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Jialie Luo, Wenming Li, Yuming Zhao, Hongjun Fu, Dik-Lung Ma, Jing Tang, Chaoying Li, Robert W Peoples, Fushun Li, Qinwen Wang, Pingbo Huang, Jun Xia, Yuanping Pang, Yifan Han
Uncompetitive N-methyl-d-aspartate (NMDA) receptor antagonists with fast off-rate (UFO) may represent promising drug candidates for various neurodegenerative disorders. In this study, we report that bis(propyl)-cognitin, a novel dimeric acetylcholinesterase inhibitor and gamma-aminobutyric acid subtype A receptor antagonist, is such an antagonist of NMDA receptors. In cultured rat hippocampal neurons, we demonstrated that bis(propyl)-cognitin voltage-dependently, selectively, and moderately inhibited NMDA-activated currents...
June 25, 2010: Journal of Biological Chemistry
Tatsuo Nagata, Susumu Ueno, Hirofumi Morita, Toshiaki Kubota, Yumiko Toyohira, Masato Tsutsui, Akihiko Tawara, Nobuyuki Yanagihara
In the present study, we investigated the direct effects of antiglaucoma drugs (timolol, betaxolol, pilocarpine, and latanoprost) on N-methyl-D-aspartate (NMDA)-receptor function using a Xenopus oocytes expression system and electrophysiological techniques. In oocytes expressing wild-type NMDA (NR1a/NR2A) receptors, timolol and betaxolol significantly inhibited glutamate-evoked currents, whereas less inhibition was obtained with pilocarpine, and latanoprost had few effects. Moreover, the effect of timolol and betaxolol was noncompetitive with respect to glutamate...
March 2008: Journal of Pharmacological Sciences
T Mirshahi, D L Anders, K M Ronald, J J Woodward
Previous studies in this laboratory have shown that the ethanol inhibition of recombinant NMDA receptors expressed in Xenopus oocytes is subunit-dependent, with the NR1/2A receptor being more sensitive than NR1/2C receptors. The ethanol sensitivity of NR1/2A receptors is reduced by substitution of the wild-type NR1-1a (NR1(011)) subunit with the calcium-impermeable NR1 (N616R) subunit. In the present study, the ethanol inhibition of NMDA receptors was determined under different conditions to examine the role that calcium plays in determining the ethanol sensitivity of recombinant NMDA receptors...
September 1998: Journal of Neurochemistry
S F Traynelis, M F Burgess, F Zheng, P Lyuboslavsky, J L Powers
Zinc inhibits NMDA receptor function through both voltage-dependent and voltage-independent mechanisms. In this report we have investigated the role that the NR1 subunit plays in voltage-independent Zn2+ inhibition. Our data show that inclusion of exon 5 into the NR1 subunit increases the IC50 for voltage-independent Zn2+ inhibition from 3-fold to 10-fold when full length exon 22 is also spliced into the mature NR1 transcript and the NMDA receptor complex contains the NR2A or NR2B subunits; exon 5 has little effect on Zn2+ inhibition of receptors that contain NR2C and NR2D...
August 15, 1998: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
F A Boeckman, E Aizenman
The cytotoxicity induced by the transient expression of functional N-methyl-D-aspartate (NMDA) receptors has been examined with the use of a luciferase reporter assay in Chinese hamster ovary cells. Various NMDA receptor antagonists, in a dose-dependent manner, prevented a loss of luciferase activity 24 to 48 hr post-transfection of either the NR1/NR2A or NR1/ NR2B subunit receptor configurations, likely correlating to the time required to express functionally these receptors. Both glutamate and NMDA were potently cytotoxic to transfected cells previously protected by antagonists...
November 1996: Journal of Pharmacology and Experimental Therapeutics
S Kawajiri, R Dingledine
The voltage-dependent block of NMDA channels by Mg2+ is an important functional element of NMDA receptors, since relief of block by depolarization plays a key role in some forms of ischemic neurodegeneration and synaptic plasticity. To identify the relevant structural domains responsible for block by Mg2+ and TCP, we used site-directed mutagenesis to change individual amino acids of the rat NR1A subunit in a transmembrane region (599-DALTLSSAMWFSWGVLLNSGIGE-621, mutated residues underlined) previously shown to donate residues that influence ionic selectivity...
November 1993: Neuropharmacology
T Mirshahi, J J Woodward
In the current study, dimeric and trimeric combinations of N-methyl-D-aspartate (NMDA) receptor subunits were expressed in Xenopus oocytes and their sensitivity to ethanol was examined using conventional two electrode voltage clamp methods. In oocytes expressing the NR1/2A subunits, ethanol (25, 50 and 100 mM) inhibited NMDA (100 microM)/glycine (10 microM) induced currents by 21, 31 and 47%; respectively. NMDA-stimulated currents in oocytes expressing NR1/2B currents were inhibited by 13, 25 and 45% while NR1/NR2C currents were inhibited by 6, 11 and 24%...
March 1995: Neuropharmacology
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