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CI 988Cat. No. 2607 |
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Alternative Name: PD 134308 Chemical Name: 4-[[(1R)-2-[[(2R)-3-(1H-indol-3-yl)-2-methyl-1-oxo-2-[[(tricyclo[3.3.1.13,7]dec-2-yloxy)carbonyl]amino]propyl]amino]-1-phenylethyl]amino]-4-oxobutanoic acid |
Biological Activity
Potent and selective CCK2 (CCK-B) receptor antagonist that displays ~ 1600-fold selectivity over CCK1 receptors (IC50 values are 1.7 and 2717 nM for CCK2 and CCK1 respectively). Has negligible affinity at a range of other binding sites (IC50 > 10 μM). Exhibits anxiolytic activity following oral administration.Certificate of Analysis / Safety Data Sheet
References
Hughes et al (1990) Development of a class of selective cholecystokinin type B receptor antagonists having potent anxiolytic activity. Proc.Natl.Acad.Sci.USA 87 6728.
Moody et al (2001) CI-988 inhibits growth of small cell lung cancer cells. J.Pharmacol.Exp.Ther. 299 1154. PMID: 11714907.
Andre et al (2005) Involvement of cholecystokininergic systems in anxiety-induced hyperalgesia in male rats: behavioral and biochemical studies. J.Neurosci. 25 7896. PMID: 16135746.
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Keywords: CI 988, supplier, Potent, selective, CCK2, antagonists, Cholecystokinin2, Receptors, CI988, PD134308
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