CYM2503 is a putative galanin receptor type 2 (GalR2) positive allosteric modulator, concentration-dependently potentiates galanin (100 nM) stimulated IP1 accumulation in HEK293-GalR2 cells with EC50 of 0.69 uM, efficacy of 9.7-fold potentiation.
CYM2503 exhibited no affinity for GalR1 anddid not modulate GalR1 signaling.
CYM2503 mediated potentiation of the agonist-stimulated GalR2 activation and the lack of affinity of CYM2503 for GalR2 orthosteric site in HEK293-GalR2 cells.
CYM2503 increased the latency to first electrographic seizure and the latency to first stage 3 behavioral seizure, decreased the latency to the establishment of SE, and dramatically decreased mortality in the rat Li-pilocarpine SE model.
CYM2503 increased the latency to first electrographic seizure and decreased the total time in seizure in Li-pilocarpine seizure model in mice, also attenuated electroshock-induced seizures in mice.