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ADX-47273 is a novel, potent and selective metabotropic glutamate receptor 5 allosteric modulator with an EC50 of 170 nM in human embryonic kidney 293 cells expressing rat mGlu5. ADX-47273 shifted mGlu5 receptor glutamate response curve to the left (9-fold at 1 μM) and competed for binding of [3H]2-methyl-6- (phenylethynyl) pyridine with a Ki of 4.3 μM in a dose-dependent manner, but not [3H]quisqualate. In vivo, ADX-47273 elevated extracellular signal-regulated kinase and cAMP-responsive element-binding protein phosphorylation in hippocampus and prefrontal cortex. In models sensitive to antipsychotic compound treatment, ADX-47273 decreased rat-conditioned avoidance responding [minimal effective dose (MED) = 30 mg/kg i.p.] and reduced mouse apomorphine-induced climbing (MED = 100 mg/kg i.p.), with little effect on stereotypy or catalepsy. Furthermore, ADX-47273 inhibited phencyclidine, apomorphine, and amphetamine-induced locomotor activities in mice and reduced extracellular levels of dopamine in the nucleus accumbens, but not in the striatum, in rats. In cognition models, ADX-47273 improved novel object recognition (MED = 1 mg/kg i.p.) and decreased impulsivity in the five-choice serial reaction time test (MED = 10 mg/kg i.p.) in rats.
| Cell Experiment | |
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| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
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| Animal models | male Long-Evans rats |
| Formulation | sterile 0.9% sodium chloride solution |
| Dosages | 10 mg/kg |
| Administration | Inject intraperitoneally at a single dose30 min before sacrifice |
| Molecular Weight | 369.36 |
| Formula | C20H17F2N3O2 |
| CAS Number | 851881-60-2 |
| Solubility (25°C) | DMSO 70 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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| ATPA
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(R)-CPP is a highly potent NMDA receptor antagonist. |
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