AM1488 is a potent, orally active glycine receptor ( GlyR ) potentiator (hGlyRα3 EC 50 =0.45 μM) [1] [2].

AM-1488 also potentiates native GlyRs in mouse spinal-cord neurons, which express mostly GlyRα1(β) and GlyRα3(β) [1]. Cell Viability Assay [1] Cell Line: Mouse spinal-cord neuron Concentration: 0.5 μM Incubation Time: 10 min Result: Increased the peak current evoked by a puff of 20 μM glycine in five out of five cells, from an average of 50.8 pA to an average of 222.2 pA.

AM-1488 (oral gavage; 20 mg/kg; once) treatment significantly reverse mechanical allodynia induced by nerve injury in a mouse model of neuropathic pain, without being confounded by sedation or motor side effects [1]. Animal Model: Mouse model of spared nerve injury (SNI) [1] Dosage: 20 mg/kg Administration: Oral gavage; 20 mg/kg; once Result: Produced a significant 94% reversal of tactile allodynia, and the unbound brain concentration was 2.8- and 1.6-fold higher than the mouse GlyRα1 and GlyRα3 EC 50 values, respectively. Animal Model: Naive mice [1] Dosage: 20 mg/kg Administration: Oral gavage; 20 mg/kg; once Result: Showed not significantly different from mice treated with vehicle.