PD 135158
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
- 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
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