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Chemical Compound Review

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

Synonyms: Lorglumide, Lorglumidum, CHEMBL24938, AGN-PC-00N9GI, SureCN149509, ...
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Disease relevance of Lorglumide

  • Feeding of cholestyramine significantly decreased survival from 25% to 0% in the CDE pancreatitis, and increased the magnitude of elevation of serum amylase levels and the extent of pancreatic necrosis in both models of pancreatitis; CCK-receptor blockade with CR-1409 completely abolished the adverse effects of cholestyramine [1].
  • The effects of bombesin on pancreatic growth and development of pancreatic lesions, except for adenomas, were not inhibited by lorglumide [2].
  • The effect of the CCK receptor antagonist CR 1409 on bile reflux pancreatitis in the opossum [3].
  • It may be concluded that dexloxiglumide, lorglumide, and amiglumide exhibit a promising therapeutic profile for biliary colic and other gastrointestinal disorders in which CCK1 receptors play important physiological roles [4].
  • In human gallbladders, the effect of lorglumide was also present (ED50 increased from 47 nM +/- 8 SEM, n = 16; to 300 nM +/- 10 SEM, n = 4) coexisting with a large inter-sample variation for CCK-OP ED50s and maximal contractions, most likely due to the histological changes of the wall in chronic cholecystitis [5].

Psychiatry related information on Lorglumide

  • Lorglumide pretreatment inhibited maternal behavior of LS vs SS group and potentiated the morphine-induced disruption of this behavior in all days of test (LM vs SM group) [6].

High impact information on Lorglumide

  • In contrast to the pancreas, binding of 125I-BH-CCK-8 to the gallbladder muscle was inhibited with high affinity by CCK-8 and lorglumide but was replaced to a small degree by gastrin and L365,260 [7].
  • The present study was undertaken to discriminate between the effects of cholecystokinin and bombesin and to establish the modulating properties of the specific cholecystokinin receptor antagonist CR-1409 on pancreatic carcinogenesis [8].
  • Apart from growth stimulation, PSBR also enhanced pancreatic exocrine function, as shown by ultrastructural evidence of an appreciable decrease in zymogen granules; CR-1409 also inhibited this functional effect of hypercholecystokininaemia [9].
  • In contrast, lorglumide significantly increased gastric acid secretion from 1.12 to 7.98 mmol/h during bombesin infusion and from 0.52 to 7.62 mmol/h during caerulein infusion [10].
  • The parent compound of this series (lorglumide) is the first nonpeptidic, potent and selective antagonist of the CCK-A receptor [11].

Biological context of Lorglumide

  • 5. The selective CCK(A) receptor antagonist, lorglumide, dose-dependently attenuated the amphetamine-induced inhibition of gastric emptying in male rats [12].
  • The concentration required for 50% inhibition (IC50) of cell growth by the amino acid-derived antagonists proglumide (3.5 x 10(-3) M), benzotript (1.8 x 10(-3) M), loxiglumide (1.1 x 10(-4) M) and lorglumide (6.7 x 10(-5) M) were of the same order and significantly correlated with their IC50 for inhibition of 125I-gastrin binding to AR4-2J cells [13].
  • In contrast, the cholecystokinin antagonist, lorglumide, caused only a slight inhibition of hexamethonium-resistant peristalsis [14].
  • Longitudinal muscle contractions induced by electrical field stimulation (with pulses delivered at 0.05 and 1 Hz in the absence, and at 5 Hz in the presence of atropine) were not or only slightly reduced by CR 1409 (0.4 microM) [15].
  • The cholecystokinin-1 receptor antagonist lorglumide inhibited food-induced down-regulation of melanin-concentrating hormone and melanin-concentrating hormone-1R [16].

Anatomical context of Lorglumide

  • Oocyte CCK receptors retained selectivity for CCK analogs (CCK8 greater than unsulfated CCK8 greater than CCK4) and were blocked by the specific CCK receptor antagonist CR 1409 [17].
  • The potency and selectivity of D,L-4-(3,4-dichloro-benzoyl-amino)-5-(dipentyl-amino)-5-oxo-pen tan oic acid (CR 1409) as a cholecystokinin (CCK) antagonist was investigated on motor responses of the longitudinal and circular muscles of the guinea-pig isolated ileum [15].
  • SR-48692 reduced the [(3)H]TC recovery rate by congruent with 50% and congruent with 24% in the duodenum and jejunum, respectively, whereas lorglumide had no effect [18].
  • To investigate the roles of endogenous NT and CCK, we administered [(3)H]TC into the rat duodenum or lower jejunum and tested the effect of the NT antagonist SR-48692 (2 nmol x kg(-1) x min(-1)) or CCK-A antagonist lorglumide (100 nmol x kg(-1) x min(-1)) [18].
  • 2. Pancreatic exocrine secretion was studied both in vitro (isolated and perfused pancreatic segments) and in vivo (anaesthetized animals with cannulation of the common bile duct) whereas the trophic effect was investigated after short-term (5 days) administration of the peptides and/or lorglumide [19].

Associations of Lorglumide with other chemical compounds


Gene context of Lorglumide

  • The inhibitory effects of CCK were completely antagonized by 1 ng PD 135-158, a selective CCKB receptor antagonist, but not by lorglumide (1 microgram), a selective CCKA receptor antagonist [25].
  • The effect of CCK in primates seems to derive from the presence of CCK receptors of the A-type on the pupillary sphincter muscle, and can be blocked by lorglumide [26].
  • CCK-8-evoked cationic current was antagonized by lorglumide, a selective CCK-A receptor antagonist [27].
  • In this report, we show that the intraperitoneal administration of a CCK-B receptor antagonist, PD135158 (0.1 mg/kg), but not a CCK-A receptor antagonist, lorglumide, inhibited hyperlocomotion [28].
  • The CCK-8S-induced Ca increases were blocked by the CCKB receptor antagonist PD135158 (100 nM) but not by the CCKA antagonist lorglumide (100 nM) [29].

Analytical, diagnostic and therapeutic context of Lorglumide


  1. Protective action of luminal bile salts in necrotizing acute pancreatitis in mice. Gomez, G., Townsend, C.M., Green, D.W., Rajaraman, S., Uchida, T., Greeley, G.H., Soloway, R.D., Thompson, J.C. J. Clin. Invest. (1990) [Pubmed]
  2. Effects of cholecystokinin and bombesin on development of azaserine-induced pancreatic tumours in rats: modulation by the cholecystokinin receptor antagonist lorglumide. Meijers, M., Appel, M.J., van Garderen-Hoetmer, A., Lamers, C.B., Rovati, L.C., Jansen, J.B., Woutersen, R.A. Carcinogenesis (1992) [Pubmed]
  3. The effect of the CCK receptor antagonist CR 1409 on bile reflux pancreatitis in the opossum. Larsen, F., Schlarman, D., Andrus, C.C., Kaminski, D.L. Pancreas (1991) [Pubmed]
  4. Effect of three nonpeptide cholecystokinin antagonists on human isolated gallbladder. Maselli, M.A., Piepoli, A.L., Pezzolla, F., Guerra, V., Caruso, M.L., Mennuni, L., Lorusso, D., Makovec, F. Dig. Dis. Sci. (2001) [Pubmed]
  5. The effect of a novel CCK-antagonist (lorglumide) on human and guinea pig gallbladder strips: a tensiometric study. Portincasa, P., Brandonisio, R., Di Ciaula, A., Maggi, V., Chiloiro, M., Palasciano, G. Boll. Soc. Ital. Biol. Sper. (1990) [Pubmed]
  6. Puerperal blockade of cholecystokinin (CCK1) receptors disrupts maternal behavior in lactating rats. Miranda-Paiva, C.M., Nasello, A.G., Yim, A.J., Felicio, L.F. J. Mol. Neurosci. (2002) [Pubmed]
  7. Cholecystokinin receptors in human pancreas and gallbladder muscle: a comparative study. Tang, C., Biemond, I., Lamers, C.B. Gastroenterology (1996) [Pubmed]
  8. Influence of cholecystokinin antagonist on the effects of cholecystokinin and bombesin on azaserine-induced lesions in rat pancreas. Douglas, B.R., Woutersen, R.A., Jansen, J.B., de Jong, A.J., Rovati, L.C., Lamers, C.B. Gastroenterology (1989) [Pubmed]
  9. Role of cholecystokinin in pancreatic adaptation to massive enterectomy. Watanapa, P., Egan, M., Deprez, P.H., Calam, J., Sarraf, C.E., Alison, M.R., Williamson, R.C. Gut (1992) [Pubmed]
  10. Effect of the cholecystokinin-receptor antagonist lorglumide on pancreatic enzyme secretion stimulated by bombesin, food, and caerulein, giving similar plasma cholecystokinin concentrations in the dog. de Jong, A.J., Singer, M.V., Jansen, J.B., Niebel, W., Rovati, L.C., Lamers, C.B. Gut (1991) [Pubmed]
  11. Structure-antigastrin activity relationships of new (R)-4-benzamido-5-oxopentanoic acid derivatives. Makovec, F., Peris, W., Revel, L., Giovanetti, R., Mennuni, L., Rovati, L.C. J. Med. Chem. (1992) [Pubmed]
  12. Inhibition of gastric emptying and intestinal transit by amphetamine through a mechanism involving an increased secretion of CCK in male rats. Doong, M.L., Lu, C.C., Kau, M.M., Tsai, S.C., Chiao, Y.C., Chen, J.J., Yeh, J.Y., Lin, H., Huang, S.W., Chen, T.S., Chang, F.Y., Wang, P.S. Br. J. Pharmacol. (1998) [Pubmed]
  13. Autocrine stimulation of growth of AR4-2J rat pancreatic tumour cells by gastrin. Blackmore, M., Hirst, B.H. Br. J. Cancer (1992) [Pubmed]
  14. Evidence for an involvement of substance P, but not cholecystokinin-like peptides, in hexamethonium-resistant intestinal peristalsis. Barthó, L., Holzer, P., Leander, S., Lembeck, F. Neuroscience (1989) [Pubmed]
  15. Evaluation of a new and potent cholecystokinin antagonist on motor responses of the guinea-pig intestine. Barthó, L., Holzer, P., Lembeck, F., Lippe, I.T., Setnikar, I. Br. J. Pharmacol. (1987) [Pubmed]
  16. Feeding-dependent depression of melanin-concentrating hormone and melanin-concentrating hormone receptor-1 expression in vagal afferent neurones. Burdyga, G., Varro, A., Dimaline, R., Thompson, D.G., Dockray, G.J. Neuroscience (2006) [Pubmed]
  17. Expression of receptors for cholecystokinin and other Ca2+-mobilizing hormones in Xenopus oocytes. Williams, J.A., McChesney, D.J., Calayag, M.C., Lingappa, V.R., Logsdon, C.D. Proc. Natl. Acad. Sci. U.S.A. (1988) [Pubmed]
  18. Endogenous neurotensin facilitates enterohepatic bile acid circulation by enhancing intestinal uptake in rats. Gui, X., Dobner, P.R., Carraway, R.E. Am. J. Physiol. Gastrointest. Liver Physiol. (2001) [Pubmed]
  19. Effect of a new potent CCK antagonist, lorglumide, on caerulein- and bombesin-induced pancreatic secretion and growth in the rat. Scarpignato, C., Varga, G., Dobronyi, I., Papp, M. Br. J. Pharmacol. (1989) [Pubmed]
  20. Modulation by CR-1409 (lorglumide), a cholecystokinin receptor antagonist, of trypsin inhibitor-enhanced growth of azaserine-induced putative preneoplastic lesions in rat pancreas. Douglas, B.R., Woutersen, R.A., Jansen, J.B., de Jong, A.J., Rovati, L.C., Lamers, C.B. Cancer Res. (1989) [Pubmed]
  21. 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]
  22. Functional comparisons of gastrin/cholecystokinin receptors in isolated preparations of gastric mucosa and ileum. Patel, M., Spraggs, C.F. Br. J. Pharmacol. (1992) [Pubmed]
  23. Cholecystokinin modulates neurotransmission through the dentate gyrus. Sinton, C.M. Neurosci. Lett. (1988) [Pubmed]
  24. Effects of evodiamine on gastrointestinal motility in male rats. Wu, C.L., Hung, C.R., Chang, F.Y., Lin, L.C., Pau, K.Y., Wang, P.S. Eur. J. Pharmacol. (2002) [Pubmed]
  25. The stimulation of cholecystokinin receptors in the rostral nucleus accumbens significantly antagonizes the EEG and behavioural effects induced by phencyclidine in rats. Popoli, P., Reggio, R., Pèzzola, A., Scotti de Carolis, A. Psychopharmacology (Berl.) (1995) [Pubmed]
  26. The 1990 Endre Balazs Lecture. Effects of some neuropeptides on the uvea. Anders, B. Exp. Eye Res. (1991) [Pubmed]
  27. CCK-8 excites substantia nigra dopaminergic neurons by increasing a cationic conductance. Wu, T., Wang, H.L. Neurosci. Lett. (1994) [Pubmed]
  28. Effects of cholecystokinin-B receptor antagonist on dopamine system in tenascin mutant mice. Fukamauchi, F., Wang, Y.J., Mataga, N., Kusakabe, M. Neuroreport (1997) [Pubmed]
  29. Cholecystokinin activates CCKB-receptor-mediated Ca-signaling in hippocampal astrocytes. Müller, W., Heinemann, U., Berlin, K. J. Neurophysiol. (1997) [Pubmed]
  30. Reversal of tolerance to the antitransit effects of morphine during acute intestinal inflammation in mice. Pol, O., Puig, M.M. Br. J. Pharmacol. (1997) [Pubmed]
  31. Cholecystokinin octapeptide increases spontaneous glutamatergic synaptic transmission to neurons of the nucleus tractus solitarius centralis. Baptista, V., Zheng, Z.L., Coleman, F.H., Rogers, R.C., Travagli, R.A. J. Neurophysiol. (2005) [Pubmed]
  32. Cholecystokinin antagonists proglumide, lorglumide and benzotript, but not L-364,718, interact with brain opioid binding sites. Gaudreau, P., Lavigne, G.J., Quirion, R. Neuropeptides (1990) [Pubmed]
  33. Role of endogenous secretin and cholecystokinin in intraduodenal oleic acid-induced inhibition of gastric acid secretion in rats. Shiratori, K., Watanabe, S., Takeuchi, T. Dig. Dis. Sci. (1992) [Pubmed]
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