Abstract
The modification of [3H]nitrendipine binding sites in rabbit brain membranes with 2,3-butanedione and diethylpyrocarbonate was investigated. 2,3-Butanedione, an arginine-specific reagent, causes a dose- and time-dependent decrease in the number of [3H]nitrendipine binding sites without altering its dissociation constant. Scatchard analysis of the binding data shows that 50 mM 2,3-butanedione decreases the binding capacity of [3H]nitrendipine from a control value of 71 ± 6 fmol/mg of protein to 40 ± 3 fmol/mg of protein. Complete and selective protection against inactivation is provided by nifedipine. No decrease of [3H]nitrendipine binding occurs when membranes are pretreated with selective histidine reagent diethylpyrocarbonate. The results indicate that arginine but not histidine residue in l-type calcium channel domain is critical for [3H]nitrendipine binding. Copyright © 1996 Elsevier Science Ltd
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