Structure, function, and pharmacology of NMDA receptor channels

Title:

Structure, function, and pharmacology of NMDA receptor channels

Creator:

Vyklicky, V., Korinek, M., Smejkalova, T., Aleš Balík, Krausova, B., Kaniakova, M., Lichnerova, K., Cerny, J., Krusek, J., Ivan Dittert, Martin Horák, and Vyklicky, L.

Identifier:

https://cdk.lib.cas.cz/client/handle/uuid:1b726303-e766-47f9-83fd-90d778a72e68
uuid:1b726303-e766-47f9-83fd-90d778a72e68

Subject:

Fyziologie člověka a srovnávací fyziologie, iontové kanály, farmakologie, ion channels, pharmacology, glutamate receptor, NMDA receptor, channel blocker, synaptic transmission, 14, and 612

Type:

article, články, model:article, and TEXT

Format:

print

Description:

NMDA receptors have received much attention over the last few decades, due to their role in many types of neural plasticity on the one hand, and their involvement in excitotoxicity on the other hand. There is great interest in developing clinically relevant NMDA receptor antagonists that would block excitotoxic NMDA receptor activation, without interfering with NMDA receptor function needed for normal synaptic transmission and plasticity. This review summarizes current understanding of the structure of NMDA receptors and the mechanisms of NMDA receptor activation and modulation, with special attention given to data describing the properties of various types of NMDA receptor inhibition. Our recent analyses point to certain neurosteroids as NMDA receptor inhibitors with desirable properties. Specifically, these compounds show use-dependent but voltage-independent block, that is predicted to preferentially target excessive tonic NMDA receptor activation. Importantly, neurosteroids are also characterized by use-independent unblock, compatible with minimal disruption of normal synaptic transmission. Thus, neurosteroids are a promising class of NMDA receptor modulators that may lead to the development of neuroprotective drugs with optimal therapeutic profiles., V. Vyklicky ... [et al.]., and Obsahuje bibliografii a bibliografické odkazy

Language:

English

Rights:

http://creativecommons.org/licenses/by-nc-sa/4.0/
policy:public

Source:

Physiological research | 2014 Volume:63 | Number:Suppl 1

Harvested from:

CDK

Metadata only:

false