title: Differences in degree of trapping between AR-R15896 and other uncompetitive NMDA receptor antagonists.
abstract: 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.
authors.affiliation: AstraZeneca R&D Boston, Rochester, New York 14602, USA.
authors.forename: T H
authors.initials: TH
authors.lastname: Lanthorn
authors.forename: G A
authors.initials: GA
authors.lastname: Mealing
authors.forename: P
authors.initials: P
authors.lastname: Morley
mesh_terms: D018691:Excitatory Amino Acid Antagonists / Q000494:pharmacology*; D011725:Pyridines / Q000494:pharmacology*; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors*
chemical_list: D018691:Excitatory Amino Acid Antagonists; D011725:Pyridines; D016194:Receptors, N-Methyl-D-Aspartate; C096406:alpha-phenyl-2-pyridineethanamine dihydrochloride