ADX71743 

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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 T_1/2 of 0.68, 0.40 hours, a C_max of 1380, 12766 ng/ml of 12.5 mg/kg and 100 mg/kg in mice^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

269.34

C₁₇H₁₉NO₂

1431641-29-0

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

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• [1]. Rebecca Klar, et al. Activation of Metabotropic Glutamate Receptor 7 Is Required for Induction of Long-Term Potentiation at SC-CA1 Synapses in the Hippocampus. J Neurosci. 2015 May 13;35(19):7600-15.  [Content Brief]

  [2]. Mikhail Kalinichev , et al. ADX71743, a Potent and Selective Negative Allosteric Modulator of Metabotropic Glutamate Receptor 7: In Vitro and in Vivo Characterization. Pharmacol Exp Ther. 2013 Mar;344(3):624-36.  [Content Brief]