What is the clinical evidence from this study?

Study design: Other. Population: Excitatory amino acid responses in rat neocortical neurons. Intervention: MK-801. Primary outcome: Current induced by N-methyl-D-aspartate (N-Me-D-Asp).

February 1, 1988Proceedings of the National Academy of SciencesOpen Access

Block of N-methyl-D-aspartate-activated current by the anticonvulsant MK-801: selective binding to open channels.

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Key result

MK-801 caused a progressive, voltage-dependent blockade of NMDA-induced currents by selectively binding to open channels, with faster recovery at positive potentials (tau ~2 min at +30 mV).

Population

Rat neocortical neurons in cell culture

Design

Preclinical

Authors

JHJames E. HuettnerHarvard University BBBruce P. BeanElectrophysiology

Discussion

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Implication

MK-801's use-dependent NMDA blockade in rat neurons leaves open its translation to neuroprotection; prospective in vivo studies needed before clinical consideration.

Structured PICO

Population

In vitro study using whole-cell and single-channel recording techniques on rat neocortical neurons in cell culture.

Intervention

MK-801 [(+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]- cyclohepten-5,10-imine maleate]

Outcome

Blockade of current induced by N-methyl-D-aspartate (N-Me-D-Asp)surrogate

MK-801 acts as an open-channel blocker of the NMDA receptor, requiring agonist activation for binding and unbinding.

Cite This Study

Huettner et al. (1988) studied Excitatory amino acid responses in rat neocortical neurons. MK-801 was evaluated on Current induced by N-methyl-D-aspartate (N-Me-D-Asp). MK-801 caused a progressive, voltage-dependent blockade of NMDA-induced currents by selectively binding to open channels, with faster recovery at positive potentials (tau ~2 min at +30 mV).

synapsesocial.com/papers/6a3155ee65e24aa33f6ab010 https://doi.org/10.1073/pnas.85.4.1307

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Implication

MK-801's use-dependent NMDA blockade in rat neurons leaves open its translation to neuroprotection; prospective in vivo studies needed before clinical consideration.

Block of N-methyl-D-aspartate-activated current by the anticonvulsant MK-801: selective binding to open channels.

Discussion

Member takes

Implication

Structured PICO

Cite This Study

Block of N-methyl-D-aspartate-activated current by the anticonvulsant MK-801: selective binding to open channels.

Discussion

Member takes

Implication

Structured PICO

Cite This Study

Also Consider

Also Consider