title: Inhibition of [3H]-MK801 binding and protection against NMDA-induced lethality in mice by a series of imipramine analogs.
abstract: A series of imipramine analogs were tested for inhibition of [3H]-MK801 binding and for their ability to protect against NMDA-induced lethality in mice. The structure-activity relationship (SAR) for the inhibition of [3H]-MK801 binding found primary amines on short linkers to be optimum. For protection against NMDA lethality, compounds containing an unsaturated link to a cyclic amine were the most potent analogs tested. Possible explanations for the lack of correlation observed are briefly discussed.
authors.affiliation: Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285.
authors.forename: L A
authors.initials: LA
authors.lastname: McQuaid
authors.forename: J D
authors.initials: JD
authors.lastname: Leander
authors.forename: L G
authors.initials: LG
authors.lastname: Mendelsohn
authors.forename: E C
authors.initials: EC
authors.lastname: Smith
authors.forename: R R
authors.initials: RR
authors.lastname: Lawson
authors.forename: N R
authors.initials: NR
authors.lastname: Mason
mesh_terms: D000818:Animals; D001667:Binding, Competitive; D002462:Cell Membrane / Q000187:drug effects / Q000378:metabolism; D016291:Dizocilpine Maleate / Q000037:antagonists & inhibitors* / Q000378:metabolism; D007099:Imipramine / Q000031:analogs & derivatives* / Q000494:pharmacology*; D008297:Male; D051379:Mice; D016202:N-Methylaspartate / Q000037:antagonists & inhibitors / Q000494:pharmacology*; D016548:Prosencephalon / Q000187:drug effects / Q000378:metabolism; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship
chemical_list: D016202:N-Methylaspartate; D016291:Dizocilpine Maleate; D007099:Imipramine