305339-41-7Relevant academic research and scientific papers
Structure-activity relationships of N-substituted 4-(trifluoromethoxy) benzamidines with affinity for GluN2B-containing NMDA receptors
Beinat, Corinne,Banister, Samuel D.,Hoban, Jane,Tsanaktsidis, John,Metaxas, Athanasios,Windhorst, Albert D.,Kassiou, Michael
, p. 828 - 830 (2014/02/14)
GluN2B subtype-selective NMDA antagonists represent promising therapeutic targets for the symptomatic treatment of multiple CNS pathologies. A series of N-benzyl substituted benzamidines were synthesised and the benzyl ring was further replaced with various polycyclic moieties. Compounds were evaluated for activity at GluN2B containing NMDA receptors where analogues 9, 12, 16 and 18 were the most potent of the series, replacement of the benzyl ring with polycycles resulted in a complete loss of activity.
Orally efficacious NR2B-selective NMDA receptor antagonists
Claiborne, Christopher F.,McCauley, John A.,Libby, Brian E.,Curtis, Neil R.,Diggle, Helen J.,Kulagowski, Janusz J.,Michelson, Stuart R.,Anderson, Kenneth D.,Claremon, David A.,Freidinger, Roger M.,Bednar, Rodney A.,Mosser, Scott D.,Gaul, Stanley L.,Connolly, Thomas M.,Condra, Cindra L.,Bednar, Bohumil,Stump, Gary L.,Lynch, Joseph J.,Macaulay, Alison,Wafford, Keith A.,Koblan, Kenneth S.,Liverton, Nigel J.
, p. 697 - 700 (2007/10/03)
A novel series of benzamidines was synthesized and shown to exhibit NR2B-subtype selective NMDA antagonist activity. Compound 31 is orally active in a carrageenan-induced rat hyperalgesia model of pain and shows no motor coordination side effects.
