838822-02-9Relevant academic research and scientific papers
Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia
Ko?aczkowski, Marcin,Marcinkowska, Monika,Bucki, Adam,?niecikowska, Joanna,Paw?owski, Maciej,Kazek, Grzegorz,Siwek, Agata,Jastrz?bska-Wi?sek, Magdalena,Partyka, Anna,Wasik, Anna,Weso?owska, Anna,Mierzejewski, Pawe?,Bienkowski, Przemyslaw
supporting information, p. 221 - 235 (2015/06/30)
We describe a novel class of designed multiple ligands (DMLs) combining serotonin 5-HT6 receptor (5-HT6R) antagonism with dopamine D2 receptor (D2R) partial agonism. Prototype hybrid molecules were designed usin
N1-arylsulfonyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives are potent and selective 5-HT6 receptor antagonists
Cole, Derek C.,Ellingboe, John W.,Lennox, William J.,Mazandarani, Hossein,Smith, Deborah L.,Stock, Joseph R.,Zhang, Guoming,Zhou, Ping,Schechter, Lee E.
, p. 379 - 383 (2007/10/03)
The development of a series of N1-sulfonyl-3-(1,2,3,6- tetrahydropyridin-4-yl)indole 5-HT6 antagonists is described. Two analogs, 15g and 15y, had 0.4 and 3.0 nM affinity, and antagonized the production of adenylate cyclase at sub-nanomolar concentrations. A series of N1-arylsulfonyl-3-(1,2,3,6-tetrahydropyridin-4-yl)indole derivatives was designed and synthesized. These compounds were shown to have high affinity for the 5-HT6 receptor. Two analogs, 4-[3-(1,2,3,6-tetrahydropyridin- 4-yl)-1H-indole-1-sulfonyl]-phenylamine 15g and 4-[3-(1,2,3,6-tetrahydropyridin- 4-yl)-5-methoxy-1H-indole-1-sulfonyl]-phenylamine 15y, had 0.4 and 3.0 nM affinity, respectively, and antagonized the production of adenylate cyclase at sub-nanomolar concentrations.
