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Chemical Compound Review

Lintitript     2-[2-[[4-(2-chlorophenyl)- 1,3-thiazol-2...

Synonyms: CHEMBL249973, AG-D-74148, ACMC-20engc, AC1L3TXG, SR-27897, ...
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Disease relevance of Lintitript

  • Administration of PD140548 (10 mg/kg, i.v.) and SR 27897B (0.6 mg/kg, i.v.) significantly inhibited the pressor effects of CCK (35 and 47%, respectively), whilst reversing the bradycardic responses to a tachycardia [1].
  • In this study in patients with advanced pancreatic cancer, we evaluated the use of fluorodeoxyglucose (FDG) PET compared with magnetic resonance imaging (MRI) in monitoring hormonal therapy using a highly selective, non-peptide CCK receptor antagonist (SR 27897B) [2].

High impact information on Lintitript

  • RSA phases were also re-established when the "alimentary" type of cholecystokinin receptors (CCKA) were blocked by selective antagonists such as L364,718 or SR27897 (1 mg/kg i.v.). The latter had better brain accessibility than L364,718 [3].
  • Under our conditions, SR-27897 increased plasma concentration of leptin both in fed and food-deprived rats [4].
  • Moreover, the competition data for SR27897, 2-NAP and YM220 were consistent with the interaction of these compounds at two binding sites [5].
  • 4. In competition studies, the low affinity of the CCKA receptor antagonists, L-364,718; SR27897 and 2-NAP, suggest that, under the assay conditions employed, [3H]-JB93182 (0.3 nM) does not label CCKA receptors in the rat cortex [6].
  • The aim of the present study was to investigate the effects of cholecystokinin (CCK) CCK(A) and CCKB receptor antagonists SR 27897 B, devazepide, L 365260 and PD 135158 (CAM 1028) on exploratory behaviour in the elevated zero-maze in the rat [7].

Biological context of Lintitript


Anatomical context of Lintitript

  • With increased interest in the pharmacology of cholecystokininA (CCKA) receptors, including their trophic and mitogenic effects, the actions of two new non-peptide CCKA receptor antagonists, PD140548 and SR 27897B, were investigated in a convenient model system, the rat isolated nodose ganglion [11].
  • Taken together, these findings support the notion that SR 27897 behaves as a potent CCK-A antagonist able to cross the blood brain barrier [9].

Associations of Lintitript with other chemical compounds

  • The excitatory response increased after administration of the cholecystokinin A (CCK(A)) receptor antagonists lorglumide (3x10(-6) M: +44.1%), devazepide (10(-8) M: +19.4%; 10(-7) M: +30.0%) and SR-27897 (10(-10) M: +21.8%, 10(-8) M: +47.0%, P<0.05, n=8) [12].
  • These binding sites were of the CCKA type, as demonstrated by the differential inhibition of the binding of [125I]CCK-8-S and CCK-8-S-induced 45Ca2+ efflux by the specific CCKA antagonist SR 27897 and the specific CCKB antagonist PD 134,308 [13].
  • Competition studies were also conducted using a number of previously well-characterized CCK-receptor selective ligands; JB93182, YF476, PD-134,308, SR27897, dexloxiglumide, L-365,260 and L-364,718 [14].
  • The potentiation of the NMDA response induced by these sigma ligands was abolished by the selective CCKA receptor antagonist SR 27897, but not by the CCKB antagonist Cl-988 [15].
  • The potency of the contraction induced by CCK-8, desulphated CCK-8, and gastrin-I, and the effect of the CCK-A (loxiglumide and SR 27897) and the CCK-B (YM022 and L-365 260) specific receptor antagonists were compared [16].

Gene context of Lintitript

  • Lintitript markedly increased postprandial plasma CCK release (P<0.001) while distinctly reducing postprandial PP levels (P<0.01) as compared to placebo [8].
  • SR 27897B (3 and 10 nM) caused 7.9- and 17.9-fold shifts in the CCK concentration-response curve and the apparent-log KB values for each concentration of antagonist were calculated to be 9.36 and 9.23 [11].
  • Acini were stimulated by sulfated gastrin in the presence of SR 27897 (1.8 microM), blocking endogenous CCKA receptors [17].
  • The activity of SR 27897, a potent and selective CCK-A vs CCK-B receptor antagonist (Ki = 0.2 nM on guinea-pig pancreas vs 2000 nM on rat brain) was studied on behavioural, electrophysiological and biochemical effects induced by peripheral or central injection of CCK-8S [9].
  • CCK-induced pancreatic secretion was abolished by SR 27897 (15 nmol kg-1 min-1, 55 min) and reduced by PD 135158 (0.15 nmol kg-1 min-1, 55 min) [18].

Analytical, diagnostic and therapeutic context of Lintitript

  • In summary, SR 27897 is a selective antagonist of CCKA receptors, is highly potent in animal models whatever the route of administration and has a long duration of action.(ABSTRACT TRUNCATED AT 250 WORDS)[10]
  • Gastric emptying was assessed in nine healthy male volunteers using a randomized, double blind, two-period crossover design with oral lintitript (15 mg 1 h prior to meal intake) or placebo on two different days [8].


  1. Effects of the CCK(A) receptor antagonists SR 27897B and PD140548 on baroreflex function in conscious rats. Bunting, M.W., Beart, P.M., Widdop, R.E. Eur. J. Pharmacol. (1997) [Pubmed]
  2. Monitoring of tumour glucose metabolism by PET in a phase I study evaluating hormonal therapy in advanced pancreatic cancer. Eckel, F., Lersch, C., Lippl, F., Schulte-Frohlinde, E., Schusdziarra, V., Helmberger, H., Neverve, J., Decker, M., Frank, R., Schwaiger, M., Weber, W. Scand. J. Gastroenterol. (2002) [Pubmed]
  3. Melatonin is involved in cholecystokinin-induced changes of ileal motility in rats. Bonouali-Pellissier, S. J. Pineal Res. (1994) [Pubmed]
  4. Regulation of leptin distribution between plasma and cerebrospinal fluid by cholecystokinin receptors. Cano, V., Ezquerra, L., Ramos, M.P., Ruiz-Gayo, M. Br. J. Pharmacol. (2003) [Pubmed]
  5. Pharmacological evidence for putative CCK(1) receptor heterogeneity in human colon smooth muscle. Morton, M.F., Harper, E.A., Tavares, I.A., Shankley, N.P. Br. J. Pharmacol. (2002) [Pubmed]
  6. Characterization of the binding of a novel radioligand to CCKB/gastrin receptors in membranes from rat cerebral cortex. Harper, E.A., Shankley, N.P., Black, J.W. Br. J. Pharmacol. (1999) [Pubmed]
  7. The effects of cholecystokinin A and B receptor antagonists on exploratory behaviour in the elevated zero-maze in rat. Matto, V., Harro, J., Allikmets, L. Neuropharmacology (1997) [Pubmed]
  8. Effect of lintitript, a new CCK-A receptor antagonist, on gastric emptying of a solid-liquid meal in humans. Kreiss, C., Schwizer, W., Borovicka, J., Jansen, J.B., Bouloux, C., Pignol, R., Bischof Delaloye, A., Fried, M. Regul. Pept. (1998) [Pubmed]
  9. Neurobehavioural effects of SR 27897, a selective cholecystokinin type A (CCK-A) receptor antagonist. Poncelet, M., Arnone, M., Heaulme, M., Gonalons, N., Gueudet, C., Santucci, V., Thurneyssen, O., Keane, P., Gully, D., Le Fur, G. Naunyn Schmiedebergs Arch. Pharmacol. (1993) [Pubmed]
  10. Peripheral biological activity of SR 27897: a new potent non-peptide antagonist of CCKA receptors. Gully, D., Fréhel, D., Marcy, C., Spinazzé, A., Lespy, L., Neliat, G., Maffrand, J.P., Le Fur, G. Eur. J. Pharmacol. (1993) [Pubmed]
  11. Electrophysiological studies of the cholecystokininA receptor antagonists SR27897B and PD140548 in the rat isolated nodose ganglion. Beart, P.M., Krstew, E., Widdop, R.E. Naunyn Schmiedebergs Arch. Pharmacol. (1996) [Pubmed]
  12. Endogenous CCK depresses contractile activity within the ascending myenteric reflex pathway of rat ileum. Storr, M., Sattler, D., Hahn, A., Schusdziarra, V., Allescher, H.D. Neuropharmacology (2003) [Pubmed]
  13. CCK-JMV-180 acts as an antagonist of the CCKA receptor in the human IMR-32 neuroblastoma cell line. Schaeffer, P., Prabonnaud, V., Roux, M., Gully, D., Herbert, J.M. FEBS Lett. (1994) [Pubmed]
  14. Pharmacological analysis of CCK2 receptors up-regulated using engineered transcription factors. Morton, M.F., Liu, P.Q., Reik, A., de la Rosa, R., Mendel, M., Li, X.Y., Case, C., Pabo, C., Moreno, V., Pyati, J., Shankley, N.P. Regul. Pept. (2005) [Pubmed]
  15. Electrophysiological evidence for the implication of cholecystokinin in the modulation of the N-methyl-D-aspartate response by sigma ligands in the rat CA3 dorsal hippocampus. Gronier, B., Debonnel, G. Naunyn Schmiedebergs Arch. Pharmacol. (1996) [Pubmed]
  16. Pharmacological and molecular characterization of muscular cholecystokinin receptors in the human lower oesophageal sphincter. González, A.A., Farré, R., Monés, J., Capellà, G., Clavé, P. Neurogastroenterol. Motil. (2000) [Pubmed]
  17. The CCKB/gastrin receptor is coupled to the regulation of enzyme secretion, protein synthesis and p70 S6 kinase activity in acinar cells from ElasCCKB transgenic mice. Desbois, C., Huërou-Luron, I.L., Dufresne, M., Estival, A., Clerc, P., Romé, V., Clemente, F., Guilloteau, P., Fourmy, D. Eur. J. Biochem. (1999) [Pubmed]
  18. Exogenous CCK and gastrin stimulate pancreatic exocrine secretion via CCK-A but also via CCK-B/gastrin receptors in the calf. Le Dréan, G., Le Huërou-Luron, I., Gestin, M., Desbois, C., Romé, V., Bernard, C., Dufresne, M., Moroder, L., Gully, D., Chayvialle, J.A., Fourmy, D., Guilloteau, P. Pflugers Arch. (1999) [Pubmed]
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