5-HT7/5-HT2A receptor antagonist 1 is a high-affinity ligand targeting both the 5-HT7 and 5-HT2A receptors, demonstrating oral bioavailability and significant brain permeability with a pKi of 8.1. This compound functions as an antagonist in in vitro assays for the 5-HT2A receptor and as an inverse agonist for the 5-HT7 receptor. In vivo studies have shown that it effectively blocks 5-Carboxamidotryptamine (5-CT)-induced hypothermia in rats and DOI-induced head-twitches in mice, while it also occupies 5-HT2A receptor binding sites in the frontal cortex. 5-HT7/5-HT2A receptor antagonist 1 is suitable for investigating neuropharmacological disorders.
5-HT7/5-HT2A receptor antagonist 1 is a high-affinity ligand targeting both the 5-HT7 and 5-HT2A receptors, demonstrating oral bioavailability and significant brain permeability with a pKi of 8.1. This compound functions as an antagonist in in vitro assays for the 5-HT2A receptor and as an inverse agonist for the 5-HT7 receptor. In vivo studies have shown that it effectively blocks 5-Carboxamidotryptamine (5-CT)-induced hypothermia in rats and DOI-induced head-twitches in mice, while it also occupies 5-HT2A receptor binding sites in the frontal cortex. 5-HT7/5-HT2A receptor antagonist 1 is suitable for investigating neuropharmacological disorders.
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