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Submit ReviewPD 135158
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% (HPLC)
Biological Activity for PD 135158
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 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 for PD 135158
| M. Wt | 616.76 |
| Formula | C35H44N4O6 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 130285-87-9 |
| PubChem ID | 44385784 |
| InChI Key | NNTPEWZUKRSTMM-CFHPNWNBSA-N |
| Smiles | C[C@](NC(OC3C4(C)CCC(C(C)4C)C3)=O)(C(NC[C@@H]([C@]5=CC=CC=C5)NC(CCC(O)=O)=O)=O)CC2=CNC1=CC=CC=C12 |
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.
Product Datasheets for PD 135158
References for PD 135158
References are publications that support the biological activity of the product.
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
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
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Keywords: PD 135158, PD 135158 supplier, Potent, selective, CCK2, antagonists, Cholecystokinin2, Receptors, PD135158, CAM1028, CAM, 1028, Receptor, 2608, Tocris Bioscience
Citations for PD 135158
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Literature in this Area
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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.