Endogenous indoles as novel polyamine site ligands at the N-methyl- d-aspartate receptor complex

• Published in: Brain research Vol. 890; no. 2; pp. 343 - 346
• Main Authors: Worthen, David R., Gibson, D.Alex, Rogers, Dennis T., Bence, Aimee K., Fu, May, Littleton, John M., Crooks, Peter A.
• Format: Journal Article
• Language: English
• Published: London Elsevier B.V 02.02.2001; Amsterdam Elsevier; New York, NY
• Subjects: Animals; Binding, Competitive - drug effects; Binding, Competitive - physiology; Biogenic Polyamines - chemistry; Biogenic Polyamines - metabolism; Biological and medical sciences; Brain - drug effects; Brain - metabolism; Cell Membrane - drug effects; Cell Membrane - metabolism; Central nervous system; Central neurotransmission. Neuromudulation. Pathways and receptors; CNS; Dizocilpine Maleate - pharmacology; Endogenous indole; Excitatory Amino Acid Antagonists - pharmacology; Fundamental and applied biological sciences. Psychology; indoles; Indoles - chemistry; Indoles - metabolism; Indoles - pharmacology; Ligands; N-Methyl- d-aspartate; Neuroprotection; Neuroprotective Agents - pharmacology; Polyamine recognition domain; polyamines; Radioligand Assay; Rats; Receptors, N-Methyl-D-Aspartate - chemistry; Receptors, N-Methyl-D-Aspartate - drug effects; Receptors, N-Methyl-D-Aspartate - metabolism; spermidine; Spermidine - pharmacology; Subcellular Fractions - chemistry; Subcellular Fractions - drug effects; Subcellular Fractions - metabolism; Tritium; Vertebrates: nervous system and sense organs; Endogenous indole; Neuroprotection; CNS; N-Methyl- d-aspartate; Polyamine recognition domain; Neurotransmitters, modulators, transporters and receptors; Vertebrata; Polyamine; Mammalia; Rat; Indole; Rodentia; Central nervous system; Glutamate receptor; Binding site; NMDA receptor; Brain (vertebrata)
• ISSN: 0006-8993; 1872-6240
• DOI: 10.1016/S0006-8993(00)03201-7

High-throughput ligand displacement screens of a series of endogenous indoles revealed that tryptamine, serotonin and 5-methoxytryptamine readily displace [ 3H]spermidine and [ 3H]MK-801 from their respective binding sites in rat brain homogenate. These data, coupled with their potent inhibition of spermidine-potentiated [ 3H]MK-801 binding, suggest that certain endogenous indoles may act as ligands to one or more polyamine binding sites in the brain, including those on the N-methyl- d-aspartate receptor complex.