Modulation of the NMDA receptor by polyamines

Journal Article · Tue Jan 01 04:00:00 EST 1991 · Life Sciences; (USA)

DOI:https://doi.org/10.1016/0024-3205(91)90463-L· OSTI ID:5961715

Williams, K; Romano, C; Dichter, M A; Molinoff, P B ^[1]

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1. Univ. of Pennsylvania School of Medicine, Philadelphia (USA)

Results of recent biochemical and electrophysiological studies have suggested that a recognition site for polyamines exists as part of the NMDA receptor complex. The endogenous polyamines spermine and spermidine increase the binding of open-channel blockers and increase NMDA-elicited currents in cultured neutrons. These polyamines have been termed agonists at the polyamine recognition site. Studies of the effects of natural and synthetic polyamines on the binding of ({sup 3}H)MK-801 and on NMDA-elicited currents in cultured neurons have led to the identification of compounds classified as partial agonists, antagonists, and inverse agonists at the polyamine recognition site. Polyamines have also been found to affect the binding of ligands to the recognition sites for glutamate and glycine. However, these effects may be mediated at a site distinct from that at which polyamines act to modulate the binding of open-channel blockers. Endogenous polyamines may modulate excitatory synaptic transmission by acting at the polyamine recognition site of the NMDA receptor. This site could represent a novel therapeutic target for the treatment of ischemia-induced neurotoxicity, epilepsy, and neurodegenerative diseases.

• OSTI ID: 5961715
• Journal Information: Life Sciences; (USA), Journal Name: Life Sciences; (USA) Vol. 48:6; ISSN 0024-3205; ISSN LIFSA
• Country of Publication: United States
• Language: English

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59 BASIC BIOLOGICAL SCIENCES
AMINES
AMINO ACIDS
ANIMAL CELLS
ASPARTIC ACID
BIOCHEMICAL REACTION KINETICS
BIOLOGICAL EFFECTS
CARBOXYLIC ACIDS
DISEASES
HYDROGEN COMPOUNDS
ISOTOPE APPLICATIONS
KINETICS
LIGANDS
MEMBRANE PROTEINS
NERVE CELLS
NERVOUS SYSTEM DISEASES
ORGANIC ACIDS
ORGANIC COMPOUNDS
PORINS
PROTEINS
REACTION KINETICS
RECEPTORS
SOMATIC CELLS
TRACER TECHNIQUES
TRITIUM COMPOUNDS