MRS5474

MRS5474 is a potent, selective, orally bioavailable small molecule agonist of the adenosine A1 receptor (A1R), designed for central nervous system applications due to its ability to cross the blood-brain barrier with minimal cardiovascular side effects. It exhibits antidepressant effects in mouse models via A1R-mediated upregulation of homer1 protein in the medial prefrontal cortex and ERK signaling pathway activation, and demonstrates anticonvulsant activity in the 6-Hz psychomotor seizure model with low behavioral toxicity. Recent studies reveal additional disease-specific modulation in epileptic tissue through inhibition of GABA transporter type 1 (GAT-1) uptake and potentiation of GABA currents, potentially involving A3R overexpression in human epileptic hippocampus.[1][2][3][7][8][9]