γ-Carbolines: binding at 5-HT5A serotonin receptors

Abstract Screening of various agents resulted in the identification of 5-methyl-1,2,3,4-tetrahydro-γ-carboline ( 1 ; K i =5,300 nM) as a compound with modest affinity for mouse 5-HT 5A receptors. Structure–affinity studies were conducted resulting in 5-methyl-2-[3-(4-fluorophenoxy)propyl]-1,2,3,4-tetrahydro-γ-carboline ( 17 ; K i =13 nM). Although 17 also binds at 5-HT 2 receptors, it serves as a novel lead for the further development of 5-HT 5A ligands.