Arylpiperazine derivatives as high-affinity 5-HT1A serotonin ligands.

摘要: Although simple arylpiperazines are commonly considered to be moderately selective for 5-HT1B serotonin binding sites, N4-substitution of such compounds can enhance their affinity 5-HT1A sites and/or decrease sites. A small series 4-substituted 1-arylpiperazines was prepared in an attempt develop agents with high Derivatives where the aryl portion is phenyl, 2-methoxyphenyl, or 1-naphthyl, and 4-substituent either a phthalimido benzamido group at distance four methylene units away from piperazine 4-position, display these One compounds, 1-(2-methoxyphenyl)-4-[4-(2-phthalimido)butyl]piperazine (18), possesses higher than 5-HT represents highest (Ki = 0.6 nM) agent yet reported