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.
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 616.76. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|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|
References are publications that support the products' biological activity.
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
If you know of a relevant reference for PD 135158, please let us know.
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Keywords: PD 135158, supplier, Potent, selective, CCK2, antagonists, Cholecystokinin2, Receptors, PD135158, CAM1028, CAM, 1028, CCK2, Receptor, CCK2, Receptor, Tocris Bioscience
Citations for PD 135158
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Literature in this Area
Peptides Involved in Appetite Modulation Scientific Review
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.