YF476 is a new potent and selective gastrin/cholecystokinin-B receptor antagonist in vitro and in vivo

Alimentary Pharmacology and Therapeutics

Volumn 11, Issue 1, 1997, Pages 113-120

  Takinami, Y ^a   Yuki, H ^a   Nishida, A ^a   Akuzawa, S ^a   Uchida, A ^a   Takemoto, Y ^a   Ohta, M ^a   Satoh, M ^a   Semple, G ^b   Miyata, K ^a  

^a ASTELLAS PHARMA INC   (Japan)

^b Ferring Research Institute   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

1 (2,3 DIHYDRO 1 METHYL 2 OXO 5 PHENYL 1H 1,4 BENZODIAZEPIN 3 YL) 3 (3 METHYLPHENYL)UREA; 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; 4 [[2 [2 [[(2 ADAMANTYLOXY)CARBONYL]AMINO] 3 (1H INDOL 3 YL) 2 METHYLPROPIONAMIDO] 1 PHENYLETHYL]AMINO] 4 OXOBUTYRIC ACID MEGLUMINE; BETHANECHOL; CHOLECYSTOKININ; CHOLECYSTOKININ RECEPTOR; CHOLECYSTOKININ RECEPTOR BLOCKING AGENT; DEVAZEPIDE; FAMOTIDINE; GASTRIN; GASTRIN RECEPTOR; HISTAMINE; PENTAGASTRIN; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; DRUG RECEPTOR BINDING; IN VITRO STUDY; IN VIVO STUDY; INTRAVENOUS DRUG ADMINISTRATION; ISOTOPE LABELING; MALE; NONHUMAN; PRIORITY JOURNAL; RAT; STOMACH ACID SECRETION;

EID: 8044235636     PISSN: 02692813     EISSN: None     Source Type: Journal    
DOI: 10.1046/j.1365-2036.1997.110281000.x     Document Type: Article

References (24)

1. Elwin C-E. Gastric acid responses to antral application of some amino acids, peptides, and isolated fractions of a protein hydrolysate. Scand J Gastroenterol 1974; 9: 139-247.
2. DelValle J, Yamada T. Amino acids and amines stimulate gastrin release from canine antral G cells via different pathways. J Clin Invest 1990; 85: 139-45.
3. Richardson CT, Walsh JH, Hicks MI, Fordtran JS. Studies on the mechanisms of food-stimulated gastric acid secretion in normal human subjects. J Clin Invest 1976; 58: 623-31.
4. Maxwell V, Eysselein VE, Kleibeuker J, Reedy T, Walsh JH. Glucose perfusion intragastric titration. Dig Dis Sci 1984; 29: 321-6.
5. Debas HT, Walsh JH, Grossman MI. Evidence for oxyntopyloric reflex for release of antral gastrin. Gastroenterol 1975; 68: 687-90.
6. Walsh JH, Richardson CT, Fordtran S, pH dependence of acid secretion and gastrin release in normal and ulcer subjects. J Clin Invest 1975; 55: 462-8.
7. Kopin AS, Lee Y-M, McBride EW, et al. Expression cloning and characterization of the canine parietal cell gastrin receptor. Proc Natl Acad Sci 1992; 89: 3605-9.
8. Pisegna JR, deWeerth A, Huppi K, Wank SA. Molecular cloning of the human brain and gastric cholecystokinin receptor: structure, functional expression and chromosomal localization. Biochem Biophys Res Communication 1992; 189: 296-303.
9. Lee Y-M, Beinborn M, McBride EW, et al. The human brain cholecystokinin-B/gastrin receptor. Cloning and characterization. J Biol Chem 1993; 268: 8164-9.
10. 14C]aminopyrine accumulation by isolated canine parietal cells. Am J Physiol 1980; 238: G366-75.
11. Sandvik AK, Waldum HL, CCK-B (gastrin) receptor regulates gastric histamine release and acid secretion. Am J Physiol 1991; 260: G925-8.
12. Lotii VJ, Chang SL. A new potent and selective non-peptide gastrin antagonist and brain cholecystokinin receptor (CCK-B) ligand: L-365, 260. Eur J Pharmacol 1989; 162: 273-80.
13. Beinborn M, Lee Y-M, McBride EW, Quinn SM, Kopin AS. A single amino acid of the cholecystokinin-B/gastrin receptor determines specificity for non-peptide antagonists. Nature 1993; 362: 348-50.
14. B/gastrin antagonists on stimulated gastric acid secretion in the anaesthetized rat. Br J Pharmacol 1991; 104: 973-7.
15. Hirst BH, Elliott KJ, Ryder H, Szelke M, Inhibition of gastrinand histamine-stimulated gastric acid secretion by gastrin and cholecystokinin antagonists in the rat. Aliment Pharmacol Ther 1991; 5: 31-9.
16. Nishida A, Yuki H, Tsutsumi R, et al. L-365, 260, a potent CCK-B/gastrin receptor antagonist. suppresses gastric acid secretion induced by histamine and bethanechol as well as pentagastrin in rats. Japan J Pharmacol 1992; 58: 137-45.
17. Horwell DC, Hughes J, Hunter JC, et al. Rationally designed 'dipeptoid' analogues of CCK. α-methyltryptophan derivatives as highly selective and orally active gastrin and CCK-B antagonists with potent anxiolytic properties. J Med Chem 1991; 34: 404-14.
18. Nishida A, Miyata K, Tsutsumi R, et al. Pharmacological profile of (R)-1-[2,3-dihydro-1-(2′-methyl-phenacyl)-2-oxo-5-pheny-1H-1.4- benzodiazepin-3-yl]-3-(3-methylphenyl)urea (YM022). a new potent and selective gastrin/cholecystokinin-B receptor antagonist, in vitro and in vivo. J Pharmacol Exp Ther 1994; 269: 725-31.
19. Satoh M, Anan H, Nishida A, et al. Substituted 1.4-benzodiazein-2-one derivatives as potent, selective and orally active gastrin/CCK-B antagonists. Abstr Pa Am Chem Soc 1995; 210 Meet., Pt. 2, MEDI166.
20. 3H]glutamate binding sites in brain synaptic membranes treated with Triton X-100. Biochem Biophys Acta 1989; 1012: 74-80.
21. Chang RSL, Lotti VJ. Biochemical and pharmacological characterization of an extremely potent and selective nonpeptide cholecystokinin antagonist. Proc Natl Acad Sci 1986; 83: 4923-6.
22. Mizushima S, Nagata S, pEF-BOS, a powerful mammalian expression vector. Nucl Acids Res 1990; 18: 5322.
23. 2+ mobilization. Eur J Pharmacol 1994; 269: 249-54.
24. Takeuchi K, Furukawa O, Tanaka H, Okabe S. A new model of duodenal ulcers induced by indomethacin and histamine. Gastroenterology 1986; 90: 636-45.