Format

Send to

Choose Destination
Life Sci. 1983 Aug 1;33(5):409-14.

Enhancement of 3H-phenytoin binding by diazepam and (+)bicuculline.

Abstract

3H-Phenytoin binding to the particulate fraction of rat wholebrain homogenate was studied using the filter assay technique. It was found that diazepam and (+)bicuculline methobromide caused a concentration-dependent enhancement of the total binding of 3H-phenytoin, whereas GABA and (-)bicuculline methobromide (the inactive bicuculline isomer) had no effect. In subsequent competition experiments (labelled versus unlabelled phenytoin), it was found that the presence of a potentiating concentration of diazepam transformed the biphasic phenytoin competition isotherm into a simple curve with a Hill coefficient of approximately one, and a Ki of 110 nM.

PMID:
6308373
DOI:
10.1016/0024-3205(83)90788-9
[Indexed for MEDLINE]

Supplemental Content

Loading ...
Support Center