Literature DB >> 15056006

NR2B-selective N-methyl-D-aspartate antagonists: synthesis and evaluation of 5-substituted benzimidazoles.

John A McCauley1, Cory R Theberge, Joseph J Romano, Susan B Billings, Kenneth D Anderson, David A Claremon, Roger M Freidinger, Rodney A Bednar, Scott D Mosser, Stanley L Gaul, Thomas M Connolly, Cindra L Condra, Menghang Xia, Michael E Cunningham, Bohumil Bednar, Gary L Stump, Joseph J Lynch, Alison Macaulay, Keith A Wafford, Kenneth S Koblan, Nigel J Liverton.   

Abstract

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 alpha(1)-adrenergic binding. Benzimidazole 37a shows excellent activity in the carrageenan-induced mechanical hyperalgesia assay in rats as well as good pharmacokinetic behavior in dogs.

Entities:  

Mesh：

Substances：

Year:  2004        PMID： 15056006     DOI： 10.1021/jm030483s

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  12 in total

Review 1.  Glutamate receptor ion channels: structure, regulation, and function.

Authors:  Stephen F Traynelis; Lonnie P Wollmuth; Chris J McBain; Frank S Menniti; Katie M Vance; Kevin K Ogden; Kasper B Hansen; Hongjie Yuan; Scott J Myers; Ray Dingledine
Journal:  Pharmacol Rev       Date:  2010-09       Impact factor: 25.468

Review 2.  Control of assembly and function of glutamate receptors by the amino-terminal domain.

Authors:  Kasper B Hansen; Hiro Furukawa; Stephen F Traynelis
Journal:  Mol Pharmacol       Date:  2010-07-21       Impact factor: 4.436

Review 3.  Ionotropic and metabotropic glutamate receptor structure and pharmacology.

Authors:  James N C Kew; John A Kemp
Journal:  Psychopharmacology (Berl)       Date:  2005-02-25       Impact factor: 4.530

4.  Mapping the binding of GluN2B-selective N-methyl-D-aspartate receptor negative allosteric modulators.

Authors:  Pieter B Burger; Hongjie Yuan; Erkan Karakas; Matthew Geballe; Hiro Furukawa; Dennis C Liotta; James P Snyder; Stephen F Traynelis
Journal:  Mol Pharmacol       Date:  2012-05-17       Impact factor: 4.436

5.  Enantiomeric propanolamines as selective N-methyl-D-aspartate 2B receptor antagonists.

Authors:  Yesim A Tahirovic; Matthew Geballe; Ewa Gruszecka-Kowalik; Scott J Myers; Polina Lyuboslavsky; Phuong Le; Adam French; Hasan Irier; Woo-Baeg Choi; Keith Easterling; Hongjie Yuan; Lawrence J Wilson; Robert Kotloski; James O McNamara; Raymond Dingledine; Dennis C Liotta; Stephen F Traynelis; James P Snyder
Journal:  J Med Chem       Date:  2008-09-25       Impact factor: 7.446

6.  A Glutamate N-Methyl-d-Aspartate (NMDA) Receptor Subunit 2B-Selective Inhibitor of NMDA Receptor Function with Enhanced Potency at Acidic pH and Oral Bioavailability for Clinical Use.

Authors:  Scott J Myers; Kamalesh P Ruppa; Lawrence J Wilson; Yesim A Tahirovic; Polina Lyuboslavsky; David S Menaldino; Zackery W Dentmon; George W Koszalka; Robert Zaczek; Raymond J Dingledine; Stephen F Traynelis; Dennis C Liotta
Journal:  J Pharmacol Exp Ther       Date:  2021-09-07       Impact factor: 4.402

7.  NR2B-selective conantokin peptide inhibitors of the NMDA receptor display enhanced antinociceptive properties compared to non-selective conantokins.

Authors:  Cai Xiao; Yuanyuan Huang; Mingxin Dong; Jie Hu; Shuangshuang Hou; Francis J Castellino; Mary Prorok; Qiuyun Dai
Journal:  Neuropeptides       Date:  2008-11-07       Impact factor: 3.286

8.  Mapping the high-affinity binding domain of 5-substituted benzimidazoles to the proximal N-terminus of the GluN2B subunit of the NMDA receptor.

Authors:  X-K Wee; K-S Ng; H-W Leung; Y-P Cheong; K-H Kong; F-M Ng; W Soh; Y Lam; C-M Low
Journal:  Br J Pharmacol       Date:  2010-01-15       Impact factor: 8.739

9.  Synthesis, structural activity-relationships, and biological evaluation of novel amide-based allosteric binding site antagonists in NR1A/NR2B N-methyl-D-aspartate receptors.

Authors:  Cara A Mosley; Scott J Myers; Ernest E Murray; Rose Santangelo; Yesim A Tahirovic; Natalie Kurtkaya; Praseeda Mullasseril; Hongjie Yuan; Polina Lyuboslavsky; Phuong Le; Lawrence J Wilson; Manuel Yepes; Ray Dingledine; Stephen F Traynelis; Dennis C Liotta
Journal:  Bioorg Med Chem       Date:  2009-07-05       Impact factor: 3.641

10.  Structural insights into phenylethanolamines high-affinity binding site in NR2B from binding and molecular modeling studies.

Authors:  Fui-Mee Ng; Matthew T Geballe; James P Snyder; Stephen F Traynelis; Chian-Ming Low
Journal:  Mol Brain       Date:  2008-11-18       Impact factor: 4.041
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.