Ro4491533
Ro4491533 is a selective, negative allosteric mGluR2/3 receptor modulator that is equally effective on both subtypes. Ro4491533 can completely block glutamate-induced calcium mobilization and glutamate-induced [35S]GTPγS binding accumulation. Ro4491533 has good pharmacokinetic properties in mice and rats, high oral bioavailability, and can pass through the blood-brain barrier. Ro4491533 can also reverse the motor inhibition effect of LY379268 in mice and show antidepressant activity in the forced swim test and tail suspension test.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: 579482-31-8
- 分子式: C24H20F3N3O
- 分子量:423.43
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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
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
<0.01 μM
Compound: 7am
|
Antagonist activity at rat mGluR2 receptor expressed in CHO cells assessed as inhibition of GIRK current
Antagonist activity at rat mGluR2 receptor expressed in CHO cells assessed as inhibition of GIRK current
|
[PMID: 20971004] |
| CHO | IC50 |
<0.01 μM
Compound: 7am
|
Antagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK current
Antagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK current
|
[PMID: 20971004] |
| CHO | IC50 |
0.003 μM
Compound: 7am
|
Antagonist activity at recombinant rat mGluR2 expressed in forskolin-stimulated CHO cells assessed as inhibition of (1S,3R)-ACPD induced cAMP production
Antagonist activity at recombinant rat mGluR2 expressed in forskolin-stimulated CHO cells assessed as inhibition of (1S,3R)-ACPD induced cAMP production
|
[PMID: 20971004] |
| CHO | IC50 |
0.014 μM
Compound: 7am
|
Antagonist activity at human mGluR2 receptor expressed in CHO cells assessed as inhibition of GIRK current
Antagonist activity at human mGluR2 receptor expressed in CHO cells assessed as inhibition of GIRK current
|
[PMID: 20971004] |
化学情報
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CAS 番号 579482-31-8
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分子量 423.43
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分子式 C24H20F3N3O
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SMILES
O=C1NC2=CC(C(F)(F)F)=C(C=C2N=C(C1)C3=CC=CC(C4=CC(C)=NC(C)=C4)=C3)C
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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 Tail Suspension Test (TST)
The Tail Suspension Test is a mouse behavioral assay in which an animal is suspended by the tail in an inescapable position, causing alternating escape-directed activity and immobility; the main readout is immobility time, and antidepressant-like treatments generally reduce immobility compared with vehicle controls. The assay detects behavioral response to acute inescapable stress rather than a molecular event; immobility is interpreted as passive stress-coping behavior, while reduced immobility is used as a predictive screen for antidepressant-like activity, with important limitations related to strain, locomotor activity, and tail-climbing behavior.
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Protocol for Pharmacokinetic Study
Pharmacokinetic studies quantify how an organism handles a drug over time through absorption, distribution, metabolism, and excretion, and the core experimental readout is the concentration-time profile of parent drug and, when relevant, metabolites in biological matrices such as plasma, whole blood, urine, bile, or tissue. Pharmacokinetic analysis links dose, route, exposure, clearance, half-life, distribution, bioavailability, and systemic exposure to drug efficacy and toxicity hypotheses rather than measuring a signaling pathway directly. The literature links pharmacokinetics to drug-development phenotypes by showing that drug metabolism and pharmacokinetics influence compound progression, exposure-response interpretation, safety margins, dosing strategy, and failure risk during discovery and development. DMPK science contributes to compound optimization by integrating physicochemical properties, in vitro metabolism, transporter behavior, in vivo exposure, and pharmacodynamic contex
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Protocol for Forced Swim Test (FST)
The Forced Swim Test is a rodent behavioral assay in which a mouse or rat is placed in an inescapable cylinder of water, and the main readout is the time spent immobile versus active escape-related behaviors such as swimming or climbing. Reduced immobility after treatment has historically been interpreted as antidepressant-like activity, but the assay should be interpreted as a behavioral response to acute inescapable stress rather than a complete model of human depression.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)