Differences in degree of trapping between AR-R15896 and other uncompetitive NMDA receptor antagonists.
NMDA antagonists like AR-R15896 have been selected on the basis of their good therapeutic indices. As Dr. Rogawski has pointed out, there may be a number of molecular factors which can improve the therapeutic index of NMDA antagonists. In this paper we will consider three factors; use-dependence, low affinity/fast kinetics, and partial trapping.
Lanthorn
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AstraZeneca R&D Boston, Rochester, New York 14602, USA.
Mealing
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GA
Morley
P
P
D018691:Excitatory Amino Acid Antagonists / Q000494:pharmacology*; D011725:Pyridines / Q000494:pharmacology*; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors*
D018691:Excitatory Amino Acid Antagonists; D011725:Pyridines; D016194:Receptors, N-Methyl-D-Aspartate; C096406:alpha-phenyl-2-pyridineethanamine dihydrochloride