Cerebrospinal fluid and serum concentrations of the N -methyl- d -aspartate (NMDA) receptor antagonist memantine in man

Cerebrospinal fluid and serum concentrations of the N -methyl- d -aspartate (NMDA) receptor... Memantine is a uncompetitive N -methyl- d -aspartate (NMDA) receptor antagonist with therapeutic potential in dementia, spasticity and Parkinson's disease. The K i -value of memantine at the phencyclidine (PCP) binding site of the NMDA receptor is 0.5 μM in human frontal cortex. We investigated whether concentrations of mementine in cerebrospinal fluid (CSF) and serum samples under therapeutic conditions are in the range of its K i -value at the PCP binding site. The serum levels ranged from 0.025 to 0.529 μM with daily doses between 5 and 30 mg. CSF levels were highly correlated to serum levels and were below serum levels in each patient with a mean CSF/serum ratio of 0.52. Serum and CSF levels were correlated to the daily dose, but not to the duration of treatment. At the concentrations reported here, memantine is expected to specifically interact with the PCP binding site of the NMDA receptor. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Neuroscience Letters Elsevier

Cerebrospinal fluid and serum concentrations of the N -methyl- d -aspartate (NMDA) receptor antagonist memantine in man

Neuroscience Letters, Volume 195 (2) – Aug 4, 1995

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Publisher
Elsevier
Copyright
Copyright © 1995 Elsevier Ltd
ISSN
0304-3940
D.O.I.
10.1016/0304-3940(95)11785-U
Publisher site
See Article on Publisher Site

Abstract

Memantine is a uncompetitive N -methyl- d -aspartate (NMDA) receptor antagonist with therapeutic potential in dementia, spasticity and Parkinson's disease. The K i -value of memantine at the phencyclidine (PCP) binding site of the NMDA receptor is 0.5 μM in human frontal cortex. We investigated whether concentrations of mementine in cerebrospinal fluid (CSF) and serum samples under therapeutic conditions are in the range of its K i -value at the PCP binding site. The serum levels ranged from 0.025 to 0.529 μM with daily doses between 5 and 30 mg. CSF levels were highly correlated to serum levels and were below serum levels in each patient with a mean CSF/serum ratio of 0.52. Serum and CSF levels were correlated to the daily dose, but not to the duration of treatment. At the concentrations reported here, memantine is expected to specifically interact with the PCP binding site of the NMDA receptor.

Journal

Neuroscience LettersElsevier

Published: Aug 4, 1995

References

  • Therapeutic brain concentration of the NMDA receptor antagonist amantadine
    Kornhuber, J.; Quack, G.; Danysz, W.; Jellinger, K.; Danielczyk, W.; Gsell, W.; Riederer, P.

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