Spermine and Arcaine Block and Permeate N-Methyl-d-Aspartate Receptor Channels
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چکیده
منابع مشابه
Spermine and arcaine block and permeate N-methyl-D-aspartate receptor channels.
Polyamines such as spermine are thought to be endogenous regulators of NMDA (N-methyl-D-aspartate)-type glutamate receptors. Polyamine block of NMDA receptors was studied in excised outside-out patches from rat hippocampal neurons and Xenopus oocytes expressing recombinant receptors. Extracellular spermine and arcaine reduced NMDA single-channel conductance in a voltage-dependent manner, with p...
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متن کاملN-Dansyl-Spermine and N-(n-Octanesulfonyl)-Spermine, Novel Glutamate Receptor Antagonists: Block and Permeation of N-Methyl-D-Aspartate Receptors
Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania (J.C., K.W.), Groupe de Recherche en Thérapeutique Anticancéreuse, URA CNRS 1529, Faculté de Médecine (N.S.) and Chimie Pharmaceutique, Faculté de Pharmacie (J.R.), Université de Rennes 1, F-35043 Rennes Cédex, France, and Faculty of Pharmaceutical Sciences, Chiba University, 1–33 Yayoi-cho, In...
متن کاملThe pore region of N-methyl-D-aspartate receptors differentially influences stimulation and block by spermine.
The transmembrane and pore-forming regions of N-methyl-D-aspartate receptors containing the NR1 and NR2B subunits were studied by measuring the effects of various NR1 and NR2B mutants on stimulation and block by spermine. Block by spermine was predominantly affected by mutations in the M3 segment of NR1 and especially in the M1 and M3 segments of NR2B. These regions are in the outer vestibule o...
متن کاملN1-dansyl-spermine and N1-(n-octanesulfonyl)-spermine, novel glutamate receptor antagonists: block and permeation of N-methyl-D-aspartate receptors.
The effects of several N-sulfonyl-polyamines, including N1-dansyl-spermine (N1-DnsSpm) and N1-(n-octanesulfonyl)-spermine (N1-OsSpm), were studied at recombinant N-methyl-D-aspartate (NMDA) receptors expressed in Xenopus laevis oocytes. N1-DnsSpm and N1-OsSpm inhibited NMDA receptors and were approximately 1000-fold more potent than spermine in oocytes voltage-clamped at -70 mV. Block by N1-Dns...
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ژورنال
عنوان ژورنال: Biophysical Journal
سال: 1999
ISSN: 0006-3495
DOI: 10.1016/s0006-3495(99)77445-x