685841-33-2Relevant academic research and scientific papers
Synthesis, evaluation and metabolic studies of radiotracers containing a 4-(4-[18F]-fluorobenzyl)piperidin-1-yl moiety for the PET imaging of NR2B NMDA receptors
Labas, Romain,Gilbert, Gwéna?lle,Nicole, Olivier,Dhilly, Martine,Abbas, Ahmed,Tirel, Olivier,Buisson, Alain,Henry, Jo?l,Barré, Louisa,Debruyne, Danièle,Sobrio, Franck
supporting information; experimental part, p. 2295 - 2309 (2011/06/21)
In this study, novel specific PET radioligands containing the 4-(4-fluorobenzyl)piperidine moiety and selectively antagonistic for the NR2B subunit containing NMDA receptors were developed. Two antagonists, RGH-896 (1a) and 4-(4-fluorobenzyl)piperidinyl-1
NR2B-Selective N-Methyl-D-aspartate Antagonists: Synthesis and Evaluation of 5-Substituted Benzimidazoles
McCauley, John A.,Theberge, Cory R.,Romano, Joseph J.,Billings, Susan B.,Anderson, Kenneth D.,Claremon, David A.,Freidinger, Roger M.,Bednar, Rodney A.,Mosser, Scott D.,Gaul, Stanley L.,Connolly, Thomas M.,Condra, Cindra L.,Xia, Menghang,Cunningham, Michael E.,Bednar, Bohumil,Stump, Gary L.,Lynch, Joseph J.,Macaulay, Alison,Wafford, Keith A.,Koblan, Kenneth S.,Liverton, Nigel J.
, p. 2089 - 2096 (2007/10/03)
Two classes of 5-substituted benzimidazoles were identified as potent antagonists of the NR2B subtype of the N-methyl-D-aspartate (NMDA) receptor. Selected compounds show very good selectivity versus the NR2A, NR2C, and NR2D subtypes of the NMDA receptor as well as versus hERG-channel activity and α1-adrenergic binding. Benzimidazole 37a shows excellent activity in the carrageenan-induced mechanical hyperalgesia assay in rats as well as good pharmacokinetic behavior in dogs.
2-[(4-BENZYL)-1-PIPERIDINYL)METHYL]BENZIMIDAZOLE-5-OL DERIVATIVES AS NR2B RECEPTOR ANTAGONISTS
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, (2008/06/13)
2-[(4-Benzyl)-1-piperidinyl)-methyl]benzimidazole-5-ol derivatives are NMDA NR2B receptor antagonists useful in the treatment of pain and other NMDA mediated diseases.
