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| | PD 135158 Basic information |
| Product Name: | PD 135158 | | Synonyms: | PD 135158;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-oxobutanoicacid | | CAS: | 130325-35-8 | | MF: | C42H61N5O11 | | MW: | 811.97 | | EINECS: | | | Product Categories: | | | Mol File: | 130325-35-8.mol |  |
| | PD 135158 Chemical Properties |
| storage temp. | Store at +4°C | | solubility | <61.68mg/ml in DMSO |
| | PD 135158 Usage And Synthesis |
| Uses | PD 135158 (CAM 1028) is a selective CCKB receptor antagonist with an IC50 of 2.8 nM against mouse cortex CCKB. PD 135158 shows anxiolytic activity[1]. | | Biological Activity | Potent and selective, nonpeptide CCK 2 receptor antagonist (IC 50 values are 2.8 and 1232 nM for CCK 2 and CCK 1 respectively) that displays negligible affinity at GABA A , benzodiazepine, substance P, neurotensin, opioid, bradykinin and 5-HT 3 receptors (IC 50 > 10 μ M). Exhibits anxiolytic activity in elevated plus maze and social interaction tests and increases food intake in rats. | | in vivo | PD 135158 (CAM 1028; 0.001-0.1 mg/kg; s.c.; once) enhances latent inhibition in the rat and shows antipsychotic potential[2]. | Animal Model: | Male Sprague-Dawley rats, conditioned suppression of drinking procedure model[2] | | Dosage: | 0.001, 0. 01, and 0.1 mg/kg | | Administration: | 0.2 mL/kg SC 30 min before prexposure and conditioning | | Result: | Elicited a clear latent inhibition effect under conditions that did not lead to latent inhibition in control rats. |
| | IC 50 | CCKBR: 2.8 nM (IC50); CCKAR: 1232 nM (IC50) | | References | [1] Hughes J, et al. Development of a class of selective cholecystokinin type B receptor antagonists having potent anxiolytic activity. Proc Natl Acad Sci U S A. 1990 Sep;87(17):6728-32. DOI:10.1073/pnas.87.17.6728
[2] Gracey DJ, et al. PD-135,158, a cholecystokinin(B) antagonist, enhances latent inhibition in the rat. Pharmacol Biochem Behav. 2000 Mar;65(3):459-63. DOI:10.1016/s0091-3057(99)00227-0 |
| | PD 135158 Preparation Products And Raw materials |
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