Literature DB >> 12639560

Novel N1-(benzyl)cinnamamidine derived NR2B subtype-selective NMDA receptor antagonists.

Neil R Curtis1, Helen J Diggle, Janusz J Kulagowski, Clare London, Sarah Grimwood, Peter H Hutson, Fraser Murray, Pawel Richards, Alison Macaulay, Keith A Wafford.   

Abstract

Novel (E)-N(1)-(benzyl)cinnamamidines were prepared and evaluated as NR2B subtype NMDA receptor ligands. Excellent affinity was achieved by appropriate substitution of either phenyl ring. The 2-methoxybenzyl compound 1h had approximately 1,000-fold lower IC(50) in NR2B than NR2A-containing cells. Replacement of the styryl unit by 2-naphthyl was well tolerated.

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Year:  2003        PMID: 12639560     DOI: 10.1016/s0960-894x(02)01060-0

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  7 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

2.  Opposing action of conantokin-G on synaptically and extrasynaptically-activated NMDA receptors.

Authors:  Rashna Balsara; Neill Li; Danielle Weber-Adrian; Louxiu Huang; Francis J Castellino
Journal:  Neuropharmacology       Date:  2012-01-27       Impact factor: 5.250

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.  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

Review 5.  Allosteric modulators of NR2B-containing NMDA receptors: molecular mechanisms and therapeutic potential.

Authors:  Laetitia Mony; James N C Kew; Martin J Gunthorpe; Pierre Paoletti
Journal:  Br J Pharmacol       Date:  2009-07-08       Impact factor: 8.739

6.  Molecular pharmacology of human NMDA receptors.

Authors:  Maiken Hedegaard; Kasper B Hansen; Karen T Andersen; Hans Bräuner-Osborne; Stephen F Traynelis
Journal:  Neurochem Int       Date:  2011-12-17       Impact factor: 3.921

7.  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

  7 in total

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