Referenced in: none

Automatically associated channels: Kv10.1

Title: 2,3-Butanedione inactivates the [3H]nitrendipine binding sites, whereas diethylpyrocarbonate does not.

Authors: B Costa, L Giusti, C Martini, A Lucacchini

Journal, date & volume: Neurochem. Int., 1996 Dec , 29, 623-7

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/9113129

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 in critical for [3H]nitrendipine binding.