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Art. -Nr.: HY-187088

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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.

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CAS. Nr.: 1198309-73-7
Formel: C₁₉H₂₀ClN₃O₃
Molecular Weight:373.84

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

AZD-8418 Chemical Structure

CAS. Nr.: 1198309-73-7

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[2]

rat mGluR2

0.86 μM (EC₅₀)

Alle mGluR Isoform-spezifische Produkte anzeigen :

In Vitro

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

Species	Dose	Route	Note	C_max	T_max	AUC
Rat^[2]	5 mg/kg	p.o.	Day 1	690 nM	1 h	3041 nM·h
Rat^[2]	5 mg/kg	p.o.	Day 7	528 nM	1 h	2761 nM·h

In Vivo

AZD-8418 (0.37-14.92 mg/kg; p.o.; single administration) dose-dependently inhibits nicotine self-administration behavior in brown rats (Rattus norvegicus) without altering their response for maintaining food intake^[2].
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.

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]
Dosage:

0.37 mg/kg; 1.12 mg/kg; 3.73 mg/kg; 7.46 mg/kg; 14.92 mg/kg
Administration:

p.o.; single dose
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.

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]
Dosage:

3.73 mg/kg/day; 7.46 mg/kg/day; 14.92 mg/kg/day
Administration:

p.o.; daily; 14 days
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.

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]
Dosage:

1.12 mg/kg; 3.73 mg/kg; 7.46 mg/kg; 14.92 mg/kg
Administration:

p.o.; single dose
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.

Chemical Information

CAS. Nr. 1198309-73-7
Molecular Weight 373.84
Formel C₁₉H₂₀ClN₃O₃
SMILES

O=C1C=2C(CN1[C@@H](C)C3CC3)=CC(=CC2Cl)C4=CC(C(N(C)C)=O)=NO4
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Li Y, et al. Radiosynthesis and Evaluation of 11C-Labeled Isoindolone-Based Positive Allosteric Modulators for Positron Emission Tomography Imaging of Metabotropic Glutamate Receptor 2. ACS pharmacology & translational science. 2024 Aug 09;7(8):2414-2423. [Content Brief]

[2]. Li X, et al. Attenuation of nicotine-taking and nicotine-seeking behavior by the mGlu2 receptor positive allosteric modulators AZD8418 and AZD8529 in rats. Psychopharmacology. 2016 May;233(10):1801-14.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

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MOQ

Minimum order quantity

100 mg

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