sensory function. Am J Physiol Gastrointest Liver Physiol 273: G997-G1006, 1997.
7. Burton DD, Camilleri M, Mullan BP, Forstrom LA, and Hung JC. Colonic transit scintigraphy labeled activated charcoal compared with ion exchange pellets. J Nucl Med 38: 1807-1810, 1997.
8. Burton MB and Gebhart GF. Effects of κ-opioid receptor agonists on responses to colorectal distension in rats with and without acute colonic inflammation. J Pharmacol Exp Ther 285: 707-715, 1998.
9. Camilleri M, Colemont LJ, Phillips SF, Brown ML, Thomforde GM, Chapman N, and Zinsmeister AR. Human gastric emptying and colonic filling of solids characterized by a new method. Am J Physiol Gastrointest Liver Physiol 257: G284-G290, 1989.
10. Cervero F. Sensory innervation of the viscera: peripheral basis of visceral pain. Physiol Rev 74: 95-138, 1994.
11. Chalazonitis A and Crain SM. Maturation of opioid sensitivity of fetal mouse dorsal root ganglion neuron perikarya in organotypic cultures: regulation by spinal cord. Neuroscience 17: 1181-1198, 1986.
12. Chen GG, Chalazonitis A, Shen KF, and Crain SM. Inhibitor of cyclic AMP-dependent protein kinase blocks opioid-induced prolongation of the action potential of mouse sensory ganglion neurons in dissociated cell cultures. Brain Res 462: 372-377, 1988.
13. Cherny N, Ripamonti C, Pereira J, Davis C, Fallon M, McQuay H, Mercadante S, Pasternak G, and Ventafridda V. Strategies to manage the adverse effects of oral morphine: an evidence-based report. J Clin Oncol 19: 2542-2554, 2001.
14. Coffin B, Bouhassira D, Chollet R, Fraitag B, De Meynard C, Geneve J, Lemann M, Willer JC, and Jian R. Effect of the κ-agonist fedotozine on perception of gastric distension in healthy humans. Aliment Pharmacol Ther 10: 919-925, 1996.
15. Crain SM and Shen KF. Opioids can evoke direct receptormediated excitatory effects on sensory neurons. Trends Pharmacol Sci 11: 77-81, 1990.
16. Danzebrink RM, Green SA, and Gebhart GF. Spinal μ and δ, but not κ, opioid-receptor agonists attenuate responses to noxious colorectal distension in the rat. Pain 63: 39-47, 1995.
17. Dapoigny M, Abitbol JL, and Fraitag B. Efficacy of peripheral κ-agonist fedotozine vs. placebo in treatment of irritable bowel syndrome. A multicenter dose-response study. Dig Dis Sci 40: 2244-2249, 1995.
18. Delgado-Aros S, Chial HJ, Burton DD, McKinzie S, Ferber I, and Camilleri C. Reliability of the nutrient drink test to assess maximum volume intake and postprandial symptoms (Abstract). Gastroenterology 122: A550, 2002.
19. Delgado-Aros S, Kim DY, Burton DD, Thomforde GM, Stephens D, Brinkmann BH, Vella A, and Camilleri M. Effect of GLP-1 on gastric volume, emptying, maximum volume ingested, and postprandial symptoms in humans. Am J Physiol Gastrointest Liver Physiol 282: G424-G431, 2002.
20. Delvaux M, Louvel D, Lagier E, Scherrer B, Abitbol JL, and Frexinos J. The κ-agonist fedotozine relieves hypersensitivity to colonic distention in patients with irritable bowel syndrome. Gastroenterology 116: 38-45, 1999.
21. De Pedro N, Delgado MJ, and Alonso-Bedate M. Central administration of β-endorphin increases food intake in goldfish: pretreatment with the opioid antagonist naloxone. Regul Pept 55: 189-195, 1995.
22. Diop L, Riviere PJ, Pascaud X, and Junien JL. Peripheral κ-opioid receptors mediate the antinociceptive effect of fedotozine (correction of fetodozine) on the duodenal pain reflex in rat. Eur J Pharmacol 271: 65-71, 1994.
23. Drossman DA, Li Z, Andruzzi E, Temple RD, Talley NJ, Thompson WG, Whitehead WE, Janssens J, Funch-Jensen P, Corazziari E, Richter JE, and Kich GG. US householder survey of functional gastrointestinal disorders: prevalence, sociodemography, and health impact. Dig Dis Sci 38: 1569-1580, 1993.
24. Duggan AW, Griersmith BT, and North RA. Morphine and supraspinal inhibition of spinal neurones: evidence that morphine decreases tonic descending inhibition in the anaesthetized cat. Br J Pharmacol 69: 461-466, 1980.
25. Ford MJ, Camilleri M, Zinsmeister AR, and Hanson RB. Psychosensory modulation of colonic sensation in the human transverse and sigmoid colon. Gastroenterology 109: 1772-1780, 1995.
26. Gebhart GF and Sengupta JN. On visceral nociceptors. In: Peripheral Neurons in Nociception: Physio-Pharmacological Aspects, edited by Besson JM, Guilbaud G, and Ollat H. Paris: Libbey Eurotext, 1994, p. 23-37.
27. Gottschlich R, Krug M, Barber A, and Devant RM. κ-Opioid activity of the four stereoisomers of the peripherally selective κ-agonists, EMD 60400 and EMD 61753. Chirality 6: 685-689, 1994.
28. Hammer HF, Phillips SF, Camilleri M, and Hanson RB. Rectal tone, distensibility, and perception: reproducibility and response to different distensions. Am J Physiol Gastrointest Liver Physiol 274: G584-G590, 1998.
29. Harada Y, Nishioka K, Kitahata LM, Nakatani K, and Collins JG. Contrasting actions of intrathecal U50488H, morphine, or [D-Pen2,D-Pen5] enkephalin or intravenous U50488H on the visceromotor response to colorectal distension in the rat. Anesthesiology 83: 336-343, 1995.
30. Kaufman PN, Krevsky B, Malmud LS, Maurer AH, Somers MB, Siegel JA, and Fisher RS. Role of opiate receptors in the regulation of colonic transit. Gastroenterology 94: 1351-1356, 1988.
31. Kest B, Marek P, and Liebeskind JC. The specific N-methyl-D-aspartate (NMDA) receptor antagonist MK-801 blocks U-50488, but not morphine, antinociception. Brain Res 589: 139-142, 1992.
32. Kirkham TC and Blundell JE. Dual action of naloxone on feeding revealed by behavioural analysis: separate effects on initiation and termination of eating. Appetite 5: 45-52, 1984.
33. Laughlin TM, Vanderah TW, Lashbrook J, Nichols ML, Ossipov M, Porreca F, and Wilcox GL. Spinally administered dynorphin A produces long-lasting allodynia: involvement of NMDA but not opioid receptors. Pain 72: 253-260, 1997.
34. Law NM, Bharucha AE, Undale AS, and Zinsmeister AR. Cholinergic stimulation enhances colonic motor activity, transit, and sensation in humans. Am J Physiol Gastrointest Liver Physiol 281: G1228-G1237, 2001.
35. Lembo T, Munakata J, Mertz H, Niazi N, Kodner A, Nikas V, and Mayer EA. Evidence for the hypersensitivity of lumbar splanchnic afferents in irritable bowel syndrome. Gastroenterology 107: 1686-1696, 1994.
36. Machelska H, Pfluger M, Weber W, Piranvisseh-Volk M, Daubert JD, Dehaven R, and Stein C. Peripheral effects of the κ-opioid agonist EMD 61753 on pain and inflammation in rats and humans. J Pharmacol Exp Ther 290: 354-361, 1999.
37. Marmonier C, Chapelot D, and Louis-Sylvestre J. Effects of macronutrient content and energy density of snacks consumed in a satiety state on the onset of the next meal. Appetite 34: 161-168, 2000.
38. Mudge AW, Leeman SE, and Fischbach GD. Enkephalin inhibits release of substance P from sensory neurons in culture and decreases action potential duration. Proc Natl Acad Sci USA 76: 526-530, 1979.
39. 2 spinal cord of the rat. J Neurophysiol 60: 1419-1438, 1988.
40. Ness TJ, Metcalf AM, and Gebhart GF. A psychophysiological study in humans using phasic colonic distension as a noxious visceral stimulus. Pain 43: 377-386, 1990.
41. Ozaki N, Sengupta JN, and Gebhart GF. Differential effects of μ-, δ, and κ-opioid receptor agonists on mechanosensitive gastric vagal afferent fibers in the rat. J Neurophysiol 83: 2209-2216, 2000.
42. Parker LA, Maier S, Rennie M, and Crebolder J. Morphineand naltrexone-induced modification of palatability: analysis by the taste reactivity test. Behav Neurosci 106: 999-1010, 1992.
43. Prokop EK, Caride VJ, Winchenbach K, Troncale FJ, and McCallum RW. Scintigraphic determination of the effect of metoclopramide and morphine on small intestinal transit time. Am J Physiol Imaging 3: 201-204, 1988.
44. Read NW, Abitbol JL, Bardhan KD, Whorwell PJ, and Fraitag B. Efficacy and safety of the peripheral κ-agonist fedotozine vs. placebo in the treatment of functional dyspepsia. Gut 41: 664-668, 1997.
45. Satoh M and Minami M. Molecular pharmacology of the opioid receptors. Pharmacol Ther 68: 343-364, 1995.
46. Saucier DM and Kavaliers M. Antagonistic effects of the selective, competitive N-methyl-D-aspartate (NMDA) receptor antagonist, NPC 12626, on κ-opiate-induced analgesia in male deer mice. Brain Res 637: 292-296, 1994.
47. Sengupta JN and Gebhart GF. Characterization of mechanosensitive pelvic nerve afferent fibers innervating the colon of the rat. J Neurophysiol 71: 2046-2060, 1994.
48. Sengupta JN, Snider A, Su X, and Gebhart GF. Effects of κ-opioids in the inflamed rat colon. Pain 79: 175-185, 1999.
49. Shen KF and Crain SM. Dual opioid modulation of the action potential duration of mouse dorsal root ganglion neurons in culture. Brain Res 491: 227-242, 1989.
50. Simonin F, Gaveriaux-Ruff C, Befort K, Matthes H, Lannes B, Micheletti G, Mattei MG, Charron G, Bloch B, and Kieffer B. κ-Opioid receptor in humans: cDNA and genomic cloning, chromosomal assignment, functional expression, pharmacology, and expression pattern in the central nervous system. Proc Natl Acad Sci USA 92: 7006-7010, 1995.
51. Sproule BA, Busto UE, Somer G, Romach MK, and Sellers EM. Characteristics of dependent and nondependent regular users of codeine. J Clin Psychopharmacol 19: 367-372, 1999.
52. Steadman CJ, Phillips SF, Camilleri M, Haddad AC, and Hanson RB. Variation of muscle tone in the human colon. Gastroenterology 101: 373-381, 1991.
53. Stein C. The control of pain in peripheral tissue by opioids. N Engl J Med 332: 1685-1690, 1995.
54. Su X, Julia V, and Gebhart GF. Effects of intracolonic opioid receptor agonists on polymodal pelvic nerve afferent fibers in the rat. J Neurophysiol 83: 963-970, 2000.
55. Tack J, Piessevaux H, Coulie B, Caenepeel P, and Janssens J. Role of impaired gastric accommodation to a meal in functional dyspepsia. Gastroenterology 115: 1346-1352, 1998.
56. Tam T, Mui H, Jundler S, Tougas S, and Armstrong D. Two-lumen tubing is required for accurate barostat studies (Abstract). Gastroenterology 114: G3471, 1998.
57. Thompson WG, Longstreth GF, Drossman DA, Heaton KW, Irvine EJ, and Muller-Lissner SA. Functional bowel disorders and functional abdominal pain. Gut 45 Suppl 2: II43-II47, 1999.
58. 2-adrenergic agonist on gastrointestinal transit, colonic motility, and sensation in humans. Am J Physiol Gastrointest Liver Physiol 281: G1468-G1476, 2001.
59. Von der Ohe MR, Camilleri M, Kvols LK, and Thomforde GM. Motor dysfunction of the small bowel and colon in patients with the carcinoid syndrome and diarrhea. N Engl J Med 329: 1073-1078, 1993.
60. Werz MA and Macdonald RL. Dynorphin and neoendorphin peptides decrease dorsal root ganglion neuron calcium-dependent action potential duration. J Pharmacol Exp Ther 234: 49-56, 1985.
61. Yeomans MR and Gray RW. Effects of naltrexone on food intake and changes in subjective appetite during eating: evidence for opioid involvement in the appetizer effect. Physiol Behav 62: 15-21, 1997.