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Vol. 280, Issue 2, 614-620, 1997
Department of Pharmacology and Division of Neurology, Department of
Internal Medicine, University of Nebraska Medical Center, Omaha,
Nebraska
The potencies of various N-methyl-D-aspartate (NMDA)
receptor channel blockers were determined at recombinant NMDA receptors containing differing combinations of NR1 and NR2 subunits expressed in
Xenopus laevis oocytes. When the NR1 subunit was varied
(NR1e/NR2A or NR1b/NR2A), none of the 9 channel blockers tested
displayed a statistically different affinity. In contrast, altering NR2 composition changed the affinities of several channel blockers. Three
of 10 compounds displayed significantly higher affinities for NR1b/NR2C
receptors than NR1b/NR2A receptors, and three of five compounds had
higher affinity at NR1b/NR2C than NR1b/NR2B receptors. Both MK-801 and
N-[1-(2-thienyl)cyclohyxyl]piperidine displayed identical affinities
at all receptor subunit combinations tested. However, these two
compounds displayed significantly slower rates of blockade and
unblockade at NR1b/NR2C than at NR1b/NR2A receptors, perhaps reflecting
the shorter mean open times of NR1/NR2C receptors. NR1b/NR2B and
NR1b/NR2A were distinguished by one of five compounds tested. Taken
together, these results indicate that NR2 subunits impart differing
pharmacological profiles to NMDA receptors; thus, it may be possible to
develop NMDA receptor channel blocker antagonists of greater subtype
selectivity.
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