Abstract：
:A series of protein modifying reagents were tested for their effects on the specific binding of [3H]MK801 to adult rat brain membranes. N-Bromosuccinimide, acetyl imidazole, 2,3-butanedione, 5,5'-dithiobis-(2-nitrobenzoic acid) and dithiothreitol all had no significant effect on binding. The carboxylic acid residue modification reagent, 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide (EDAC), inhibited [3H]MK801 specific binding in a dose-dependent manner with an IC50 = 1.9 mM. The inhibition by EDAC was due to a decrease in the Bmax with no change in KD. The inhibition of [3H]MK801 binding by EDAC was not prevented by prior incubation with competitive antagonists. Protection against EDAC inactivation was obtained, however, in a dose-dependent manner by preincubation with the divalent cations, Ca2+ and Mg2+, but not Zn2+. These results suggest that EDAC modifies an important carboxyl group located within the voltage-dependent Mg2+ binding site of the N-methyl-D-aspartate receptor. This modification yields a decrease in the specific [3H]MK801 binding activity thus demonstrating a close association between the two allosteric regulatory sites.
journal_name
Biochem Pharmacoljournal_title
Biochemical pharmacologyauthors
Chazot PL,Fotherby A,Stephenson FAdoi
10.1016/0006-2952(93)90133-hsubject
Has Abstractpub_date
1993-02-09 00:00:00pages
605-10issue
3eissn
0006-2952issn
1873-2968pii
0006-2952(93)90133-Hjournal_volume
45pub_type
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pub_type： 杂志文章
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更新日期：1992-03-17 00:00:00
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journal_title：Biochemical pharmacology
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