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PD 135158Cat. No. 2608 |
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Alternative Name: CAM 1028 Chemical Name: 4-[[(1R)-2-[[(2R)-3-(1H-Indol-3-yl)-2-methyl-1-oxo-2-[[[[(1S,2R,4S)-1,7,7-trimethylbicyclo[2.2.1]hept-2-yl]oxy]carbonyl]amino]propyl]amino]-1-phenylethyl]amino]-4-oxobutanoic acid |
Biological Activity
Potent and selective, nonpeptide CCK2 receptor antagonist (IC50 values are 2.8 and 1232 nM for CCK2 and CCK1 respectively) that displays negligible affinity at GABAA, benzodiazepine, substance P, neurotensin, opioid, bradykinin and 5-HT3 receptors (IC50 > 10 μM). Exhibits anxiolytic activity in elevated plus maze and social interaction tests and increases food intake in rats.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.
Dorre and Smith (1998) CholecystokininB receptor antagonist increases food intake in rats. Physiol.Behav. 65 11. PMID: 9811359.
Tsutsumi et al (1999) Suppression of conditioned fear by administration of CCKB receptor antagonist PD135158. Neuropeptides 33 483. PMID: 10657528.
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Keywords: PD 135158, supplier, Potent, selective, CCK2, antagonists, Cholecystokinin2, Receptors, PD135158, CAM1028
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