Polyamines and the NMDA receptor: Modifying intrinsic activities with aromatic substituents

The inhibiting effects of 34 spermidine and spermine derivatives on the binding of [ 3H]MK-801 to NMDA receptors on rat brain membranes were investigated. Several compounds, including 1c, appeared to inhibit radioligand binding via the polyamine regulatory site, whereas others, including 2c, more li...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2006-06, Vol.16 (11), p.2837-2841
Hauptverfasser:	Berger, Michael L., Bitar, Abdallah Y., Waitner, Matthew J., Rebernik, Patrick, O’Sullivan, Mary C.
Format:	Artikel
Sprache:	eng
Schlagworte:	[ 3H]MK-801 binding Animals Aromatic substituents Biological and medical sciences Glutamatergic system (aspartate and other excitatory aminoacids) Medical sciences Molecular Structure Neuropharmacology Neurotransmitters. Neurotransmission. Receptors NMDA receptor Pharmacology. Drug treatments Polyamines - chemistry Polyamines - metabolism Rats Receptors, N-Methyl-D-Aspartate - antagonists & inhibitors Receptors, N-Methyl-D-Aspartate - metabolism Spermidine Spermine Structure-Activity Relationship
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