209481-70-9Relevant articles and documents
Synthesis and SAR of (piperazin-1-yl-phenyl)-arylsulfonamides: A novel series of atypical antipsychotic agents
Park, Chul Min,Kim, So Young,Park, Woo Kyu,Choi, Jung Hwan,Seong, Churl Min
supporting information; experimental part, p. 5221 - 5224 (2010/10/01)
(Piperazin-1-yl-phenyl)-arylsulfonamides were synthesized and identified to show high affinities for both 5-HT2C and 5-HT6 receptors. Among them, naphthalene-2-sulfonic acid isopropyl-[3-(4-methyl-piperazin-1-yl)- phenyl]-amide (6b) exhibits the highest affinity towards both 5-HT2C (IC50 = 4 nM) and 5-HT6 receptors (IC50 = 3 nM) with good selectivity over other serotonin (5-HT1A, 5-HT 2A, and 5-HT7) and dopamine (D2-D4) receptor subtypes. In 5-HT2C and 5-HT6 receptor functional assays, this compound showed considerable antagonistic activity for both receptors.