Novel 5-HT7 receptor inverse agonists. Synthesis and molecular modeling of arylpiperazine- and 1,2,3,4-tetrahydroisoquinoline-based arylsulfonamides.

@article{Vermeulen2004Novel5R,
  title={Novel 5-HT7 receptor inverse agonists. Synthesis and molecular modeling of arylpiperazine- and 1,2,3,4-tetrahydroisoquinoline-based arylsulfonamides.},
  author={Erik S Vermeulen and Marjan van Smeden and Anne W. Schmidt and Jeffrey S Sprouse and H{\aa}kan V. Wikstr{\"o}m and Cor J. Grol},
  journal={Journal of medicinal chemistry},
  year={2004},
  volume={47 22},
  pages={5451-66}
}
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… CONTINUE READING

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