1. GPCR/G Protein
    Neuronal Signaling
  2. mGluR
  3. ADX71743

ADX71743 

Cat. No.: HY-110278
Handling Instructions

ADX71743 is a highly selective, noncompetitive and brain-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM). ADX71743 has anxiolytic-like activity.

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

ADX71743 Chemical Structure

ADX71743 Chemical Structure

CAS No. : 1431641-29-0

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Description

ADX71743 is a highly selective, noncompetitive and brain-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM). ADX71743 has anxiolytic-like activity[1][2].

IC50 & Target[1]

mGlu7

 

In Vitro

ADX71743 has an IC50 of 300 nM in-house cell lines. Pretreatment of ADX71743 (3 μM; for 20 min) before high-frequency stimulation (HFS) results in an almost complete blockade of LTP induction[1].
ADX71743 (0.1, 10 μM) reverses L-AP4-induced depression of synaptic transmission and results in a concentration-dependent reversal of the L-AP4-induced depression. 0.1 μM ADX71743 reverses the effects of L-AP4 by 11% and 10 μM results in a 20% reversal[2].
ADX71743 can against an EC80 of glutamate (IC50 of 22 nM) as well as against an EC80 of L-AP4 (IC50 of 125 nM)[2].

In Vivo

ADX71743 (50, 100, 150 mg/kg; SC) results in robust reductions in numbers of buried marbles to near maximal levels at lower doses (50 and 100 mg/kg)[2].
ADX71743 (12.5, 100 mg/kg for mice and 100 mg/kg for rat; SC) has a T1/2 of 0.68, 0.40 hours, a Cmax of 1380, 12766 ng/ml of 12.5 mg/kg and 100 mg/kg in mice[2].

Animal Model: Adult male C57Bl6/J mice (24-30 g)[2]
Dosage: 50, 100, 150 mg/kg
Administration: SC
Result: Resulted in robust reductions in numbers of buried marbles to near maximal levels at lower doses (50 and 100 mg/kg).
Animal Model: Adult male C57Bl6/J mice (24-30 g) and Sprague-Dawley rats (250-350 g)[2]
Dosage: 12.5, 100 mg/kg for mice and 100 mg/kg for rat (Pharmacokinetic Analysis)
Administration: SC
Result: Had a T1/2 of 0.68, 0.40 hours, a Cmax of 1380, 12766 ng/ml of 12.5 mg/kg and 100 mg/kg in mice.
Had a T1/2 of 1.5 hours, a Cmax of 16800 ng/ml of 100 mg/kg in rat.
Molecular Weight

269.34

Formula

C₁₇H₁₉NO₂

CAS No.

1431641-29-0

SMILES

O=C1C2=C(OC(CC)=N2)CC(C3=C(C=C(C)C=C3)C)C1

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:

ADX71743ADX 71743ADX-71743mGluRMetabotropic glutamate receptorsbrain-penetrantbbbmetabotropicglutamatereceptorNAManxiolytic-likeInhibitorinhibitorinhibit

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