Literature DB >> 28514141

Subtype-Specific Agonists for NMDA Receptor Glycine Binding Sites.

Alex R Maolanon1, Rune Risgaard1, Shuang-Yan Wang1, Yoran Snoep1, Athanasios Papangelis1, Feng Yi2, David Holley2, Anne F Barslund1,3, Niels Svenstrup3, Kasper B Hansen2, Rasmus P Clausen1.   

Abstract

A series of analogues based on serine as lead structure were designed, and their agonist activities were evaluated at recombinant NMDA receptor subtypes (GluN1/2A-D) using two-electrode voltage-clamp (TEVC) electrophysiology. Pronounced variation in subunit-selectivity, potency, and agonist efficacy was observed in a manner that was dependent on the GluN2 subunit in the NMDA receptor. In particular, compounds 15a and 16a are potent GluN2C-specific superagonists at the GluN1 subunit with agonist efficacies of 398% and 308% compared to glycine. This study demonstrates that subunit-selectivity among glycine site NMDA receptor agonists can be achieved and suggests that glycine-site agonists can be developed as pharmacological tool compounds to study GluN2C-specific effects in NMDA receptor-mediated neurotransmission.

Entities:  

Keywords:  Ionotropic glutamate receptor; NMDA; d-cycloserine; d-serine; subtype selectivity; superagonist

Mesh：

Substances：

Year:  2017        PMID： 28514141      PMCID： PMC5559341          DOI： 10.1021/acschemneuro.7b00117

Source DB:  PubMed          Journal:  ACS Chem Neurosci        ISSN： 1948-7193            Impact factor:   4.418


  22 in total

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Journal:  J Med Chem       Date:  2016-03-08       Impact factor: 7.446

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Journal:  Mol Pharmacol       Date:  2013-04-26       Impact factor: 4.436

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Authors:  J B Monahan; W F Hood; R P Compton; A A Cordi; R M Williams
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10.  NMDA receptor structures reveal subunit arrangement and pore architecture.

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Journal:  Nature       Date:  2014-06-22       Impact factor: 49.962
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3.  Derivatives of (R)-3-(5-Furanyl)carboxamido-2-aminopropanoic Acid as Potent NMDA Receptor Glycine Site Agonists with GluN2 Subunit-Specific Activity.

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Review 9.  Structure, function, and allosteric modulation of NMDA receptors.

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