PD 135158
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.
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- CAS No.: 130325-35-8
- Formule: C42H61N5O11
- Masse moléculaire:811.96
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
CCKBR 2.8 nM (IC50) |
CCKAR 1232 nM (IC50) |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats, conditioned suppression of drinking procedure model[2]
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Dosage:0.001, 0. 01, and 0.1 mg/kg
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Administration:0.2 mL/kg SC 30 min before prexposure and conditioning
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Result:Elicited a clear latent inhibition effect under conditions that did not lead to latent inhibition in control rats.
Chemical Information
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CAS No. 130325-35-8
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Masse moléculaire 811.96
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Formule C42H61N5O11
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SMILES
C[C@@](C1(C)C)(CC[C@@]1([H])C2)[C@@H]2OC(N[C@](C(NC[C@@H](C3=CC=CC=C3)NC(CCC(O)=O)=O)=O)(C)CC4=CNC5=CC=CC=C45)=O.O[C@H]([C@@H](O)CNC)[C@H](O)[C@H](O)CO
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Synonyms
CAM 1028
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Protocol for Elevated Plus Maze Test
The Elevated Plus Maze is a rodent anxiety-like behavior assay based on the conflict between spontaneous exploration and avoidance of open, elevated, exposed spaces. The apparatus contains two open arms and two closed arms arranged in a plus shape, and rodents normally spend more time in closed arms than open arms. The assay readout is generated by recording arm entries, time spent in open and closed arms, and related exploratory behaviors. Increased open-arm time or open-arm entries is commonly interpreted as reduced anxiety-like behavior, whereas reduced open-arm exploration is interpreted as increased anxiety-like behavior.
Pureté et documentation
Références
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PD 135158 Related Classifications
HY-129810 Related Classifications
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