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Chemical Compound Review

Loxizin     4-[(3,4- dichlorophenyl)carbonylamino]- 4-(3...

Synonyms: LOXIGLUMIDE, Loxiglumida, Loxiglumidum, CHEMBL206025, SureCN385563, ...
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Disease relevance of D01113


Psychiatry related information on D01113


High impact information on D01113

  • The present study was designed (a) to characterize the activity of loxiglumide as a peripheral cholecystokinin (CCK) antagonist in healthy human subjects, and (b) to determine whether CCK is a physiologic regulator of the intestinal phase of meal-stimulated exocrine pancreatic and biliary secretions in man [9].
  • Intravenous loxiglumide (22 mumol/kg per h) was highly potent in antagonizing CCK8-induced pancreatic enzyme and bile acid secretion as well as pancreatic polypeptide release [9].
  • A 12-carbon but not a 10-carbon-long chain fatty acid reduced antral contractile amplitude, an effect that was abolished by loxiglumide (a specific CCK-A receptor antagonist) [10].
  • Loxiglumide inhibited postprandial gallbladder emptying, reflux episodes, TLESRs, and time of pH of <4 and prevented the decrease in LES pressure induced by cholestyramine [11].
  • In other groups of rats, the effect of 10 nmol/kg PACAP-27 was studied under the influence of either atropine; loxiglumide, an antisecretin serum; a combination of both loxiglumide and the antiserum; or a PACAP antagonist (PACAP 6-38) [12].

Chemical compound and disease context of D01113


Biological context of D01113


Anatomical context of D01113


Associations of D01113 with other chemical compounds

  • The experiments were repeated under cholinergic (atropine) and cholecystokinin (loxiglumide) blockade [26].
  • Tests were undertaken with and without elimination of endogenous CCK by loxiglumide, a selective CCK-A receptors antagonist, before and after eradication of H pylori with triple therapy (omeprazole, amoxicyllin, bismuth) [27].
  • Cephalic phase stimulated by modified sham feeding in group A subjects increased gastric acid secretion to about 50% of pentagastrin maximum and the treatment with loxiglumide in a standard dose (20 mumol/kg iv loading dose plus infusion of 20 mumol/kg/h afterwards) failed to affect this secretion [28].
  • More speculative new drugs for IBS include cholecystokinin antagonists such as loxiglumide and the gonadotrophin-releasing hormone analogue, leuprorelin (leuprolide) [29].
  • 2. TP-680 showed approximately 2 and 22 times greater selectivity for peripheral CCKA receptors relative to brain CCK (CCKB) receptors than MK-329 and loxiglumide, respectively, when IC50 values for inhibition of [125I]-CCK-8 binding in isolated acini and cerebral cortex were compared [30].

Gene context of D01113

  • In 7 additional volunteers, the effect of cholestyramine was studied during intravenous perfusion of saline or the CCK-A receptor antagonist loxiglumide [11].
  • Meal-stimulated integrated incremental plasma PP concentrations were significantly suppressed (55-65% inhibition, P less than 0.01) by loxiglumide [31].
  • Loxiglumide inhibits cholecystokinin stimulated somatostatin secretion and simultaneously enhances gastric acid secretion in humans [32].
  • Administration of loxiglumide (1200 mg orally) caused a reduction in the postprandial intragastric pH and the two- to three-fold increase in plasma gastrin [33].
  • When loxiglumide was added, the acid responses to caerulein and GRP were further increased by 2-3 folds, attaining a peak similar to the p-gastrin maximum [34].

Analytical, diagnostic and therapeutic context of D01113


  1. Treatment of biliary colic with loxiglumide. Beglinger, C., Dill, S., Meyer, B., Werth, B., Adler, G. Lancet (1989) [Pubmed]
  2. Cholecystokinin's role in regulation of colonic motility in health and in irritable bowel syndrome. Niederau, C., Faber, S., Karaus, M. Gastroenterology (1992) [Pubmed]
  3. Cholecystokinin receptor antagonist, loxiglumide, inhibits invasiveness of human pancreatic cancer cell lines. Hirata, M., Itoh, M., Tsuchida, A., Ooishi, H., Hanada, K., Kajiyama, G. FEBS Lett. (1996) [Pubmed]
  4. Pharmacological profile of T-0632, a novel potent and selective CCKA receptor antagonist, in vivo. Taniguchi, H., Yazaki, N., Yomota, E., Shikano, T., Endo, T., Nagasaki, M. Eur. J. Pharmacol. (1996) [Pubmed]
  5. A cholecystokinin receptor antagonist, loxiglumide, stimulates biliary secretion in conscious rats. Watanabe, N., Otsuki, M. Eur. J. Pharmacol. (1994) [Pubmed]
  6. Role of circulating cholecystokinin in control of fat-induced inhibition of food intake in humans. Drewe, J., Gadient, A., Rovati, L.C., Beglinger, C. Gastroenterology (1992) [Pubmed]
  7. Effect of a low dose of intraduodenal fat on satiety in humans: studies using the type A cholecystokinin receptor antagonist loxiglumide. Lieverse, R.J., Jansen, J.B., Masclee, A.A., Rovati, L.C., Lamers, C.B. Gut (1994) [Pubmed]
  8. Loxiglumide Rotta research. Katschinski, M. IDrugs : the investigational drugs journal. (2002) [Pubmed]
  9. Effects of a cholecystokinin receptor antagonist on intestinal phase of pancreatic and biliary responses in man. Hildebrand, P., Beglinger, C., Gyr, K., Jansen, J.B., Rovati, L.C., Zuercher, M., Lamers, C.B., Setnikar, I., Stalder, G.A. J. Clin. Invest. (1990) [Pubmed]
  10. Fatty acid chain length determines cholecystokinin secretion and effect on human gastric motility. McLaughlin, J., Grazia Lucà, M., Jones, M.N., D'Amato, M., Dockray, G.J., Thompson, D.G. Gastroenterology (1999) [Pubmed]
  11. Endogenous cholecystokinin enhances postprandial gastroesophageal reflux in humans through extrasphincteric receptors. Clavé, P., González, A., Moreno, A., López, R., Farré, A., Cussó, X., D'Amato, M., Azpiroz, F., Lluís, F. Gastroenterology (1998) [Pubmed]
  12. Pituitary adenylate cyclase-activating peptide stimulates rat pancreatic secretion via secretin and cholecystokinin releases. Lee, S.T., Lee, K.Y., Li, P., Coy, D., Chang, T.M., Chey, W.Y. Gastroenterology (1998) [Pubmed]
  13. Pancreatic fluid hypersecretion in rats after acute pancreatitis. Czakó, L., Yamamoto, M., Otsuki, M. Dig. Dis. Sci. (1997) [Pubmed]
  14. Differential mode of action of high- and low-affinity CCK/gastrin receptor antagonists in growth inhibition of gastrin--responsive human gastric adenocarcinoma cells in vitro. Piontek, M.K., Hengels, K.J. Anticancer Res. (1993) [Pubmed]
  15. Involvement of endogenous cholecystokinin and somatostatin in gastroprotection induced by intraduodenal fat. Brzozowski, T., Konturek, P.C., Konturek, S.J., Kwiecién, S., Pajdo, R., Brzozowska, I., Hahn, E.G. J. Clin. Gastroenterol. (1998) [Pubmed]
  16. Therapeutic effects of loxiglumide on experimental acute pancreatitis using various models. Satake, K., Kimura, K., Saito, T. Digestion (1999) [Pubmed]
  17. Effect of a new cholecystokinin receptor antagonist loxiglumide on acute pancreatitis in two experimental animal models. Tani, S., Okabayashi, Y., Nakamura, T., Fujii, M., Itoh, H., Otsuki, M. Pancreas (1990) [Pubmed]
  18. Role of cholecystokinin in regulation of gastrointestinal motor functions. Meyer, B.M., Werth, B.A., Beglinger, C., Hildebrand, P., Jansen, J.B., Zach, D., Rovati, L.C., Stalder, G.A. Lancet (1989) [Pubmed]
  19. Effects of loxiglumide on gallbladder emptying in healthy volunteers. Niederau, C., Heintges, T., Rovati, L., Strohmeyer, G. Gastroenterology (1989) [Pubmed]
  20. Physiological role of cholecystokinin on postprandial insulin secretion and gastric meal emptying in man. Studies with the cholecystokinin receptor antagonist loxiglumide. Fried, M., Schwizer, W., Beglinger, C., Keller, U., Jansen, J.B., Lamers, C.B. Diabetologia (1991) [Pubmed]
  21. Opposite effects of cholestyramine and loxiglumide on gallbladder dynamics in humans. Palasciano, G., Portincasa, P., Belfiore, A., Baldassarre, G., Albano, O. Gastroenterology (1992) [Pubmed]
  22. Effect of loxiglumide on basal and gastrin- and bombesin-stimulated gastric acid and serum gastrin levels. Jebbink, M.C., Lamers, C.B., Mooy, D.M., Rovati, L.C., Jansen, J.B. Gastroenterology (1992) [Pubmed]
  23. Effects of cholecystokinin-receptor blockade on pancreatic and biliary function in healthy volunteers. Schwarzendrube, J., Niederau, M., Lüthen, R., Niederau, C. Gastroenterology (1991) [Pubmed]
  24. Lorglumide and loxiglumide inhibit gastrin-stimulated DNA synthesis in a rat tumoral acinar pancreatic cell line (AR42J). Seva, C., Scemama, J.L., Bastié, M.J., Pradayrol, L., Vaysse, N. Cancer Res. (1990) [Pubmed]
  25. Effect of a cholecystokinin antagonist on meal-stimulated insulin and pancreatic polypeptide release in humans. Hildebrand, P., Ensinck, J.W., Ketterer, S., Delco, F., Mossi, S., Bangerter, U., Beglinger, C. J. Clin. Endocrinol. Metab. (1991) [Pubmed]
  26. Effect of loxiglumide, a cholecystokinin antagonist, on pancreatic polypeptide release in humans. Meier, R., Hildebrand, P., Thumshirn, M., Albrecht, C., Studer, B., Gyr, K., Beglinger, C. Gastroenterology (1990) [Pubmed]
  27. Eradication of Helicobacter pylori restores the inhibitory effect of cholecystokinin on postprandial gastrin release in duodenal ulcer patients. Konturek, J.W., Gillessen, A., Konturek, S.J., Domschke, W. Gut (1995) [Pubmed]
  28. Cholecystokinin in the control of gastric acid secretion in man. Konturek, J.W., Stoll, R., Konturek, S.J., Domschke, W. Gut (1993) [Pubmed]
  29. New drugs in the management of the irritable bowel syndrome. Farthing, M.J. Drugs (1998) [Pubmed]
  30. Pharmacological profile of TP-680, a new cholecystokininA receptor antagonist. Akiyama, T., Tachibana, I., Hirohata, Y., Shirohara, H., Yamamoto, M., Otsuki, M. Br. J. Pharmacol. (1996) [Pubmed]
  31. Cholecystokinin receptor antagonist loxiglumide modulates plasma levels of gastro-entero-pancreatic hormones in man. Feedback control of cholecystokinin and gastrin secretion. Schmidt, W.E., Creutzfeldt, W., Höcker, M., Nustede, R., Choudhury, A.R., Schleser, A., Rovati, L.C., Fölsch, U.R. Eur. J. Clin. Invest. (1991) [Pubmed]
  32. Loxiglumide inhibits cholecystokinin stimulated somatostatin secretion and simultaneously enhances gastric acid secretion in humans. Verhulst, M.L., Gielkens, H.A., Hopman, W.P., van Schaik, A., Tangerman, A., Rovati, L.C., Jansen, J.B. Regul. Pept. (1994) [Pubmed]
  33. Cholecystokinin in the regulation of gastric acid and endocrine pancreatic secretion in humans. Konturek, J.W., Stoll, R., Gutwinska-Konturek, M., Konturek, S.J., Domschke, W. Scand. J. Gastroenterol. (1993) [Pubmed]
  34. Cholecystokinin in the control of gastric acid and plasma gastrin and somatostatin secretion in healthy subjects and duodenal ulcer patients before and after eradication of Helicobacter pylori. Konturek, J.W. J. Physiol. Pharmacol. (1994) [Pubmed]
  35. Role of cholecystokinin in the regulation of gastric emptying and pancreatic enzyme secretion in humans. Studies with the cholecystokinin-receptor antagonist loxiglumide. Fried, M., Erlacher, U., Schwizer, W., Löchner, C., Koerfer, J., Beglinger, C., Jansen, J.B., Lamers, C.B., Harder, F., Bischof-Delaloye, A. Gastroenterology (1991) [Pubmed]
  36. Satiety effects of the type A CCK receptor antagonist loxiglumide in lean and obese women. Lieverse, R.J., Masclee, A.A., Jansen, J.B., Rovati, L.C., Lamers, C.B. Biol. Psychiatry (1995) [Pubmed]
  37. Combined dose-ratio analysis of cholecystokinin receptor antagonists, devazepide, lorglumide and loxiglumide in the guinea-pig gall bladder. Bishop, L.A., Gerskowitch, V.P., Hull, R.A., Shankley, N.P., Black, J.W. Br. J. Pharmacol. (1992) [Pubmed]
  38. Involvement of cholecystokininA receptors in transient lower esophageal sphincter relaxations triggered by gastric distension. Boeckxstaens, G.E., Hirsch, D.P., Fakhry, N., Holloway, R.H., D'Amato, M., Tytgat, G.N. Am. J. Gastroenterol. (1998) [Pubmed]
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