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.
|Animal models||male Long-Evans rats|
|Formulation||sterile 0.9% sodium chloride solution|
|Administration||Inject intraperitoneally at a single dose30 min before sacrifice|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 70 mg/mL|
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