Pharmacological analysis of CCK2 receptor antagonists using isolated rat stomach ECL cells

British Journal of Pharmacology

Volumn 127, Issue 2, 1999, Pages 530-536

  Lindström, Erik ^a   Björkqvist, Maria ^a   Håkanson, Rolf ^a  

^a LUND UNIVERSITY   (Sweden)

Author keywords

CCK B gastrin receptor antagonists; CCK B gastrin receptors; CCK2 receptor antagonists; CCK2 receptors; ECL cells; Gastrin; Pancreastatin

Indexed keywords

1 [2,3 DIHYDRO 1 (2' METHYLPHENACYL) 2 OXO 5 PHENYL 1H 1,4 BENZODIAZEPIN 3 YL] 3 (3 METHYLPHENYL)UREA; 1 [2,3 DIHYDRO 2 OXO 1 PIVALOYLMETHYL 5 (2 PYRIDYL) 1H 1,4 BENZODIAZEPIN 3 YL] 3 [3 (METHYLAMINO)PHENYL]UREA; 1 [5 (3 AZABICYCLO[3.2.2]NON 3 YL) 2,3 DIHYDRO 1 METHYL 2 OXO 1H 1,4 BENZODIAZEPIN 3 YL] 3 (3 METHYLPHENYL)UREA; 4 [[2 [2 [[(2 ADAMANTYLOXY)CARBONYL]AMINO] 3 (1H INDOL 3 YL) 2 METHYLPROPIONAMIDO] 1 PHENYLETHYL]AMINO] 4 OXOBUTYRIC ACID MEGLUMINE; 5 [[[[(3,5 DICARBOXYPHENYL)AMINO]CARBONYL] 2 PHENYLETHYLAMINO]CARBONYL] 6 [[(1 ADAMANTYLMETHYL)AMINO]CARBONYL]INDOLE; AG 041R; CHOLECYSTOKININ RECEPTOR BLOCKING AGENT; DEVAZEPIDE; GASTRIN; PANCREASTATIN; PD 135158; PD 136450; RP 73870; UNCLASSIFIED DRUG; CHOLECYSTOKININ A RECEPTOR; CHOLECYSTOKININ B RECEPTOR; CHOLECYSTOKININ RECEPTOR; PANCREAS HORMONE;

ANIMAL CELL; ARTICLE; CELL SECRETION; MALE; NONHUMAN; PRIORITY JOURNAL; RADIOIMMUNOASSAY; RAT; STOMACH; ANIMAL; CELL CULTURE; CYTOLOGY; DRUG ANTAGONISM; DRUG EFFECT; ENTEROENDOCRINE CELL; KINETICS; METABOLISM; SPRAGUE DAWLEY RAT; STOMACH MUCOSA;

ANIMALS; CELLS, CULTURED; ENTEROENDOCRINE CELLS; GASTRIC MUCOSA; KINETICS; MALE; PANCREATIC HORMONES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTOR, CHOLECYSTOKININ A; RECEPTOR, CHOLECYSTOKININ B; RECEPTORS, CHOLECYSTOKININ; STOMACH;

EID: 0032589130     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0702538     Document Type: Article

References (64)

1. Andersson, K., Cabero, J.L., Mattsson, H. & Håkanson, R. (1996). Gastric acid secretion after depletion of enterochromaffin-like cell histamine. Scand. J. Gastroenterol., 31, 24-30.
2. Asahara, M., Kinoshita, H., Nakata, H., Matsushima, Y., Naribayashi, Y., Nakamura, A., Matsui, K., Chihara, K., Yamamoto, J., Ichikawa, A. & Chiba, T. (1994). Gastrin receptor genes are expressed in gastric parietal and enterochromaffin-like cells of mastomys natalensis. Dig. Dis. Sci., 39, 2149-2156.
3. Baba, A., Hoshino, E., Onoma, M., Esaki, T. & Takeda, K. (1995). Pharmacological profile of AG041R. A novel selective gastrin/CCK-B antagonist. Gastroenterology, 108, A950 (abstract).
4. Beinborn, M., Lee, Y.-M., McBride, E.W., Quinn, S.M. & Kopin, A.S. (1993). A single amino acid of the cholecystokinin-B/gastrin receptor determines specificity for non-peptide antagonists. Nature, 362, 348-350.
5. Beinfeld, M.C. (1983). Cholecystokinin in the central nervous system: A minireview. Neuropeptides, 3, 411-427.
6. Bertrand, P., Bohme, G.A., Durieux, C., Guyon, C., Capet, M., Jeantaud, B., Boudeau, P., Ducos, B., Pendley, C.E. & Martin, G.E. (1994). Pharmacological properties of ureidoacetamides, new potent and selective non-peptide CCK/gastrin receptor antagonists. Eur. J. Pharmacol., 262, 233-245.
7. Black, J.W. & Shankley, N.P. (1985). The isolated stomach preparation of the mouse: a physiological unit for pharmacological analysis. Br. J. Pharmacol., 86, 571-579.
8. 3H] I.-365,260: a new potent and selective brain cholecystokinin (CCK-B) and gastrin receptor antagonist radioligand. Mol. Pharm., 35, 803-810.
9. Chang, R.S.L. & Lotti, V.J. (1986). Biochemical and pharmacological characterization of an extremely potent and selective nonpeptide cholecystokinin antagonist. Proc. Natl. Acad. Sci. U.S.A., 83, 4923-4926.
10. Chen, D., Marvik, R., Ronning, K., Andersson, K., Waldum, H.L. & Håkanson, R. (1996). Gastrin-evoked secretion of histamine, pancreastatin and acid from the isolated, vascularly perfused rat stomach. Effects of isobutylmethylxanthin and α-fluoromethylhistidine. Regul. Pept., 65, 133-138.
11. Chen, D., Monstein, H.-J., Nylander, A.-G., Zhao, C.-M., Sundler, F. & Håkanson, R. (1994). Acute responses of rat stomach enterochromaffin-like cells to gastrin: Secretory activation and adaptation. Gastroenterology, 107, 18-27.
12. Chiba, T., Kinoshita, Y., Morishita, T., Nakata, H., Nakamura, A. & Hosoda, S. (1991). Receptors for gastrin on gastric carcinoid tumor membranes of Mastomys Natalensis. Biochem. Biophys. Res. Commun., 177, 739-744.
13. Dartsch, C., Chen, D. & Persson, L. (1998). Multiple forms of rat histidine decarboxylase may reflect posttranslational activation of the enzyme. Regul. Pept., 77, 33-41.
14. Dartsch, C. & Persson, L. (1998). Recombinant expression of rat histidine decarboxylase: generation of antibodies useful for western blot analysis. Int. J. Biochem. Cell Biol., 30, 773-782.
15. Ding, X.-Q., Chen, D. & Håkanson, R. (1995). Cholecystokinin-B receptor ligands of the dipeptoid series act as agonists on rat stomach histidine decarboxylase. Gastroenterology, 109, 1181-1187.
16. Ding, X.-Q. & Håkanson, R. (1996a). Effect of gastrin receptor blockade on gastric acid secretion in conscious rats. Pharmacol. Toxicol., 79, 324-330.
17. Ding, X.-Q. & Håkanson, R. (1996b). Evaluation of the specificity and potency of a series of cholecystokinin-B/gastrin receptor antagonists in vivo. Pharmacol. Toxicol., 79, 124-130.
18. Ding, X.-Q., Kitano, M. & Håkanson, R. (1998). Sustained cholecystokinin-B/gastrin receptor blockade does not impair basal and histamine-stimulated acid secretion in chronic gastric fistula rats. Pharmacol. Toxicol., 87, 177-182.
19. Ding, X.-Q., Lindström, E. & Håkanson, R. (1997a). Time-course of deactivation of rat stomach ECL cells following cholecystokinin-B/gastrin receptor blockade. Br. J. Pharmacol., 122, 1-6.
20. Ding, X.-Q., Lindström, E. & Håkanson, R. (1997b). Cholecystokinin-B/gastrin receptor blockade suppresses the activity of rat stomach ECL cells. Pharmacol. Toxicol., 81, 19-25.
21. Ding, X.-Q., Lindström, E. & Håkanson, R. (1997c). Evaluation of three novel cholecytokinin-B/gastrin receptor antagonists: A study of their effects on rat stomach ECL cell activity. Pharmacol. Toxicol., 81, 232-237.
22. Dunlop, J., Brammer, N., Evans, N. & Ennis, C. (1997). YM022 [(R)-1-[2,3-dihdro-1-(2′-methylphenacyl)-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-y1]-3-(3-methylphenyl)urea]: an irreversible cholecystokinin type-B receptor antagonist. Biochem. Pharm., 54, 81-85.
23. Håkanson, R, Chen, D. & Sundler, F. (1994). The ECL cells. In Physiology of the Gastrointestinal Tract. ed. Johnson, L.R. Volume 2, 3rd ed. pp. 1171-1184. New York: Raven Press.
24. Håkanson, R, Ding, X.-Q., Norlén, P. & Chen, D. (1995). Circulating pancreastatin is a marker for the enterochromaffin-like cells of the rat stomach. Gastroenterology, 108, 1445-1452.
25. 2 receptor antagonists: pharmacological tools to study the gastrin-ECL cell-parietal cell axis. Regul. Pept., 80, 1-11.
26. Håkanson, R, Tielemans, Y., Chen, D., Andersson, K., Ryberg, B., Mattsson, H. & Sundler, F. (1992). The biology and pathobiology of the ECL cells. Yale J. Biol. Med., 65, 761-774.
27. Håkanson, R, Tielemans, Y., Chen, D., Andersson, K., Mattsson, H. & Sundler, F. (1993). Time-dependent changes in enterochromaffinlike cell kinetics in stomach of hypergastrinemic rats. Gastroenterology, 105, 15-21.
28. B/gastrin receptors mediating pentagastrin-stimulated gastric acid secretion in the isolated stomach of the immature rat. Br. J. Pharmacol., 119, 1401-1410.
29. Hughes, J., Boden, P., Costall, B., Domeney, A., Kelly, E., Horwell, D.C., Hunter, J.C., Pinnock, R.D. & Woodruff, G.N. (1990). Development of a class of selective cholecystokinin type B receptor antagonists having potent anxiolytic activity. Proc. Natl. Acad. Sci. U.S.A., 87, 6728-6732.
30. Innis, R.B. & Snyder, S.H. (1980). Distinct cholecystokinin receptors in brain and pancreas. Proc. Natl. Acad. Sci. U.S.A., 77, 6917-6928.
31. Jenkinson, D.H. (1991). How we describe competitive antagonists: three questions of usage. Trends Pharmacol. Sci., 12, 53-54.
32. B/gastrin receptor antagonists: recent advances and potential uses in gastric secretory disorders. Yale J. Biol Med., 69, 245-259.
33. Kalindijan, S.B., Buck, I.M., Davis, M.M.R., Dunstone, D.J., Hudson, M.L., Low, C.M.R., McDonald, I.M., Pether, M.J., Steel, K.I.M., Tozer, M.J. & Vinter, J.G. (1996). Non-peptide cholecystokinin-B/gastrin receptor antagonists based on bicyclic, heteroaromatic skeletons. J. Med. Chem., 39, 1806-1815.
34. Kawabata, S., Kanayama, S., Shinomura, Y., Miyazaki, Y., Imamura, I., Moriwaki, K., Wada, H. & Tarui, S. (1991). Effect of CCK receptor antagonists, MK-329 and L-365,260 on CCK-induced acid secretion and HDC activity in the rat. Regul. Pept., 35, 1-10.
35. Kimura K., Chen, D., Lindström, E., Zhao, C.-M. & Håkanson, R. (1997). Evidence that rat stomach ECL cells represent the main source of circulating pancreastatin. Regul. Pept., 68, 177-180.
36. Kinoshita, Y., Nakata, H., Asahara, M., Kawanami, C., Matsushima, Y., Kishi, K., Hoshino, E., Baba, A. & Chiba, T. (1996). Effects of a new gastrin/cholecystokinin-B receptor antagonist AG-041R on ECL carinoid tumor cells of mastomys natalensis. Regul. Pept., 64 (suppl), 90 (abstract).
37. Kinoshita, Y., Nakata, H., Kishi, K., Kawanamai, C., Sawada, M. & Chiba, T. (1998). Comparison of the signal transduction pathways activated by gastrin in enterochromaffin-like and parietal cells. Gastroenterology, 115, 93-100.
38. Kopin, A.S., Lee, Y.-M., McBride, E.W., Miller, L.J., Lu, M., Lin, H.Y., Kolakowski, L.F. & Beinborn, M. (1992). Expression cloning and characterization of the canine parietal cell gastrin receptor. Proc. Natl. Acad. Sci. U.S.A., 89, 3605-3609.
39. Kopin, A.S., McBride, E.W., Gordon, M.C., Quinn, S.M. & Beinborn, M. (1997). Inter- and intrapsecies polymorphisms in the cholecystokinin-B/gastrin receptor alter drug efficacy. Proc. Natl. Acad. Sci. U.S.A., 94, 11043-11048.
40. Leff, P. & Dougall, I.G. (1993). Further concerns over Cheng-Prusoff analysis. Trends Pharmacol. Sci., 14, 110-112.
41. 2+ evaluation in rabbit parietal cells: a novel method to screen gastrin receptor antagonists. Eur. J. Pharmacol., 306, 325-333.
42. Lindström, E., Björkqvist, M., Boketoft, Å., Chen, D., Zhao, C.-M., Kimura, K. & Håkanson, R. (1997). Neurohormonal regulation of histamine and pancreAstatin secretion from isolated rat stomach ECL cells. Regul. Pept., 71, 73-86.
43. B/gastrin receptor antagonists as potential drugs for peptic ulcer therapy. Drug Discovery Today, 7, 283-293.
44. Miyake, A., Mochizuki, S. & Kawashima, H. (1994). Characterization of cloned human cholecystokinin-B receptor as a gastrin receptor. Biochem. Pharmacol., 47, 1339-1343.
45. Nishida, A., Miyata, R., Tsutsumi, H., Yuki, S., Akuzawa, A., Kobayashi, T., Kamato, H., Ito, M., Yamano, Y., Katauyama, M., Satoh, M., Ohta, M. & Honda, K. (1994a). Pharmacological profile of (R)-1-[2,3-dihydro-1-(2′methylphenacyl)-2-oxo-5-phenyl-1H-1,4-benzodiazepine-3-y1]-3-(methylphenyl)urea (YM022), a new potent and selective gastrin/ cholecystokinin (CCK)-B receptor antagonist, in vitro and in vivo. J. Pharmacol. Exp. Ther., 269, 725-731.
46. Nishida, A., Takinami, Y., Yuki, H., Kobayashi, A., Akuzawa, S., Kamato, T., Ito, H., Yamano, M., Nagakura, Y. & Miyata, K. (1994b). YM022 {(R)-1-[2,3-dihydro-1-)2′methylphenacyl)-2-oxo-5-phenyl-1-H1, 4-benzodiazepine-3-y1]-3-(3′methylphenyl)urea}, a potent and selective gastrin/cholecystokinin-B receptor antagonist, prevents gastric and duodenal lesions in rats. J. Pharmacol. Exp. Ther., 270, 1256-1261.
47. Norlén, P., Curry, W.J., Chen, D., Zhao, C.-M., Johnston, C.F., Håkanson, R. (1997). Expression of the chromogranin A-derived peptides pancreastatin and WEI4 in rat stomach ECL cells. Regul. Pept., 70, 121-133.
48. Patel, S., Smith, A.J., Chapman, K.L., Fletcher, A.E., Kemp, J.A., Marshall, G.R., Hargreaves, R.J., Ryecroft, W., Iversen, L.L., Iversen, S.D., Baker, R., Showell, G.A., Bourrain, S., Neduvelil, J.G., Matassa, V.G. & Freedman, S.B. (1994). Biological properties of the benzodiazepine amidine derivative L-740,093, a cholecystokinin-B/gastrin receptor antagonist with high affinity in vitro and high potency in vivo. Mol. Pharmacol., 46, 943-948.
49. Pendley, C.E., Fitzpatrick, L.R., Capolino, A.J., Davis, M.A., Esterline, N.J., Jakubowska, A., Bertrand, P., Guyon, C., Dubroeucq, M.-C. & Martin, G.E. (1995). RP73870, a gastrin/cholecystokinin-B antagonist with potent anti-ulcer activity in the rat. J. Pharmacol. Exp. Ther., 273, 1015-1022.
50. Prinz, C., Kajimura, M., Scott, D.R., Mercier, F., Helander, H.F., Sachs, G. (1993). Histamine secretion from rat enterochromafinlike cells. Gastroenterology, 105, 449-461.
51. Prinz, C., Scott, D.R., Hurwitz, D., Helander, H.F. & Sachs, G. (1994). Gastrin effects on isolated rat enterochromaffin-like cells in primary culture. Am. J. Physiol., 267, G663-G675.
52. Roche, S., Gusdinar, T., Bali, J.P. & Magous, R. (1991a). 'Gastrin' and 'CCK' receptors on histamine-and somatostatin-containing cells from rabbit fundic mucosa-I. Characterization by means of agonists. Biochem. Pharmacol., 42, 765-770.
53. Roche, S., Gusdinar, T., Bali, J.P. & Magous, R. (1991b). 'Gastrin' and 'CCK' receptors on histamine-and somatostain-containing cells from rabbit fundic mucosa-II. Characterization by means of selective antagonists (L-364,718 and L-365,260). Biochem. Pharmacol., 42, 771-776.
54. Sandvik, A.K. & Waldum, H.L. (1991). CCK-B (gastrin) receptor regulates histamine release and acid secretion. Am. J. Physiol., 260, G925-G928.
55. χ and competitive drug antagonism. Br. J. Pharmacol., 4, 277-280.
56. Schmassmann, A., Garner, A., Flogerzi, B., Hasan, M.Y., Sanner, M., Varga, I. & Halter, F. (1994). Cholecystokinin type B receptor antagonist PD-136,450 is a partial agonist in the stomach and a full agonist in the pancreas of the rat. Gut, 35, 270-274.
57. Semple, G., Ryder, H., Rooker, D.P., Batt, A.R., Kendrick, D.A., Szelke, M., Ohta, M., Satoh, M., Nishida, A., Akuzawa, S. & Miyata, K. (1997). (3R)-N-(1-(tert-Butylcarbonylmethyl)-2,3-dihdro-2-oxo-5-(2-pyridyl)-1H-1,4-benzodiazepin-3-y1)-N′-(3-(methylamino)phenyl)urea (YF476): A potent and orally active gastrin/CCK-B antagonist. J. Med. Chem., 40, 331-341.
58. Takinami, Y., Yuki, H., Nishida, A., Akuzawa, S., Uchida, A., Takemoto, Y., Ohta, M., Satoh, M., Semple, G. & Miyata, K. (1997). YF476 is a new potent and selective gastrin/ cholecystokinin-B receptor antagonist in vitro and in vivo. Aliment. Pharmacol. Ther., 11, 113-120.
59. Wank, S.A. (1998). G protein-coupled receptors in gastrointestinal physiology I. CCK receptors: an exemplary family. Am. J. Physiol., 274, G607-G613.
60. Wank, S.A., Harkins, R., Jensen, R.T., Shapira, H., Weerth, A.D. & Slattery, T. (1992a). Purification, molecular cloning, and functional expression of the cholecystokinin receptor from rat pancreas. Proc. Natl. Acad. Sci. U.S.A., 89, 3125-3129.
61. Wank, S.A., Pisegna, J.R. & Weerth, A.D. (1992b). Brain and gastrointestinal cholecystokinin receptor family: Structure and functional expression. Proc. Natl. Acad Sci. U.S.A., 89, 8691-8695.
62. Winkler, H., Apps, D.-K. & Fischer-Colbrie, R. (1986). The molecular function of adrenal chromaffin granules: established facts and unresolved topics. Neuroscience, 18, 261-290.
63. Winkler, H. & Fischer-Colbrie, R. (1992). The chromogranins A and B: the first 25 years and futrue perspectives. Neuroscience, 49, 497-528.
64. Yuki, H., Nishida, A., Miyake, A., Ito, H., Akuzawa, S., Takinami, Y., Takemoto, Y. & Miyata, K. (1997). YM022, a potent and selective gastrin/CCK-B receptor antagonists, inhibits peptone meal-induced gastric acid secretion in Heidenhain pouch dogs. Dig. Dis. Sci., 42, 707-714.