Pharmacological Study of IQM-97,423, a Potent and Selective CCK1 Receptor Antagonist with Protective Effect in Experimental Acute Pancreatitis

@article{Latorre2004PharmacologicalSO,
  title={Pharmacological Study of IQM-97,423, a Potent and Selective CCK1 Receptor Antagonist with Protective Effect in Experimental Acute Pancreatitis},
  author={M. Latorre and J. Bartolom{\'e}-Nebreda and M. Garc{\'i}a-L{\'o}pez and R. Gonz{\'a}lez-Mu{\~n}iz and R. Herranz and J. del R{\'i}o and E. Cenarruzabeitia},
  journal={Pharmacology},
  year={2004},
  volume={72},
  pages={68 - 76}
}
The pharmacological profile of the new CCK1 receptor antagonist IQM-97,423, (4aS,5R)-2-benzyl-5-(tert-butylaminocarbonyl-tryptophyl)amino-1,3-dioxoperhydropyrido-[1,2-c]pyrimidine, was examined in in vitro and in vivo studies and compared with typical CCK1 antagonists such as devazepide and lorglumide. IQM-97,423 showed a high affinity at [3H]-pCCK8-labeled rat pancreatic CCK1 receptors, and was virtually devoid of affinity at brain CCK2 receptors. IQM-97,423 antagonized CCK8S-stimulated… Expand
6 Citations
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Importance of gut hormones in gastrointestinal, metabolic, and malignant diseases
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Understanding of the role of gastrin and cholecystokinin gene products in cancer has improved, and inhibitors of these peptides are likely to be useful as chemopreventive agents or as adjunctive therapeutics in cancer. Expand
Synthesis of 1,3-dioxo-hexahydropyrido[1,2-c][1,3]diazepine carboxylates, a new bicyclic skeleton formed by ring expansion-RCM methodology.
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References

SHOWING 1-10 OF 59 REFERENCES
Biochemical and pharmacological characterization of an extremely potent and selective nonpeptide cholecystokinin antagonist.
  • R. Chang, V. Lotti
  • Biology, Medicine
  • Proceedings of the National Academy of Sciences of the United States of America
  • 1986
TLDR
L-364,718 exhibited a very high selectivity for peripheral CCK receptors relative to brain CCK, gastrin, and various other peptide and nonpeptide receptors in both in vitro radioligand and isolated tissue assays. Expand
Pharmacological evaluation of IQM‐95,333, a highly selective CCKA receptor antagonist with anxiolytic‐like activity in animal models
TLDR
In conclusion, IQM‐95,333 is a potent and selective CCKA receptor antagonist both in vitro and in vivo with an anxiolytic‐like activity in two different animal models, which can only be attributed to blockade of this CCK receptor subtype. Expand
Characterization of a New Cholecystokinin Receptor Antagonist FK480 in in Vitro Isolated Rat Pancreatic Acini
TLDR
FK480 is a potent, competitive, and specific antagonist of CCK's stirnulatory action on the exocrine pancreas and appears to be bound to the receptors on acinar cells in a slowly dissociating state. Expand
Effect of T-0632, a cholecystokininA receptor antagonist, on experimental acute pancreatitis.
TLDR
T-0632 showed preventive effects on all of these pancreatitis models by oral or intraduodenal administration, and it is suggested that CCK plays an important role in progression and aggravation of acute pancreatitis, and T- 0632 may have a therapeutic value in these disease states. Expand
SR146131: a new potent, orally active, and selective nonpeptide cholecystokinin subtype 1 receptor agonist. I. In vitro studies.
TLDR
In conclusion, these in vitro experiments show that SR146131 is a highly potent and selective agonist of the CCK1 receptor. Expand
SR146131: a new potent, orally active, and selective nonpeptide cholecystokinin subtype 1 receptor agonist. II. In vivo pharmacological characterization.
TLDR
Pharmacodynamic studies suggest that SR146131 should have a high absolute bioavailability, and it may be a promising drug for the treatment of eating and motor disorders in humans. Expand
Pharmacological profile of T-0632, a novel potent and selective CCKA receptor antagonist, in vitro.
TLDR
It is suggested that T-0632 is a potent, reversible and more selective CCKA receptor antagonist compared with L-364,718 and loxiglumide. Expand
CCK-mediated response in the activation of 5-HT receptor types in the guinea-pig ileum.
TLDR
Results suggest that CCK is involved in the 5- HT-induced contractile response, particularly in the response induced by 5-HT4 receptor stimulation. Expand
Development of a class of selective cholecystokinin type B receptor antagonists having potent anxiolytic activity.
  • J. Hughes, P. Boden, +6 authors G. Woodruff
  • Chemistry, Medicine
  • Proceedings of the National Academy of Sciences of the United States of America
  • 1990
TLDR
Evidence is provided of a selective role for CCK-B receptors in the control of anxiety in mice previously made tolerant to diazepam and members of a class of anxiolytic agents that have a greatly improved profile compared with benzodiazepines or serotonin-related anxIOlytics. Expand
CCK-B receptor: chemistry, molecular biology, biochemistry and pharmacology
TLDR
The strategies followed to design these probes, and their use to study the anatomy of CCK pathways, the neurochemical and pharmacological properties of this peptide and the clinical perspectives offered by manipulation of the CCK system will be reported. Expand
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