1431641-29-0
1431641-29-0 structure
- Name: ADX71743
- Chemical Name: ADX71743
- CAS Number: 1431641-29-0
- Molecular Formula: C17H19NO2
- Molecular Weight: 269.34
- Catalog: Signaling Pathways GPCR/G Protein mGluR
- Create Date: 2020-08-07 18:18:43
- Modify Date: 2024-01-09 15:11:34
-
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].
| Name | ADX71743 |
|---|
| 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]. |
|---|---|
| Related Catalog | |
| Target |
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. |
| References |
| Molecular Formula | C17H19NO2 |
|---|---|
| Molecular Weight | 269.34 |