Competitive inhibition of benzodiazepine binding by fractions from porcine brain.

Competitive inhibition of benzodiazepine binding by fractions from porcine brain.

Fractions of porcine cerebral cortex extract separated by molecular weight on a Sephadex G-75 column were tested for their activities and potencies to inhibit [3H]benzodiazepine binding to rat brain homogenates. The fractions spanned molecular weights from 500 to 100,000. A potent inhibitor (benzodiazepine-competitive factor I, BCF-I) was discovered in the fraction containing substances with mo...

MICROSOME-MEDIATED BENZO[A]PYRENE-DNA BINDING AND INHIBITION BY CYTOSOLIC FRACTIONS FROM LIVER AND SKIN OF ADULT AND WEANLING RATS

Biotransformation of benzo[a]pyrene (BaP) in the presence of microsomal fractions derived from liver and epiderm of adult and weanling rats was examined. The aim of this study was to evaluate the effect of age on the capacity of two organs in transformation of BaP. Subcellular fractions were prepared from skin and liver by ultracentrifugation and were used as the source of BaP metabolizing enzy...

The Non-competitive Inhibition of Brain

A non-competitive inhibition by glucose-6-P1 of brain (1, 2) and other animal tissue (1) hexokinases has been described, as well as a similar inhibition of brain hexokinase by L-sorbose-1-P (3). The present paper is concerned with the specificity for inhibition of brain hexokinase by glucose6-P and related compounds. Ry means of a comparison of the structures of twenty-five compounds, six of xv...

Visualization of specific binding sites of benzodiazepine in human brain.

Using 11C-labeled Ro15-1788 and positron emission tomography, studies of benzodiazepine binding sites in the human brain were performed on four normal volunteers. Rapid and high accumulation of 11C activity was observed in the brain after i.v. injection of [11C]Ro15-1788, the maximum of which was within 12 min. Initial distribution of 11C activity in the brain was similar to the distribution of...

Enzyme-Linked Immunosorbent Assay Competitive Binding Inhibition