PD 135158

Key Product Details

Product Description

PD 135158 is a 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 GABA_A, 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.

Product Specifications for PD 135158

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for PD 135158

The following data is based on the product molecular weight 616.76.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.62 mL	8.11 mL	16.21 mL
5 mM	0.32 mL	1.62 mL	3.24 mL
10 mM	0.16 mL	0.81 mL	1.62 mL
50 mM	0.03 mL	0.16 mL	0.32 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Tsutsumi Suppression of conditioned fear by administration of CCKB receptor antagonist PD135158. Neuropeptides 1999 PMID: 10657528
• Hughes Development of a class of selective cholecystokinin type B receptor antagonists having potent anxiolytic activity. Proc.Natl.Acad.Sci.USA
• Dorre and Smith Cholecystokinin_B receptor antagonist increases food intake in rats. Physiol.Behav. 1998 PMID: 9811359

Product Documents for PD 135158