Novel Benzo[b]quinolizinium Cations as Uncompetitive N-Methyl-D-aspartic Acid (NMDA) Antagonists: The Relationship between log D and Agonist Independent (Closed) NMDA Channel Block

A series of permanently charged benzo[b]quinolizinium cations having lower lipophilicity than MK-801 or phencyclidine (PCP) were synthesized. Data relating agonist independent block of N-methyl-D-aspartic acid (NMDA) ion channels to log D are described. Closed channel access is predicted to result i...

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Veröffentlicht in:	Journal of medicinal chemistry 1995-09, Vol.38 (18), p.3586-3592
Hauptverfasser:	Earley, William G, Kumar, Virendra, Mallamo, John P, Subramanyam, Chakrapani, Dority, John A, Miller, Matthew S, DeHaven-Hudkins, Diane L, Aimone, Lisa D, Kelly, Michael D, Ault, Brian
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Binding Sites Biological and medical sciences Cations Cells, Cultured Dizocilpine Maleate - analogs & derivatives Dizocilpine Maleate - chemistry Female Glutamatergic system (aspartate and other excitatory aminoacids) In Vitro Techniques Medical sciences Mice N-Methylaspartate - antagonists & inhibitors N-Methylaspartate - metabolism Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Oocytes - cytology Pharmacology. Drug treatments Phencyclidine - analogs & derivatives Phencyclidine - chemistry Quinolizines - chemistry Quinolizines - pharmacology Structure-Activity Relationship Xenopus laevis
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