Design, Synthesis and 5-HT1A Binding Affinity of N-(3-(4-(2-Methoxyphenyl)piperazin-1-yl)propyl)tricyclo[3.3.1.13,7]decan-1-amine and N-(3-(4-(2-Methoxyphenyl)piperazin-1-yl)propyl)-3,5-dimethyl-tricylo[3.3.1.13,7]decan-1-amine

Based on previously highlighted structural features, the development of highly selective 5-HT1A receptor inhibitors is closely linked to incorporation a 4-alkyl-1-arylpiperazine scaffold them. In this paper, we present synthesis two new compounds bearing 2-MeO-Ph-piperazine moiety via three carbon atom linker amine group 1-adamantanamine and memantine, respectively. Both were tested for their binding affinity against receptor. N-(3-(4-(2-methoxyphenyl)piperazin-1-yl)propyl)tricyclo[3.3.1.13,7]decan-1-amine fumarate (8) N-(3-(4-(2-methoxyphenyl)piperazin-1-yl)propyl)-3,5-dimethyl-tricylo[3.3.1.13,7]decan-1-amine (10) proved be ligands towards with constant 1.2 nM 21.3 nM, respectively, while 5-carboxamidotriptamine (5-CT) (2) was used as an internal standard assay measured Ki = 0.5 nM.