5-HT7/5-HT2A receptor antagonist 1

5-HT7/5-HT2A receptor antagonist 1 is a high-affinity, orally active compound capable of crossing the blood-brain barrier, serving as a ligand for both 5-HT7 and 5-HT2A receptors with a pKi of 8.1 at each receptor. It acts as an antagonist in vitro in 5-HT2A functional assays and as an inverse agonist in 5-HT7 functional assays. This compound blocks hypothermia in rats induced by 5-Carboxamidotryptamine (5-CT) and prevents head twitches in mice caused by 2,5-Dimethoxy-4-iodoamphetamine (DOI) . Additionally, it occupies 5-HT2A receptor binding sites in the frontal cortex of rat brains and is applicable in the study of neurological disorders.