AZD-8418
AZD-8418 is an orally active positive allosteric modulator of metabotropic glutamate receptor 2 (mGluR2), with an EC50 of 0.86 μM for rat mGlu2 receptors. AZD-8418 reduces the in vitro binding level of [3H]AZ12559322 in prefrontal cortex brain tissues of non-human primates. AZD8418 enhances the inhibitory effect of the mGlu2/3 agonist DCG-IV (HY-101335) on field excitatory postsynaptic potentials (fEPSP) in rat hippocampal brain slices. AZD-8418 reduces nicotine self-administration behavior in rats, and blocks cue-induced reinstatement of nicotine-seeking and food-seeking behaviors. The attenuating effect on nicotine self-administration behavior develops rapid tolerance, while inhibition of food self-administration behavior requires chronic administration. AZD-8418 can be used in research related to nicotine dependence and neuropsychiatric disorders.
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: 1198309-73-7
- 分子式: C19H20ClN3O3
- 分子量:373.84
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
[2]|
rat mGluR2 0.86 μM (EC50) |
体外実験
AZD-8418 (5 μM; 30 min) potently binds to [3H]AZ12559322 at metabotropic glutamate receptor 2 in tissue sections of cynomolgus monkey prefrontal cortex, reducing signal intensity by approximately 40-45%[1].
AZD-8418 acts as a positive allosteric modulator of mGlu2 receptors in in vitro experiments using rat hippocampal CA1 brain slices. It potentiates DCG-IV-induced inhibition of fEPSP, with an EC50 value of 0.86 μM, and exhibits no intrinsic agonist activity[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
体内実験
AZD8418 (3.73-14.92 mg/kg/day; p.o.; for 14 consecutive days) produces a dose-dependent reduction in nicotine self-administration behavior in rats at the initial stage of administration, but tolerance develops rapidly; the highest dose also inhibits food self-administration, and this effect has a delayed onset[2].
AZD-8418 (1.12-14.92 mg/kg; p.o.; single administration) completely blocks cue-induced relapse of nicotine-seeking behavior in rats at all tested doses, and also blocks cue-induced food-seeking behavior[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar (male, 300-350 g at study start, trained to self-administer nicotine intravenously via jugular catheter under an FR5 TO20-s schedule)[2]
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Dosage:0.37 mg/kg; 1.12 mg/kg; 3.73 mg/kg; 7.46 mg/kg; 14.92 mg/kg
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Administration:p.o.; single dose
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Result:Dose-dependently inhibited nicotine self-administration.
Significantly inhibited nicotine infusions earned at 3.73 mg/kg, 7.46 mg/kg, and 14.92 mg/kg.
Significantly inhibited active lever presses at 7.46 mg/kg and 14.92 mg/kg.
Showed no effect on inactive lever presses.
Showed no significant effects on food self-administration at any tested dose.
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Animal Model:Wistar (male, 300-350 g at study start, trained to self-administer nicotine intravenously via jugular catheter under an FR5 TO20-s schedule)[2]
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Dosage:3.73 mg/kg/day; 7.46 mg/kg/day; 14.92 mg/kg/day
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Administration:p.o.; daily; 14 days
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Result:Significantly attenuated nicotine self-administration.
Significantly decreased nicotine intake at 3.73 mg/kg, 7.46 mg/kg, and 14.92 mg/kg on day 1; at 14.92 mg/kg on day 2 and day 3.
Developed rapid tolerance, with no significant inhibition observed after day 3.
Significantly inhibited food self-administration at 14.92 mg/kg/day, with significant decreases observed on days 2-5, 7, 8, and 14.
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Animal Model:Wistar (male, 300-350 g at study start, trained to self-administer nicotine then extinguished from responding before cue-induced reinstatement testing)[2]
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Dosage:1.12 mg/kg; 3.73 mg/kg; 7.46 mg/kg; 14.92 mg/kg
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Administration:p.o.; single dose
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Result:Significantly attenuated cue-induced reinstatement of nicotine-seeking behavior.
Attenuated the significant increase in active lever presses during reinstatement vs. extinction seen in the vehicle group at all tested doses.
Significantly decreased cue-induced reinstatement of food-seeking behavior, with no significant increase in responding observed in any treated group vs. extinction, unlike the vehicle group.
化学情報
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CAS 番号 1198309-73-7
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分子量 373.84
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分子式 C19H20ClN3O3
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SMILES
O=C1C=2C(CN1[C@@H](C)C3CC3)=CC(=CC2Cl)C4=CC(C(N(C)C)=O)=NO4
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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.
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)
AZD-8418 関連分類
HY-187088 関連分類
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Keywords
- AZD-8418
- 1198309-73-7
- AZD8418
- AZD 8418
- mGluR
- synaptic glutamate transmission
- rats
- tobacco alkaloid dependence
- mGluR2
- rat hippocampal CA1 slices
- rat mGlu2 receptor
- mGlu2/3 receptor agonists
- metabotropic glutamate receptor 2
- nonhuman primate prefrontal cortex brain tissue
- cynomolgus monkey prefrontal cortex tissue sections
- Inhibitor
- inhibitor
- inhibit