title: Heteroatom-substitution as a strategy for increasing the potency of competitive NMDA antagonists.
abstract: We report the synthesis and characterization of compounds that are competitive NMDA receptor antagonists. Significant increases in affinity and potency were obtained by incorporation of a heteroatom into the substructure of the tetrazole-substituted amino acid LY233053.
authors.affiliation: Lilly Research Laboratories, Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, Indiana 46285, USA.
authors.forename: P L
authors.initials: PL
authors.lastname: Ornstein
authors.forename: M B
authors.initials: MB
authors.lastname: Arnold
authors.forename: W H
authors.initials: WH
authors.lastname: Lunn
authors.forename: L J
authors.initials: LJ
authors.lastname: Heinz
authors.forename: J D
authors.initials: JD
authors.lastname: Leander
authors.forename: D
authors.initials: D
authors.lastname: Lodge
authors.forename: D D
authors.initials: DD
authors.lastname: Schoepp
mesh_terms: D000818:Animals; D018691:Excitatory Amino Acid Antagonists / Q000737:chemistry / Q000494:pharmacology*; D051379:Mice; D009474:Neurons / Q000187:drug effects / Q000502:physiology; D010875:Pipecolic Acids / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors*; D013116:Spinal Cord / Q000187:drug effects / Q000502:physiology; D013329:Structure-Activity Relationship; D013777:Tetrazoles / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D018691:Excitatory Amino Acid Antagonists; D010875:Pipecolic Acids; D016194:Receptors, N-Methyl-D-Aspartate; D013777:Tetrazoles; C066685:LY 233053