| Bioactivity | 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]. |
| Invitro | 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: |
| Name | ADX71743 |
| CAS | 1431641-29-0 |
| Formula | C17H19NO2 |
| Molar Mass | 269.34 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. [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. |