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- W2999911279 abstract "Allosteric modulators of ion channels typically alter the transitions rates between conformational states without changing the properties of the open pore. Here we describe a new class of positive allosteric modulators of N-methyl D-aspartate receptors (NMDARs) that mediate a calcium-permeable component of glutamatergic synaptic transmission and play essential roles in learning, memory and cognition, as well as neurological disease. EU1622-14 increases agonist potency and channel-open probability, slows receptor deactivation and decreases both single-channel conductance and calcium permeability. The unique functional selectivity of this chemical probe reveals a mechanism for enhancing NMDAR function while limiting excess calcium influx, and shows that allosteric modulators can act as biased modulators of ion-channel permeation." @default.
- W2999911279 created "2020-01-23" @default.
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- W2999911279 date "2020-01-20" @default.
- W2999911279 modified "2023-09-28" @default.
- W2999911279 title "Biased modulators of NMDA receptors control channel opening and ion selectivity" @default.
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- W2999911279 doi "https://doi.org/10.1038/s41589-019-0449-5" @default.
- W2999911279 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/6986806" @default.
- W2999911279 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/31959964" @default.
- W2999911279 hasPublicationYear "2020" @default.
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