ADX-47273

ADX-47273 is a potent, selective and brain-penetrant mGluR5 positive allosteric modulator (PAM), with an EC₅₀ of 0.17 μM for potentiation of glutamate (50 nM) response. ADX-47273 has antipsychotic and procognitive activities^[1][2]. IC50 & Target: EC50: 0.17 μM (mGluR5)^[1] In Vitro: ADX-47273 (0.1 nM-10 μM; 5 min) causes a concentration-dependent increase in the response to 50 nM glutamate in HEK 293 cells expressing rat mGlu5 without eliciting a response by itself^[1].
ADX-47273 (0.1 nM-10 μM; 5 min) causes a concentration-dependent increase in the response to 300 nM glutamate in primary astrocyte cultures, with an EC₅₀ of 0.23 μM^[1].
ADX47273 (0.01-10 μM; 60 min) inhibits [³H]MPEP binding to rat mGlu5 receptor HEK cell membranes, with a K_i of 4.3 μM^[1]. In Vivo: ADX47273 (1-10 mg/kg; a single i.p.) dose-dependently increases ERK and CREB phosphorylation in rat hippocampus and prefrontal cortex^[1].
ADX47273 (10-100 mg/kg; a single i.p.) decreases conditioned avoidance responding in a dose-dependent manner in rats^[1].
ADX47273 (10-300 mg/kg; i.p.) blocks apomorphine-induced climbing in mice^[1].
ADX47273 (0.1-50 mg/kg; i.p.) increases novel object recognition and reduces impulsivity in the five-choice serial reaction time test in rats^[1].
ADX47273 (15 mg/kg; i.p.) enhances reversal learning in the Morris Water Maze (MWM) in mice^[3].