TPH2 agonist-1

TPH2 agonist-1 (compound 20e) is an orally active TPH2 agonist that can penetrate the blood-brain barrier and is derived from 1,3,4-oxadiazol-2(3H)-one. In models with SCN1A defects, TPH2 agonist-1 enhances TPH2 expression and increases levels of 5-HT and GABA, demonstrating anticonvulsant activity. It stabilizes neuronal network electrophysiological activity and suppresses abnormal spike and burst activities. TPH2 agonist-1 shows no significant hERG inhibition or cytotoxicity and is suitable for studies related to severe myoclonic epilepsy in infancy (Dravet syndrome).