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Novel NMDA Receptor Antagonists: A Review of Compounds Patented since 2006

Koller, Manuel and Urwyler, S (2010) Novel NMDA Receptor Antagonists: A Review of Compounds Patented since 2006. Expert Opinion On Therapeutic Patents, 20 (12). pp. 1683-1702. ISSN 1354-3776


Background: The N-methyl-D-aspartate (NMDA) receptor is a complex ligand gated, voltage dependent ion channel, consisting of an assembly of several subunits and equipped with numerous binding sites for small molecules. Largely restricted to the central nervous system, it is a drug target since more than 25 years for neurological as well as psychiatric indications. Whereas the initial optimism to turn preclinically active compounds rapidly into drugs for human use was dampened, new insights into cellular receptor localization, role of subunits and receptor operation have kept the interest alive to modulate this receptor for therapeutic intervention.
Objective/method: This review presents the novel NMDA receptor antagonists patented since 2006 and puts them in the context of their respective binding site, together with their pharmacological activity. Also included are novel NMDA receptor ligands potentially useful for PET imaging.
Conclusion: The most important approaches followed today for inhibition of NMDA receptor mediated neurotransmission are blockade of the channel with compounds of low affinity for the pore region, and antagonizing receptor activity by highly potent and selective NR2B ligands. Other approaches comprise partial agonism at the glutamate or glycine binding site, and improvement of pharmacokinetic properties of established antagonists by deuteration.

Item Type: Article
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Date Deposited: 13 Oct 2015 13:15
Last Modified: 13 Oct 2015 13:15


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