Pharmacological study of IQM-97,423, a potent and selective CCK1 receptor antagonist with protective effect in experimental acute pancreatitis

Pharmacology

Volumn 72, Issue 2, 2004, Pages 68-76

  Latorre, M ^a   Bartolome Nebreda J M ^b   Garcia LoPez M T ^b   GonzaLez Muniz R ^b   Herranz, R ^b   Del Rio J ^a   Cenarruzabeitiaa, E ^a  

^a UNIVERSITY OF NAVARRA   (Spain)

^b INSTITUTO DE QUÍMICA MÉDICA   (Spain)

Author keywords

Acute pancreatitis; Amylase release; CCK1 receptors; Cholecystokinin

Indexed keywords

2 BENZYL 5 (TERT BUTYLAMINOCARBONYLTRYPTOPHYL)AMINO 1,3 DIOXOPERHYDROPYRIDO[1,2 C]PYRIMIDINE; AMYLASE; CERULETIDE; CHOLECYSTOKININ 1 RECEPTOR ANTAGONIST; CHOLECYSTOKININ OCTAPEPTIDE; CHOLECYSTOKININ RECEPTOR BLOCKING AGENT; DEVAZEPIDE; IQM 97423; LORGLUMIDE; PANCREAS ENZYME; PD 135158; UNCLASSIFIED DRUG;

ACUTE PANCREATITIS; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BILE DUCT INJURY; BINDING AFFINITY; CONTROLLED STUDY; DRUG ACTIVITY; DRUG ANTAGONISM; DRUG BINDING; DRUG MECHANISM; DRUG POTENCY; ENZYME ACTIVITY; ENZYME INHIBITION; ENZYME RELEASE; GUINEA PIG; IN VITRO STUDY; INTESTINE MUSCLE; MALE; MOUSE; MYENTERIC PLEXUS; NONHUMAN; ORGAN WEIGHT; PANCREAS DUCT STENOSIS; PHARMACODYNAMICS; PRIORITY JOURNAL; RECEPTOR BINDING;

ACUTE DISEASE; ALPHA-AMYLASE; ANIMALS; BINDING, COMPETITIVE; CEREBRAL CORTEX; CHOLECYSTOKININ; DEVAZEPIDE; DISEASE MODELS, ANIMAL; GUINEA PIGS; ILEUM; MALE; MICE; MUSCLE CONTRACTION; MUSCLE, SMOOTH; MYENTERIC PLEXUS; NEUROMUSCULAR JUNCTION; PANCREATITIS; PEPTIDE FRAGMENTS; PROGLUMIDE; PYRIMIDINONES; RATS; RATS, WISTAR; RECEPTOR, CHOLECYSTOKININ A;

EID: 4444380590     PISSN: 00317012     EISSN: None     Source Type: Journal    
DOI: 10.1159/000079134     Document Type: Article

References (53)

1. Liddle RA: Cholecystokinin; in Walsh JH, Dockray GJ (eds): Gut Peptides. Biochemistry and Physiology. New York, Raven Press, 1994, pp 175-215.
2. Beinfeld MC: An introduction to neuronal cholecystokinin. Peptides 2001;22:1197-2000.
3. Crawley JN, Corwin RL: Biological actions of cholecystokinin. Peptides 1994;15:731-55.
4. Wank SA: Cholecystokinin receptors. Am J Physiol 1995;269:G628-G646.
5. Wank SA: G protein-coupled receptors in gastrointestinal physiology. I. CCK receptors: An exemplary family. Am J Physiol 1998;274: G607-G613.
6. Han J: Cholecystokinin octapeptide (CCK-8): a negative feedback control mechanism for opioid analgesia. Prog Brain Res 1995;105: 263-271.
7. Brenner LA, Ritter RC: Type A CCK receptors mediate satiety effects of intestinal nutrients. Pharmacol Biochem Behav 1996;54:625-631.
8. Ritter RC, Covasa M, Matson CA: Cholecystokinin: Proofs and prospects for involvement in control of food intake and body weight. Neuropeptides 1999;33:387-399.
9. Noble F, Roques B: CCK-B receptor: Chemistry, molecular biology, biochemistry and pharmacology. Prog Neurobiol 1999;58:349-379.
10. Daugé V, Lena I: CCK in anxiety and cognitive processes. Neurosci Biobehav Rev 1998;22: 815-825.
11. Griebel G: Is there a future for neuropeptide receptor ligands in the treatment of anxiety disorders? Pharmacol Ther 1999;82:1-61.
12. Lena I, Dh-tel H, Garbay C, Daugé V: Involvement of D2 dopamine receptors in the opposing effects of the two CCK-B agonists in a spatial recognition memory task: Role of the anterior nucleus accumbens. Psychopharmacology 2001;153:170-179.
13. Seva C, Kowalski-Chauvel A, Blanchet JS, Vaysse N, Pradayrol L: Gastrin induces tyrosine phosphorylation of Shc proteins and their association with the Grb2/Sos complex. FEBS Lett 1996;378:74-78.
14. Beglinger C: Potential role of cholecystokinin in the development of acute pancreatitis. Digestion 1999;60(suppl 1):61-63.
15. Niederau C, Grendell JH: Role of cholecystokinin in the development and progression of acute pancreatitis and the potential of therapeutic application of cholecystokinin receptor antagonists. Digestion 1999;60(suppl 1):69-74.
16. Ochi K, Harada H, Satake K: Clinical evaluation of cholecystokinin-A- receptor antagonist (loxiglumide) for the treatment of acute pancreatitis. A preliminary clinical trial. Study group of loxiglumide in Japan. Digestion 1999; 60(suppl 1):81-85.
17. Shiratori K, Takeuchi T, Satake K, Matsuno S: Clinical evaluation of oral administration of a cholecystokinin-A receptor antagonist (loxiglumide) to patients with acute, painful attacks of chronic pancreatitis: A multicenter dose-response study in Japan. Pancreas 2002;25:E1-E5.
18. Jensen R, Zhou Z, Murphy R, Jones S, Stenikar I, Rovarti L, Gardner J: Structural features of various proglumide-related cholecystokinin receptor antagonists. Am J Physiol 1986;251: G839-G846.
19. Setnikar I, Bani M, Cereda R, Chiste R, Makovec F, Pacini MA, Revel L: Loxiglumide protects against experimental pancreatitis. Arzneimittelforschung 1987;37:1172-1174.
20. Chang RS, Lotti VJ: Biochemical and pharmacological characterization of a new and extremely potent and selective non-peptide cholecystokinin antagonist. Proc Natl Acad Sci USA 1986;83:4923-4926.
21. A receptor antagonist. Br J Pharmacol 1996;90:753-761.
22. A receptor antagonist, in vitro. Eur J Pharmacol 1996;304:147-154.
23. A receptor antagonist with anxiolytic-like activity in animal models. Br J Pharmacol 1997;121:759-767.
24. Bignon E, Bachy A, Boigegrain R, Brodin R, Cottineau M, Gully D, Herbert JM, Keane P, Labie C, Molimard JC, Olliero D, Oury-Donat F, Petereau C, Prabonnaud V, Rockstroh MP, Shaeffer P, Servant O, Thurneyssen O, Soubrie P, Pascal M, Maffrand, JP, Le Fur G: SR146131: A new potent, orally active, and selective nonpeptide cholecystokinin subtype 1 receptor agonist. I. In vitro studies. J Pharmacol Exp Ther 1999;289:742-751.
25. Bignon E, Alonso R, Arnone M, Boigegrain R, Brodin R, Gueudet C, Heaulme M, Keane P, Landi M, Molimard JC, Olliero D, Poncelet M, Seban E, Simiand J, Soubrie P, Pascal M, Maffrand JP, Le Fur G: SR146131: A new potent, orally active and selective nonpeptide cholecystokinin subtype 1 receptor agonist. II. In vivo pharmacological characterization. J Pharmacol Exp Ther 1999;289:752-761.
26. 1 receptor antagonists: Structural modifications at the tryptophan domain. J Med Chem 1999; 42:4659-4668.
27. 1 receptor antagonists: Structure-activity relationship studies on the substituent at N2-position. J Med Chem 2001;44:2219-2228.
28. 1 receptor antagonists: Structure-activity relationship studies on the central 1,3-dioxoperhydropyrido[1,2-c]pyrimidine scaffold. J Med Chem 2001;44:4196-4206.
29. 1 receptor antagonists. J Med Chem 2000; 432:3770-3777.
30. B receptors by using a new highly potent CCK analog: BC 264. Synapse 1990;6:73-80.
31. Peikin S, Rottman A, Batzri S, Gardner D: Kinetics of amylase release by dispersed acini prepared from guinea pig pancreas. Am J Physiol 1978;4:E743-E749.
32. Fortuño A, Ballaz J, Del Río J, Barber A: CCK-mediated response in the activation of 5-HT receptor types in the guinea-pig ileum. J Physiol Biochem 1999;55:85-92.
33. 2 and affinity constants for pharmacological competitive antagonists be estimated? J Pharm Pharmacol 1978;30:312-313.
34. Tani, S, Otsuki M, Itoh H, Fujii, M, Nakamura T, Oka T, Baba S: Histologic and biochemical alterations in experimental acute pancreatitis induced by supramaximal caerulein stimulation. Int J Pancreatol 1987;2:337-348.
35. Murayama KM, Samuel I, Toriumi Y, Solomon TE, Turkelson CM, Joehl RJ, Drew J, Nahrwold D, Joehl R: Increased circulating cholecystokinin in obstruction-induced acute pancreatitis. I. Bile duct obstruction with and without pancreatic duct obstruction. J Surg Res 1993;54:126-131.
36. Hughes J, Boden P, Costall B, Domeney A, Kelly E, Horwell D, Hunter C, Pinnock R, Woodruff G: Development of a class of selective cholecystokinin type B receptor antagonists having potent anxiolytic activity. Proc Natl Acad Sci USA 1990;87:6728-6732.
37. Jensen R, Wank SA, Rowley WH, Sato S, Gardner J: Interaction of CCK with pancreatic acinar cells. Trends Pharmacol Sci 1989;10: 418-423.
38. Williams JA, Blevins GT: Cholecystokinin and regulation of pancreatic acinar cell function. Physiol Rev 1993;73:701-723.
39. Akiyama T, Otsuki M: Characterization of a new cholecystokinin receptor antagonist FK480 in in vitro isolated rat pancreatic acini. Pancreas 1994;9:324-331.
40. Lucaites, V, Mendelsohn L, Mason N, Cohen M: CCK-8, CCK-4 and gastrin-induced contractions in guinea pig ileum: Evidence for differential release of acetylcholine and substance P by CCK-A and CCK-B receptors. J Pharmacol Exp Ther 1991;256:695-703.
41. Dal Forno G, Pietra C, Urciouli M, Van Amsterdam F, Toson G, Gavigarhi G, Trist D: Evidence for two cholecystokinin receptor mediating the contraction of guinea pig isolated ileum longitudinal muscle myenteric plexus. J Pharmacol Exp Ther 1992;261:1056-1063.
42. Shutte IW, Akkermans LM, Kroese AB: CCKA and CCKB receptor subtypes both mediate the effects of CCK-8 on myenteric neurons in the guinea pig ileum. J Auton Nerv Syst 1997;67: 51-59.
43. Wettstein JG, Bueno L, Junien JL: CCK antagonists: Pharmacological and therapeutic interest. Pharmacol Ther 1994;62:267-284.
44. A receptor antagonist, on experimental acute pancreatitis. Jpn Pharmacol 1997;73: 105-112.
45. Murayama KM, Drew J, Nahrwold D, Joehl R: Cholecystokinin antagonist prevents hyperamylasemia and improves pancreatic exocrine function in cerulein-induced acute pancreatitis. Pancreas 1990;5:439-444.
46. García-Montero AC, Manso MA, Rodríguez AI, De Dios I: Therapeutic and protective effect of subcutaneous injections of L-364,718 on caerulein-induced acute pancreatitis. Pancreas 1994;9:309-315.
47. Satake K, Kimura K, Saito T: Therapeutic effects of loxiglumide on experimental acute pancreatitis using various models. Digestion 1999;60(suppl 1):64-68.
48. D'Amato M, Rovati LC: CCK-A antagonists: Which and how. Eur J Clin Invest 1995;25:213-214.
49. Varga G, Kisfalvi K, Pelosini I, D'Amato M, Scarpignato C: Different actions of CCK on pancreatic and gastric growth in the rat: Effect of CCK(A) receptor blockade. Br J Pharmacol 1998;124:435-440.
50. Toriumi Y, Samuel I, Wilcockson DP, Turkelson CM, Solomon T, Joehl R: Octreotide and cholecystokinin antagonist reduce edema in obstruction-induced acute pancreatitis. J Lab Clin Med 1993;122:450-454.
51. Otzuki M: Pathophysiological role of cholecystokinin in humans. J Gastroenterol Hepatol 2000;15(suppl):D71-D83.
52. Oshio G, Saluja A, Steer ML: Effects of short-term pancreatic duct obstruction in rats. Gastroenterology 1991;100:196-202.
53. De Dios I, Uruñuela A, Orfao A, Manso M: Cholecystokinin antagonist L-364,718 induces alterations in acinar cells that prevent improvement of acute pancreatitis induces by obstruction. Dig Dis Sci 2002;47:1800-1809.