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Review

Novel approaches to the pharmacological blockade of gastric acid secretion

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Pages 411-421 | Published online: 22 Apr 2005

Bibliography

  • VAN PINXTEREN B, NUMANS ME, LAU J, DE WIT NJ, HUNGIN AP, BONIS PA: Short-term treatment of gastroesophageal reflux disease. J. an. Intern. Med. (2003) 18:755–763.
  • CHIBA N, DE GARA CJ, WILKINSON JM, HUNT RH: Speed of healing and symptom relief in grade II to IV gastroesophageal reflux disease: a meta-analysis. Gastroenterology (1997) 112:1798–1810.
  • CRAWLEY JA, SCHMITT CM: How satisfied are chronic heartburn suffers with their prescription medications? Results of the patient unmet needs survey. J. Clin. Outcomes Management (2000) 7:29–34.
  • ANDERSSON T: Pharmacokinetics, metabolism and interactions of acid pump inhibitors. Focus on omeprazole, lansoprazole and pantoprazole. Clin. Pharmacokinet. (1996) 31:9–28.
  • TONINI M, GIORGIO RD, PONTI FD:Novel therapeutic strategies in acid-related disorders. Expert Opin. Ther. Targets (2003) 13:639–649.
  • KIL BJ, KIM IW, SHIN CY et al: Comparison of IY81149 with omeprazole in rat reflux oesophagitis. Auton. Pharmacol. (2000) 20:291–296.
  • DOMAGALA F, FICHEUX H: Pharmacokinetics of tenatoprazole, a novel proton pump inhibitor, in healthy male caucasian volunteers. Gastroenterology (2003) 124:S1608 (Abstract).
  • GALMICHE JP, BRULEY DV, DUCROTTE P et al.: Tenatoprazole, a novel proton pump inhibitor with a prolonged plasma half-life: effects on intragastric pH and comparison with esomeprazole in healthy volunteers. Aliment. Pharmacol. Ther. (2004) 19:655–662.
  • TONINI M, DE GIORGIO R, DE PONTI F: Progress with novel pharmacological strategies for gastro-oesophageal reflux disease. Drugs (2004) 64:347–361.
  • DAJANI EZ, KLAMUT MJ: Novel therapeutic approaches to gastric and duodenal ulcers: an update. Expert. Opin. Investig. Drugs (2000) 9:1537–1544.
  • VAKIL N: New pharmacological agents for the treatment of gastro-oesophageal reflux disease. Aliment. Pharmacol Ther. (2004) 19:1–9.
  • ••An important paper that provides anoverview of a number of new drug groups that may represent the future medical therapy for GORD.
  • BLACK JW, DUNCAN WA, DURANT CJ, GANELLIN CR, PARSONS EM: Definition and antagonism of histamine H2 receptors. Nature (1972) 236:385–390.
  • ••An important paper on the discovery of1–12 receptors.
  • CORUZZI G, MORINI G, ADAMI M, GRANDI D: Role of histamine H3 receptors in the regulation of gastric functions. J. Physiol Pharmacol. (2001) 52:539–553.
  • PRINZ C, KAJIMURA M, SCOTT DR, MERCIER F, HELANDER HF, SACHS G: Histamine secretion from rat enterochromaffin like cells. Gastroenterology (1993) 105:449–461.
  • KIDD M, TANG LH, MIU K, LAWTON GP, SANDORA, MODLIN IM: Autoregulation of enterochromaffin-like cell histamine secretion via the histamine 3 receptor subtype. Yale J. Biol. Med. (1996) 69:9–19.
  • HOLLANDE F, BALI JP, MAGOUS R: Autoregulation of histamine synthesis through H3 receptors in isolated fundic mucosal cells. Am. Physic] (1993) 265:G1039–G1044.
  • BADO A, MOIZO L, LAIGNEAU JP, LEWIN MJ: Pharmacological characterization of histamine H3 receptors in isolated rabbit gastric glands. Am. Physic] (1992) 262:G56–G61.
  • LINDSTROM E, BJORKQVIST M, BOKETOFT A et al.: Neurohormonal regulation of histamine and pancreastatin secretion from isolated rat stomach ECL cells. Regal. Pept. (1997) 71:73–86.
  • YOKOTANI K, MURAKAMI Y, OKADA S, WANG M, NAKAMURA K: Histamine H(3) receptor-mediated inhibition of endogenous acetylcholine release from the isolated, vascularly perfused rat stomach. Eur. Pharmacol (2000) 392:23–29.
  • BADO A, LAIGNEAU JP, MOIZO L, CHERIFI Y, LEWIN MJ: H3-receptor activation inhibits cholinergic stimulation of acid secretion in isolated rabbit fundic glands. I Pharmacol Exp. Ther. (1995) 275:1099–1103.
  • CORUZZI G, ADAMI M, BERTACCINI G: Histamine H3 receptors are not involved in the regulation of rat gastric secretion. Pharmacology (1992) 44:190–195.
  • VUYYURU L, SCHUBERT ML: Histamine, acting via H3 receptors, inhibits somatostatin and stimulates acid secretion in isolated mouse stomach. Gastroenterology (1997) 113:1545–1552.
  • CORUZZI G, BERTACCINI G, SCHWARTZ JC: Evidence that histamine H3 receptors are involved in the control of gastric acid secretion in the conscious cat. Naunyn Schmiedebergs. Arch. Pharmacol (1991) 343:225–227.
  • BADO A, HERVATIN F, LEWIN MJ: Pharmacological evidence for histamine H3 receptor in the control of gastric acid secretion in cats. Am. J. Physic] (1991) 260:G631–G635.
  • •A key paper that investigates the Involvement of the H3 receptor in the control of gastric acid secretion.
  • BAROCELLI E, BALLABENI V, CHIAVARINI M, IMPICCIATORE M: R-a-methylhistamine-induced inhibitionof gastric acid secretion in pylorus-ligatedrats via central histamine H3 receptors. BEPharmacol. (1995) 115:1326–1330.
  • BALLABENI V, CALCINA F, BOSETTI M et al.: Different role of the histamine H3-receptor in vagal-, betanechol-, pentagastrin-induced gastric acid secretion in anaesthetized rats. Scand. Gastroenterol. (2002) 37:754–758.
  • SOLDANI G, MENGOZZI G, INTORRE L, DE GIORGI G, CORUZZI G, BERTACCINI G: Histamine H3 receptor-mediated inhibition of gastric acid secretion in conscious dogs. Naunyn Schmiedebergs. Arch. Pharmacol (1993) 347:61–65.
  • SOLDANI G, GARBARG M, INTORRE L, BERTINI S, ROULEAU A, SCHWARTZ JC: Modulation of pentagastrin-induced histamine release by histamine H3 receptors in the dog. Scand. Gastroenterol. (1996) 31:631–638.
  • •A key paper that examines the control of acid secretion by the H3 receptor.
  • SOLDANI G, INTORRE L, BERTINI S, LUCHETTI E, CORUZZI G, BERTACCINI G: Regulation of gastric acid secretion by histamine H3 receptors in the dog: an investigation into the site of action. Naunyn Schmiedebergs. Arch. Pharmacol. (1994) 350:218–223.
  • ROULEAU A, GARBARG M, LIGNEAU X et al.: Bioavailability, antinociceptive and antiinflammatory properties of BP 2-94, a histamine H3 receptor agonist prodrug. Pharmacol Exp. Ther. (1997) 281:1085–1094.
  • STARK H, KRAUSE M, ROULEAU A, GARBARG M, SCHWARTZ JC, SCHUNACK W: Enzyme-catalyzed prodrug approaches for the histamine H3-receptor agonist N-a-methylhistamine. Bioorg. Med. Chem. (2001) 9:191–198.
  • KRAUSE M, STARK H, SCHUNACK W: Azomethine prodrugs of (R)-a-methylhistamine, a highly potent and selective histamine H3-receptor agonist. Curr. Med. Chem. (2001) 8:1329–1340.
  • SOLDANI G, BERTINI S, ROULEAU A, SCHWARTZ JC, CORUZZI G: Gastric antisecretory effects of compound BP 2-94: a histamine H3-receptor agonist prodrug. Dig. Dis. Sci. (1999) 44:2380–2385.
  • ••A key paper that confirms the mainmechanism underlying the inhibition of acid production induced by H3 receptor activation.
  • FOZARD JR: BP-294 Ste Civile Bioprojet. Curr. Opin. Investig. Drugs (2000) 1:86–89.
  • BLAIR AJ III, RICHARDSON CT, WALSH JH, FELDMAN M: Variable contribution of gastrin to gastric acid secretion after a meal in humans. Gastroenterology (1987) 92:944–949.
  • KIDD M, MODLIN IM, TANG LH: Gastrin and the enterochromaffin-like cell: an acid update. Dig. &mg. (1998) 15:209–217.
  • HOLST JJ, KNUHTSEN S, ORSKOV C, SKAK-NIELSEN T, POULSEN SS, NIELSEN OV: GRP-producing nerves control antral somatostatin and gastrin secretion in pigs. Am. J. Physic] (1987) 253:G767–G774.
  • PRINZ C, SCOTT DR, HURWITZ D, HELANDER HF, SACHS G: Gastrin effects on isolated rat enterochromaffin-like cells in primary culture. Am. Physic] (1994) 267:G663–G675.
  • KOPIN AS, LEE YM, McBRIDE EW et al.: Expression cloning and characterization of the canine parietal cell gastrin receptor. Proc. Natl. Acad. Sci. USA (1992) 89:3605–3609.
  • SOLL AH, AMIRIAN DA, THOMAS LP, REEDY TJ, ELASHOFF JD: Gastrin receptors on isolated canine parietal cells. Clin. Invest. (1984) 73:1434–1447.
  • NOBLE F, WANK SA, CRAWLEY JN et al.: International Union of Pharmacology. XXI. Structure, distribution, and functions of cholecystokinin receptors. Pharmacol Rev (1999) 51:745–781.
  • SAND VIK AK, WALDUM HL: CCK-B(gastrin) receptor regulates gastric histamine release and acid secretion. Am. Physic] (1991) 260:G925–G928.
  • CHEY WY, SIVASOMBOON B, HENDRICKS J: Actions and interactions of gut hormones and histamine on gastric secretion of acid in the rat. Am. J. Physic] (1973) 224:852–856.
  • •A key paper describing histamine and gastric acid secretion.
  • KAMINSKI DL, RUWART MJ, JELLINEK M: Structure-function relationships of peptide fragments of gastrin and cholecystokinin. Am. J. Physic] (1977) 233:E286–E292.
  • DELVALLE J, CHIBA T, PARK J, YAMADA T: Distinct receptors for cholecystokinin and gastrin on canine fundic D-cells. Am. J. Physic] (1993) 264:G811–G815.
  • NISHIDA A, MIYATA K, TSUTSUMI R et al.: Pharmacological profile of (A -1-12,3-dihydro-1-(2'-methylphenacy1)-2-oxo- 5-pheny1-1H-1,4-benzodiazepin-3-y11-3-(3-methylphenyOurea (YM022), a new potent and selective gastrin/ cholecystokinin-B receptor antagonist, in vitro and in vivo. J. Pharmacol. Exp. Ther. (1994) 269:725–731.
  • NISHIDA A, TAKINAMI Y, YUKI H et al: YM022 ag -1- (2, 3-dihydro- 1 - [2'-methylphenacy1]-2-oxo-5-phenyl-1H-1,4-benzodiazepin 3 yl) 3 [3 methylphenyl]urea), a potent and selective gastrin/cholecystokinin-B receptor antagonist, prevents gastric and duodenal lesions in rats. .1 Pharmacol. Exp. Ther. (1994) 270:1256–1261.
  • PENDLEY CE, FITZPATRICK LR, CAPOLINO AJ et al: RP 73870, a gastrin/cholecystokinin-B receptor antagonist with potent anti-ulcer activity in the rat../. Pharmacol. Exp. Ther. (1995) 273:1015–1022.
  • TAKEUCHI K, HIRATA T, YAMAMOTO H, KUNIKATA T, ISHIKAWA M, ISHIHARA Y: Effects of S-0509, a novel CCKB/gastrin receptor antagonist, on acid secretion and experimental duodenal ulcers in rats. Aliment. Pharmacol Ther. (1999) 13:87–96.
  • AMAGASE K, IKEDA K, OKABE S: Antisecretory and ulcer healing effects of S-0509, a novel CCK-B/gastrin receptor antagonist, in rats. Dig. Dis. Sci. (1999) 44:879–888.
  • STEEL K: Gastrin and gastrin receptor ligands - a review of recent patent literature. 'Drugs (2002) 5:689–695.
  • BELTINGER J, HILDEBRAND P, DREWE J et al.: Effects of spiroglumide, a gastrin receptor antagonist, on acid secretion in humans. Eur..1. Clin. Invest. (1999) 29:153–159.
  • BASTAKI SM, HASAN MY, CHANDRANATH SI, SCHMASSMANN A, GARNER A: PD-136450: a CCK2 (gastrin) receptor antagonist with antisecretory, anxiolytic and antiulcer activity. Mol. Cell Biochem. (2003) 252:83–90.
  • MAKOVEC F, D'AMATO M: CCKB/ gastrin receptor antagonists as potential drugs for peptic ulcer therapy. Drug Disco v. Today (1997) 7:283–293.
  • ••A key paper that provides an overview ofgastrin receptor antagonists.
  • MIURA N, YONETA T, UKAWA H et al.: Pharmacological Profiles of Z-360, a Novel CCK/Gastrin (CCK2) Receptor Antagonist with Excellent Oral Potency. Gastroenterology (2001) 120:A311 (Abstract).
  • MORITA H, MIURA N, HORI Y et al.: Effects of Z-360, a novel CCKB/gastrin (CCK2) receptor antagonist, on meal-induced acid secretion and experimental ulcer models in dogs and rats. Gastroenterology (2001) 120:A311 (Abstract).
  • MAKOVEC F, REVEL L, LETARI 0, MENNUNI L, IMPICCIATORE M: Characterization of antisecretory and antiulcer activity of CR 2945, a new potent and selective gastrin/CCK(B) receptor antagonist. Eur..1. Pharmacol (1999) 369:81–90.
  • BLACK JW, KALINDJIAN SB: Gastrin agonists and antagonists. Pharmacol Toxicol (2002) 91:275–281.
  • GANSER AL, FORTE JG: 1('-stimulated ATPase in purified microsomes of bullfrog oxyntic cells. Biochim. Biophys. Acta. (1973) 307:169–180.
  • ••A key paper that identified the HVI('-ATPase as the primary gastric enzyme of II' secretion.
  • METZ DC, FERRON GM, PAUL J et al: Proton pump activation in stimulated parietal cells is regulated by gastric acid secretory capacity: a human study. J. Clin. Pharmacol. (2002) 42:512–519.
  • YAO X, FORTE JG: Cell biology of acid secretion by the parietal cell. Ann. Rev Physic] (2003) 65:103–131.
  • •A key paper that summarises the progress made toward an understanding of the cell biology of gastric acid secretion.
  • GRAHAMMER F, HERLING AW, LANG HJ et al.: The cardiac K.* channel KCNQ1 is essential for gastric acid secretion. Gastroenterology (2001) 120:1363–1371.
  • DEDEK K, WALDEGGER S: Colocalization of KCNQl/KCNE channel subunits in the mouse gastrointestinal tract. Pllugers Arch. (2001) 442:896–902.
  • FUJITA A, HORIO Y, HIGASHI K et al:Specific localization of an inwardly rectifying K(') channel, Kir4.1, at the apical membrane of rat gastric parietal cells; its possible involvement in KO recycling for the H(1-K(1-pump. J. Physic] (2002) 540:85–92.
  • MALINOWSKA DH, SHERRY AM, TEWARI KP, CUPPOLETTI J: Gastric parietal cell secretory membrane contains PKA- and acid-activated Kir2.1 channels. Am. J. Physic] Cell. Physic] (2004) 286:C495–0506.
  • SHERRY AM, MALINOWSKA DH, MORRIS RE, CIRAOLO GM, CUPPOLETTI J: Localization of C1C-2 Cl-channels in rabbit gastric mucosa. Am. J. Physic] Cell. Physic] (2001) 280:C1599–C1606.
  • SAKAI H, OKADA Y, MORII M, TAKEGUCHI N: Anion and cation channels in the basolateral membrane of rabbit parietal cells. Pllugers. Arch. (1989) 414:185–192.
  • SUPPLISSON S, LOO DD, SACHS G: Diversity of K.' channels in the basolateral membrane of resting Necturus oxyntic cells. .1 Membr. Biol. (1991) 123:209–221.
  • POST RL, HEGYVARY C, KUME S: Activation by adenosine triphosphate in the phosphorylation kinetics of sodium and potassium ion transport adenosine triphosphatase. ./. Biol. Chem. (1972) 247:6530–6540.
  • ••A historic paper.
  • ALBERS R: Biochemical aspects of active transport. Ann. Rev Biochem. (1967) 36:727–756.
  • ••A historic paper.
  • KUHLBRANDT W: Biology, structure and mechanism of P-type ATPases. Nat. Rev Mol..Cell. Biol. (2004) 5:282–295.
  • •An elegant and recent review summarising the biology of ATPase.
  • WALLMARK B, STEWART HB, RABON E, SACCOMANI G, SACHS G. The catalytic cycle of gastric (H-11(1-ATPase. J. Biol. Chem. (1980) 255:5313–5319.
  • ••An important paper describing thereaction sequence of gastric
  • SWARTS HG, KLAASSEN CH, DE BOER M, FRANSEN JA, DE PONT JJ: Role of negatively charged residues in the fifth and sixth transmembrane domains of the catalytic subunit of gastric FP/K.'-ATPase../. Biol. Chem. (1996)271:29764–29772.
  • VAGIN 0, MUNSON K, LAMBRECHT N, KARLISH SJ, SACHS G: Mutational analysis of the K* competitive inhibitor site of gastric H/K-ATPase. Biochemistry (2001) 40:7480–7490.
  • ASANO S, TEGA Y, KONISHI K, FUJIOKA M, TAKEGUCHI N: Functional expression of gastric FIVIc(1-ATPase and site-directed mutagenesis of the putative cation binding site and catalytic center. J. Biol. Chem. (1996) 271:2740–2745.
  • KOENDERINK JB, SWARTS HG, WILLEMS PH, KRIEGER E, DE PONT JJ: A conformation-specific interhelical salt bridge in the K.' binding site of gastric H/K-ATPase. .1 Biol. Chem. (2004) 279:16417–16424.
  • KEELING DJ, LAING SM, SENN-BILFINGER J: SCH 28080 is a lumenally acting, K+-site inhibitor of the gastric (HV Kl-ATPase. Biochem. Pharmacol (1988) 37:2231–2236.
  • WALLMARK B, BRIVING C, FRYKLUND J et al.: Inhibition of gastric FIVIc+-ATPase and acid secretion by SCH 28080, a substituted pyridy1(1,2a)imidazole. J. Biol. Chem. (1987) 262:2077–2084.
  • VAGIN 0, DENEVICH S, MUNSON K, SACHS G: 5CH28080, a K*-competitive inhibitor of the gastric H/K-ATPase, binds near the M5-6 luminal loop, preventing K.' access to the ion binding domain. Biochemistry (2002) 41:12755–12762.
  • VAGIN 0, MUNSON K, DENEVICH S, SACHS G: Inhibition kinetics of the gastric H/K-ATPase by K-competitive inhibitor 5CH28080 as a tool for investigating the luminal ion pathway. Ann. NY Acad. Sci. (2003) 986:111–115.
  • KEELING DJ, TAYLOR AG, SCHUDT C: The binding of a K.+ competitive ligand, 2-methy1,8-(phenylmethoxy)imidazo(1,2-a)pyridine 3-acetonitrile, to the gastric (FIVIcl-ATPase. J. Biol. Chem. (1989)264:5545–5551.
  • ASANO S, YOSHIDA A, YASHIRO H et al.: The cavity structure for docking the KO-competitive inhibitors in the gastric proton pump. J. Biol. Chem. (2004)279:13968–13975.
  • BESANCON M, SIMON A, SACHS G, SHIN JM: Sites of reaction of the gastric H/K-ATPase with extracytoplasmic thiol reagents. .1 Biol. Chem. (1997) 272:22438–22446.
  • MORII M, TAKEGUCHI N: Different biochemical modes of action of two irreversible RiK(÷)-ATPase inhibitors, omeprazole and E3810. j. Biol. Chem. (1993) 268:21553–21559.
  • ENE MD, KHAN-DANESHMEND T, ROBERTS CJ: A study of the inhibitory effects of SCH 28080 on gastric secretion in man. BE J. Pharmacol (1982) 76:389–391.
  • MARTINEK J, BLUM AL, STOLTE M et al.: Effects of pumaprazole (BY841), a novel reversible proton pump antagonist, and of omeprazole, on intragastric acidity before and after cure of Helicobacter pylori infection. Aliment. Pharmacol Ther. (1999) 13:27–34.
  • POPE AJ, PARSONS ME: Reversible inhibitors of the gastric FT-A((0-transporting ATPase: a new class of anti-secretory agent. Trends Pharmacol Sri. (1993) 14:323–325.
  • PARKS, AHN B, LEE B, KANG H, SONG K: Pharmacokinetics of YH1885. Gut (2003) 52(Suppl. VI):IVION-G-008 (Abstract).
  • PARKS, LEES, SONG K, LEE B, KANG H, KANG J: The pharmacological properties of a novel acid pump antagonist, YH1885. Gut (2003)52(Suppl. VI):MON-G-009 (Abstract).
  • YU KS, BAE KS, SHON JH ET AL.: Pharmacokinetic and pharmacodynamic evaluation of a novel proton pump inhibitor, YH1885, in healthy volunteers. Pharmacol (2004) 44:73–82.
  • BRIVING C, SVENSSON K, MAXVALL I, ANDERSSON K: Mechanism of action of AZD-0865, an FIVIc+-ATPase selective, potassium-competitive acid blocker. Gastroenterology (2004) 126:A-333 (Abstract M1436).
  • HOLSTEIN B, HOLMBERG A, FLORENTZSON M, AURELL HOLMBERG A, ANDERSSON M, ANDERSSON K: AZD0865 - a new potassium-competitive acid blocker exhibits maximal gastric antisecretory effects from first dose. Gastroenterology (2004) 126:A-334 (Abstract M1437).
  • HOLSTEIN B, HOLMBERG A, FLORENTZSON M, AURELL HOLMBERG A, ANDERSSON M, ANDERSSON K: Pharmacokinetic and pharmacodynamic profiles of AZD0865, a novel, potassium-competitive acid blocker. Gastroenterology (2004) 126:A-334 (Abstract M1440).
  • ANDERSSON K, AURELL HOLMBERG A, BRIVING C, HOLSTEIN B: Preclinical profile of AZD0865, a novel, selective, potassium-competitive acid blocker. Gastroenterology (2004) 126:A-56 (Abstract 448).
  • HOLSTEIN, B, FLORENTZSON M, ANDERSSON M, ANDERSSON K: AZD-0865, a potassium-competitive acid blocker (P-CAB), has a long duration of effect in the rat. Am. Gastroenterol (2004) 99\(Suppl. 10):58 (Abstract 22).
  • ITO K, KINOSHITA K, TOMIZAWA A et al: The anti-secretory and anti-ulcer properties of R-105266, a novel acid pump antagonist. Gut (2001)49 (Suppl. III):(Abstract 3061).
  • POPE AJ, SACHS G: Reversible inhibitorsof the gastric (FIVIcl-ATPase as both potential therapeutic agents and probes of pump function. Biochem. Soc. Trans. (1992) 20:566–572.

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