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Chemical Compound Review

YM-11170     3-[[2- (diaminomethylideneamino)- 1,3...

Synonyms: Pepcidac, Famotidina, Gastro, Famotidinum, Prestwick_212, ...
 
 
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Disease relevance of MK 208

  • Familial multiple endocrine neoplasia type 1 (FMEN1) is an autosomal dominant trait characterized by tumors of the parathyroids, gastro-intestinal endocrine tissue, anterior pituitary and other tissues [1].
  • Toxic side effects, i.e., damage to the gastro-intestinal tract and hemorrhages in the lungs, were more pronounced with full dose either in the single or the split daily dose regimen [2].
  • Aortoesophageal fistula (AEF) is a relatively rare but life-threatening cause of upper gastro-intestinal bleeding [3].
  • RESULTS OF DATA SYNTHESIS: A high incidence of lymphoma primarily in the gastro-intestinal tract in Third World countries has stimulated enormous epidemiologic and pathogenetic interests globally [4].
  • The efficacy and safety of prazosin GITS (gastro-intestinal therapeutic system), a new extended-release once-a-day formulation, were assessed both as monotherapy in mild essential hypertension and in combination with a diuretic in moderate essential hypertension in two multicenter, double-blind, placebo-controlled trials [5].
 

Psychiatry related information on MK 208

  • We compared the outcomes of PO and IV DEX administration because of individual differences in gastro-intestinal absorption of DEX and the issue of noncompliance in patients undergoing the dexamethasone suppression test (DST) [6].
  • Fluvoxamine provided a good clinical efficacy for six of these patients, whereas the other ten had to discontinue the drug because of the presence of severe adverse effects such as acute total insomnia, gastro-intestinal disturbances together with anorexia, aggressive and impulsive behavior and excessive sedation [7].
  • Dietary habits and gastro-intestinal cancers: a comparative case-control study of stomach and large intestinal cancers in Nagoya, Japan [8].
  • Physical activity potentially encourages a healthy lifestyle, and it could have more direct effects on certain forms of carcinogenesis (for instance, by a speeding of gastro-intestinal transit, or a moderation of sex hormone levels) [9].
  • Geophagia was postulated to occur in animals who experience a generalized stress reponse since this state may involve gastro-intestinal malaise [10].
 

High impact information on MK 208

 

Chemical compound and disease context of MK 208

 

Biological context of MK 208

  • The results of this study show interspecies and organ differences between calmodulin binding proteins, but suggest that a 67 kDa protein is the major binding protein present throughout normal gastro-intestinal tract and neoplastic human tissue [21].
  • AIMS: The aim was to investigate the effects of biliary obstruction and isolated external biliary diversion on gastro-intestinal structure and caecal bacterial flora in relation to bacterial translocation [22].
  • The DCC tumor suppressor gene has been shown to be frequently deleted or its expression reduced or absent in colorectal, gastro-intestinal, pancreatic, prostatic, and breast carcinomas, and glioblastomas [23].
  • The aim of this study was to investigate gastro-intestinal protein loss in adults with congenital heart disease, both with and without Fontan surgery, and to correlate findings with systemic venous pressure [24].
  • The human pathogen Vibrio cholerae employs such an assembly, called the Eps system, for the export of its major virulence factor, cholera toxin, from its periplasm into the lumen of the gastro-intestinal tract of the host [25].
 

Anatomical context of MK 208

 

Associations of MK 208 with other chemical compounds

  • Published data have indicated that metoclopramide assists radiological identification of lesions in the small intestine, facilitates duodenal intubation and small intestine biopsy, and eases emergency endoscopy in upper gastro-intestinal haemorrhage [31].
  • The inducible COX-2 enzyme is responsible for some aspects of pain and inflammation in arthritis while the constitutive COX-1 enzyme appears responsible for most of the gastro-protective prostaglandin synthesis in the stomach and duodenum [32].
  • In most instances, increasing the rate of gastric emptying and gastro-intestinal motility increases the rate of absorption of a drug but, for digoxin and riboflavin, increased gastrointestinal motility is associated with a decrease in the rate of absorption [33].
  • We conclude that intravenous famotidine can maintain intragastric pH greater than 6 in fasting patients with acute upper gastro-intestinal bleeding from peptic ulceration [34].
  • Outcome of patients with advanced gastro-intestinal stromal tumours crossing over to a daily imatinib dose of 800 mg after progression on 400 mg [35].
 

Gene context of MK 208

 

Analytical, diagnostic and therapeutic context of MK 208

References

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  2. Acetyldinaline: a new oral cytostatic drug with impressive differential activity against leukemic cells and normal stem cells--preclinical studies in a relevant rat model for human acute myelocytic leukemia. el-Beltagi, H.M., Martens, A.C., Lelieveld, P., Haroun, E.A., Hagenbeek, A. Cancer Res. (1993) [Pubmed]
  3. Aortoesophageal fistula: a comprehensive review of the literature. Hollander, J.E., Quick, G. Am. J. Med. (1991) [Pubmed]
  4. Immunoproliferative small intestinal disease: portrait of a potentially preventable cancer from the Third World. Khojasteh, A., Haghighi, P. Am. J. Med. (1990) [Pubmed]
  5. Efficacy and safety of Minipress XL, a new once-a-day formulation of prazosin. Singleton, W., Dix, R.K., Monsen, L., Moisey, D., Levenstein, M., Bottiglieri, D.F., Silver, L. Am. J. Med. (1989) [Pubmed]
  6. Effects of intravenous and oral dexamethasone on selected lymphocyte subpopulations in normal subjects. Chiappelli, F., Gormley, G.J., Gwirstman, H.E., Lowy, M.T., Nguyen, L.D., Nguyen, L., Esmail, I., Strober, M., Weiner, H. Psychoneuroendocrinology (1992) [Pubmed]
  7. Notes on the use of fluvoxamine as treatment of depression in HIV-1-infected subjects. Grassi, B., Gambini, O., Scarone, S. Pharmacopsychiatry (1995) [Pubmed]
  8. Dietary habits and gastro-intestinal cancers: a comparative case-control study of stomach and large intestinal cancers in Nagoya, Japan. Tajima, K., Tominaga, S. Jpn. J. Cancer Res. (1985) [Pubmed]
  9. Physical activity and cancer. Shephard, R.J. International journal of sports medicine. (1990) [Pubmed]
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  11. Selective effects of somatostatin-14, -25 and -28 on in vitro insulin and glucagon secretion. Mandarino, L., Stenner, D., Blanchard, W., Nissen, S., Gerich, J., Ling, N., Brazeau, P., Bohlen, P., Esch, F., Guillemin, R. Nature (1981) [Pubmed]
  12. Ingested mineral fibers: elimination in human urine. Cook, P.M., Olson, G.F. Science (1979) [Pubmed]
  13. Dramatic increase in the numbers of functionally mature dendritic cells in Flt3 ligand-treated mice: multiple dendritic cell subpopulations identified. Maraskovsky, E., Brasel, K., Teepe, M., Roux, E.R., Lyman, S.D., Shortman, K., McKenna, H.J. J. Exp. Med. (1996) [Pubmed]
  14. Bacterial toxin interaction with the developing intestine. Chu, S.H., Walker, W.A. Gastroenterology (1993) [Pubmed]
  15. Frameshift mutations in Fas, Apaf-1, and Bcl-10 in gastro-intestinal cancer of the microsatellite mutator phenotype. Yamamoto, H., Gil, J., Schwartz, S., Perucho, M. Cell Death Differ. (2000) [Pubmed]
  16. Reactive oxygen species-induced gastric ulceration: protection by melatonin. Bandyopadhyay, D., Chattopadhyay, A. Current medicinal chemistry. (2006) [Pubmed]
  17. Gastric Helicobacter infection inhibits development of oral tolerance to food antigens in mice. Matysiak-Budnik, T., van Niel, G., Mégraud, F., Mayo, K., Bevilacqua, C., Gaboriau-Routhiau, V., Moreau, M.C., Heyman, M. Infect. Immun. (2003) [Pubmed]
  18. Treatment with tranexamic acid during pregnancy, and the risk of thrombo-embolic complications. Lindoff, C., Rybo, G., Astedt, B. Thromb. Haemost. (1993) [Pubmed]
  19. Decreased toxicity and increased efficacy of cancer chemotherapy using the pineal hormone melatonin in metastatic solid tumour patients with poor clinical status. Lissoni, P., Barni, S., Mandalà, M., Ardizzoia, A., Paolorossi, F., Vaghi, M., Longarini, R., Malugani, F., Tancini, G. Eur. J. Cancer (1999) [Pubmed]
  20. Opposite effects of flurbiprofen and the nitroxybutyl ester of flurbiprofen on apoptosis in cultured guinea-pig gastric mucous cells. Johal, K., Hanson, P.J. Br. J. Pharmacol. (2000) [Pubmed]
  21. Interspecies comparison of calmodulin binding proteins throughout the gastrointestinal tract: comparison with human colon adenomas and adenocarcinomas. McGarrity, T.J., Peiffer, L.P., Billingsley, M.L. Gut (1991) [Pubmed]
  22. Role of the gut in the pathophysiology of extrahepatic biliary obstruction. Clements, W.D., Parks, R., Erwin, P., Halliday, M.I., Barr, J., Rowlands, B.J. Gut (1996) [Pubmed]
  23. Frequent allelic deletions and loss of expression characterize the DCC gene in male germ cell tumors. Murty, V.V., Li, R.G., Houldsworth, J., Bronson, D.L., Reuter, V.E., Bosl, G.J., Chaganti, R.S. Oncogene (1994) [Pubmed]
  24. Gastro-intestinal protein loss in late survivors of Fontan surgery and other congenital heart disease. Thorne, S.A., Hooper, J., Kemp, M., Somerville, J. Eur. Heart J. (1998) [Pubmed]
  25. The structure of the cytoplasmic domain of EpsL, an inner membrane component of the type II secretion system of Vibrio cholerae: an unusual member of the actin-like ATPase superfamily. Abendroth, J., Bagdasarian, M., Sandkvist, M., Hol, W.G. J. Mol. Biol. (2004) [Pubmed]
  26. The epidermal growth factor receptor (EGF-R) is present on the basolateral, but not the apical, surface of enterocytes in the human gastrointestinal tract. Playford, R.J., Hanby, A.M., Gschmeissner, S., Peiffer, L.P., Wright, N.A., McGarrity, T. Gut (1996) [Pubmed]
  27. Expression of the HER-2/neu proto-oncogene in normal human adult and fetal tissues. Press, M.F., Cordon-Cardo, C., Slamon, D.J. Oncogene (1990) [Pubmed]
  28. The proto-oncogene RON is involved in development of epithelial, bone and neuro-endocrine tissues. Gaudino, G., Avantaggiato, V., Follenzi, A., Acampora, D., Simeone, A., Comoglio, P.M. Oncogene (1995) [Pubmed]
  29. Recent advances in the chemistry of cholecystokinin receptor ligands (agonists and antagonists). de Tullio, P., Delarge, J., Pirotte, B. Current medicinal chemistry. (1999) [Pubmed]
  30. Peritoneal cell responses to acute gastro-intestinal inflammation. Steer, H.W., Lewis, D.A. J. Pathol. (1983) [Pubmed]
  31. Metoclopramide: a review of its pharmacological properties and clinical use. Pinder, R.M., Brogden, R.N., Sawyer, P.R., Speight, T.M., Avery, G.S. Drugs (1976) [Pubmed]
  32. COX-2 selective nonsteroidal anti-Inflammatory drugs: do they really offer any advantages? Jackson, L.M., Hawkey, C.J. Drugs (2000) [Pubmed]
  33. Drugs, diseases and altered gastric emptying. Nimmo, W.S. Clinical pharmacokinetics. (1976) [Pubmed]
  34. Controlled study of the effects of intravenous famotidine on intragastric pH in bleeding peptic ulcers. Fullarton, G.M., Macdonald, A.M., Mann, S.G., McColl, K.E. Aliment. Pharmacol. Ther. (1991) [Pubmed]
  35. Outcome of patients with advanced gastro-intestinal stromal tumours crossing over to a daily imatinib dose of 800 mg after progression on 400 mg. Zalcberg, J.R., Verweij, J., Casali, P.G., Le Cesne, A., Reichardt, P., Blay, J.Y., Schlemmer, M., Van Glabbeke, M., Brown, M., Judson, I.R. Eur. J. Cancer (2005) [Pubmed]
  36. Gastro-intestinal tumorigenesis in Smad4 mutant mice. Taketo, M.M., Takaku, K. Cytokine Growth Factor Rev. (2000) [Pubmed]
  37. Transforming growth factor-alpha-mediated growth pathways in human gastro-intestinal cell lines in relation to the gastrin autocrine pathway. Watson, S.A., Robinson, K.E., McWilliams, D., Michaeli, D., Smith, A.M., Robinson, G. Int. J. Cancer (2000) [Pubmed]
  38. Expression of beta 1-integrins, H-CAM (CD44) and LECAM-1 in primary gastro-intestinal B-cell lymphomas as compared to the adhesion receptor profile of the gut-associated lymphoid system, tonsil and peripheral lymph node. Möller, P., Eichelmann, A., Mechtersheimer, G., Koretz, K. Int. J. Cancer (1991) [Pubmed]
  39. Effects of inhibition of prostaglandin endoperoxide synthase-2 in chronic gastro-intestinal ulcer models in rats. Schmassmann, A., Peskar, B.M., Stettler, C., Netzer, P., Stroff, T., Flogerzi, B., Halter, F. Br. J. Pharmacol. (1998) [Pubmed]
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  41. Recurrent gastrointestinal bleeding associated with chronic pancreatitis. Jenkins, A.P., el-Omar, M.M., Booth, J.C., Banerjee, A.K., Burnand, K.G., Thompson, R.P. Gut (1995) [Pubmed]
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  44. Multifactorial analysis of parameters influencing chemosensitivity of human cancer xenografts in nude mice. Fujita, F., Fujita, M., Taguchi, T., Shimozuma, K., Sakamoto, Y., Kimoto, Y., Hirai, T. Int. J. Cancer (1989) [Pubmed]
  45. Gastrectomy induces impaired insulin and glucagon secretion: evidence for a gastro-insular axis in mice. Salehi, A., Chen, D., Håkanson, R., Nordin, G., Lundquist, I. J. Physiol. (Lond.) (1999) [Pubmed]
 
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