Referenced in: none

Automatically associated channels: Kir2.3

Title: beta-Carboline inhibition of benzodiazepine receptor binding in vivo.

Authors: K J Fehske, W E Müller

Journal, date & volume: Brain Res., 1982 Apr 22 , 238, 286-91

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/6282397

Abstract
The in vivo potencies of 4 beta-carboline derivatives as inhibitors of benzodiazepine receptor binding were investigated. For all 4 derivatives maximal inhibition was seen within 2 min after i.v. application but decreased continuously for the next 20 min and after this time accounted for less than one-third of maximal inhibition. The in vivo potencies of the beta-carbolines as inhibitors of benzodiazepine receptor binding are much smaller than one would expect from their affinities measured in vitro. Thus, it is assumed than only a small portion of the i.v. dose reaches the brain.