PMID: 6109759Jan 1, 1981Paper

Endogenous modulator of benzodiazepine binding in rat cortex

Journal of Neurochemistry
T H Chiu, H C Rosenberg

Abstract

Benzodiazepine binding sites, solubilized with 1% digitonin, were used to study specific [3H]flunitrazepam ([3H]FNP) binding. Specific binding increased nonlinearly with increasing amounts of digitonin extract in the assay. Specific binding was increased, and the relationship to amount of extract became linear, in the presence of 2% polyethylene glycol 6000 (PEG). Heat treatment destroyed binding activity of the extract, but not ability to inhibit [3H]FNP binding. Kinetic analysis showed inhibition to be noncompetitive. The inhibitory activity was sensitive to trypsin. Extracts of repeatedly frozen, thawed, and washed membrane preparations still possessed inhibitory activity. It is suggested that digitonin solubilizes a membrane protein that inhibits benzodiazepine binding. PEG apparently removes this substance from the binding sites.

References

Dec 1, 1978·Proceedings of the National Academy of Sciences of the United States of America·G D ColelloK Folkers
Aug 20, 1979·Life Sciences·M NielsenC Braestrup
Jul 1, 1979·European Journal of Pharmacology·T H Chiu, H C Rosenberg
Feb 1, 1979·Proceedings of the National Academy of Sciences of the United States of America·T Asano, S Spector
Aug 27, 1979·Life Sciences·M GavishS H Snyder
Jul 1, 1978·Proceedings of the Society for Experimental Biology and Medicine·C R Mackerer, R L Kochman
Apr 21, 1977·Nature·R F Squires, C Brastrup
Jan 15, 1980·Biochemical and Biophysical Research Communications·L G Davis, R K Cohen

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Citations

May 18, 1984·European Journal of Pharmacology·J H Skerritt, R L Macdonald
Jan 1, 1988·Life Sciences·C E KetelaarsJ Bruinvels
May 1, 1985·Journal of Neurochemistry·E I TietzH C Rosenberg

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