Generation of N-methyl-D-aspartate agonist and competitive antagonist pharmacophore models. Design and synthesis of phosphonoalkyl-substituted tetrahydroisoquinolines as novel antagonists

The preparation and binding affinity of a series of tetrahydroisoquinoline carboxylic acids at the N-methyl-D-aspartate (NMDA) subtype of the glutamate receptor is described, together with a molecular modeling analysis of NMDA agonists and antagonists. Using published NMDA ligands, the active analog...

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Veröffentlicht in:	Journal of medicinal chemistry 1992-04, Vol.35 (8), p.1345-1370
Hauptverfasser:	Ortwine, Daniel F, Malone, Thomas C, Bigge, Christopher F, Drummond, James T, Humblet, Christine, Johnson, Graham, Pinter, Garry W
Format:	Artikel
Sprache:	eng
Schlagworte:	Binding, Competitive Isoquinolines - chemical synthesis Isoquinolines - pharmacology Models, Molecular Molecular Conformation N-Methylaspartate - antagonists & inhibitors Receptors, N-Methyl-D-Aspartate - antagonists & inhibitors Receptors, N-Methyl-D-Aspartate - drug effects Structure-Activity Relationship
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