793672-13-6Relevant academic research and scientific papers
Arene- and quinoline-sulfonamides as novel 5-HT7 receptor ligands
Zajdel, Pawe?,Marciniec, Krzysztof,Ma?lankiewicz, Andrzej,Paluchowska, Maria H.,Sata?a, Grzegorz,Partyka, Anna,Jastrzbska-Wisek, Magdalena,Wróbel, Dagmara,Weso?owska, Anna,Duszyńska, Beata,Bojarski, Andrzej J.,Paw?owski, MacIej
, p. 6750 - 6759 (2011/12/04)
Novel arene- and quinolinesulfonamides were synthesized using different solutions and a solid-support methodology, and were evaluated for their affinity for 5-HT1A, 5-HT2A, 5-HT6, and 5-HT 7 receptors. Compound
Novel 5-HT7 receptor inverse agonists. Synthesis and molecular modeling of arylpiperazine- and 1,2,3,4-tetrahydroisoquinoline-based arylsulfonamides.
Vermeulen, Erik S,van Smeden, Marjan,Schmidt, Anne W,Sprouse, Jeffrey S,Wikstroem, Hakan V,Grol, Cor J
, p. 5451 - 5466 (2007/10/03)
A series of arylpiperazine- and 1,2,3,4-tetrahydroisoquinoline-based arylsulfonamides was synthesized and evaluated for their interactions with the constitutively active 5-HT7 receptor. Effects on basal adenylate cyclase activity were measured using HEK-293 cells expressing the rat 5-HT7. All ligands produced a decrease of adenylate cyclase activity, indicative of their inverse agonism. Additionally, computational studies with a set of 22 inverse agonists, including these novel inverse agonists and inverse agonists known from literature, resulted in a pharmacophore model and a CoMFA model (R2 = 0.97, SE = 0.18). Docking of inverse agonists at the binding site of a model of the helical parts of the 5-HT7 receptor, based on the alpha carbon template for 7-TM GPCRs, revealed interesting molecular interactions and a possible explanation for observed structure-activity relationships.
