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

AZD-8529 mesylate 

Cat. No.: HY-107457A
Handling Instructions

AZD-8529 mesylate 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 mesylate Chemical Structure

AZD-8529 mesylate Chemical Structure

CAS No. : 1314217-69-0

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Description

AZD-8529 mesylate 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[1].

IC50 & Target

EC50: 285 nM (mGluR2)[1]

In Vitro

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

In Vivo

AZD-8529 mesylate (0.3-mg/kg, i.m.) reduces nicotine priming-induced and cue-induced reinstatement in squirrel monkeys[1].
AZD-8529 mesylate (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.
Molecular Weight

583.58

Formula

C₂₅H₂₈F₃N₅O₆S

CAS No.

1314217-69-0

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

AZD-8529AZD8529AZD 8529mGluRMetabotropic glutamate receptorsmGluR2receptornicotineaddictiontreatmentInhibitorinhibitorinhibit

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AZD-8529 mesylate
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