PD 135158

Catalog # Availability Size / Price Qty
2608/10
2608/50
PD 135158 | CAS No. 130285-87-9 | CCK2 Receptor Antagonists
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Description: Potent and selective CCK2 antagonist
Alternative Names: 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

Purity: ≥98%

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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.

Technical Data

M.Wt:
616.76
Formula:
C35H44N4O6
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at +4°C
CAS No:
130285-87-9

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. CholecystokininB receptor antagonist increases food intake in rats.
    Dorre and Smith
    Physiol.Behav., 1998;65:11
  2. Suppression of conditioned fear by administration of CCKB receptor antagonist PD135158.
    Tsutsumi et al.
    Neuropeptides, 1999;33:483
  3. Development of a class of selective cholecystokinin type B receptor antagonists having potent anxiolytic activity.
    Hughes et al.
    Proc.Natl.Acad.Sci.USA, 1990;87:6728

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