1. GPCR/G Protein
    Neuronal Signaling
  2. mGluR
  3. AZD-8529

AZD-8529 

Cat. No.: HY-107457
Handling Instructions

AZD-8529 is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.

For research use only. We do not sell to patients.

AZD-8529 Chemical Structure

AZD-8529 Chemical Structure

CAS No. : 1092453-15-0

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Description

AZD-8529 is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.

IC50 & Target

EC50: 285 nM (mGluR2)[1]

In Vitro

AZD-8529 potentiates the effects of glutamate at mGluR2 with an EC50 of 195 nM[1].
AZD-8529 does not elicit antagonist responses on mGluRs at 25 μM[1].

In Vivo

AZD-8529 (0.3-mg/kg, i.m.) reduces nicotine priming-induced and cue-induced reinstatement in squirrel monkeys[1].
AZD-8529 (30 mg/kg; i.p.) decreases the increased extracellular dopamine induced by nicotine in accumbens shell of freely-moving rats[1].

Animal Model: Sprague-Dawley rats[1]
Dosage: 10 mg/kg, 30 mg/kg
Administration: Intraperitoneal injection; 2 hours before nicotine injections
Result: Decreased the increased extracellular dopamine induced by nicotine (0.4 mg/kg, s.c.) in accumbens shell of freely-moving rats.
Clinical Trial
Molecular Weight

487.47

Formula

C₂₄H₂₄F₃N₅O₃

CAS No.

1092453-15-0

SMILES

O=C1C2=C(C)C=C(C3=NC(CN4CCNCC4)=NO3)C=C2CN1CC5=CC=C(OC(F)(F)F)C=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

AZD-8529AZD8529AZD 8529mGluRMetabotropic glutamate receptorsmGluR2receptornicotineaddictiontreatmentInhibitorinhibitorinhibit

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AZD-8529
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