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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 130325-35-8
- 分子式: C42H61N5O11
- 分子量:811.96
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[1]|
CCKBR 2.8 nM (IC50) |
CCKAR 1232 nM (IC50) |
体内実験
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.
化学情報
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CAS 番号 130325-35-8
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分子量 811.96
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分子式 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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別名
CAM 1028
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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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.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)