title: Structure and activity of hydrogenated derivatives of (+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine (MK-801).
abstract: Several hydrogenated derivatives of the potent NMDA antagonist 1 have been prepared and evaluated as competitive inhibitors of [3H]-1 binding. These compounds were also tested for their ability to act as noncompetitive antagonists of NMDA in vitro. These studies indicate that two aromatic rings are not strictly required for high-affinity binding or NMDA antagonism.
authors.affiliation: Merck Sharp and Dohme Research Laboratories, West Point, Pennsylvania 19486.
authors.forename: T A
authors.initials: TA
authors.lastname: Lyle
authors.forename: C A
authors.initials: CA
authors.lastname: Magill
authors.forename: S F
authors.initials: SF
authors.lastname: Britcher
authors.forename: G H
authors.initials: GH
authors.lastname: Denny
authors.forename: W J
authors.initials: WJ
authors.lastname: Thompson
authors.forename: J S
authors.initials: JS
authors.lastname: Murphy
authors.forename: A R
authors.initials: AR
authors.lastname: Knight
authors.forename: J A
authors.initials: JA
authors.lastname: Kemp
authors.forename: G R
authors.initials: GR
authors.lastname: Marshall
authors.forename: D N
authors.initials: DN
authors.lastname: Middlemiss
mesh_terms: D000818:Animals; D000927:Anticonvulsants / Q000494:pharmacology*; D001224:Aspartic Acid / Q000031:analogs & derivatives* / Q000037:antagonists & inhibitors; D003986:Dibenzocycloheptenes / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology*; D016291:Dizocilpine Maleate; D066298:In Vitro Techniques; D008968:Molecular Conformation; D016202:N-Methylaspartate; D051381:Rats; D016194:Receptors, N-Methyl-D-Aspartate; D017981:Receptors, Neurotransmitter / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D000927:Anticonvulsants; D003986:Dibenzocycloheptenes; D016194:Receptors, N-Methyl-D-Aspartate; D017981:Receptors, Neurotransmitter; D001224:Aspartic Acid; D016202:N-Methylaspartate; D016291:Dizocilpine Maleate