Dr. F. Anne Stephenson is Department of Biochemistry, Imperial College of Science and Technology, London SW7 2AZ, England.
Solubilization by CHAPS Detergent of Barbiturate-Enhanced Benzodiazepine-GABA Receptor Complex
Version of Record online: 5 OCT 2006
Journal of Neurochemistry
Volume 39, Issue 6, pages 1579–1586, December 1982
How to Cite
Stephenson, F. A. and Olsen, R. W. (1982), Solubilization by CHAPS Detergent of Barbiturate-Enhanced Benzodiazepine-GABA Receptor Complex. Journal of Neurochemistry, 39: 1579–1586. doi: 10.1111/j.1471-4159.1982.tb07990.x
- Issue online: 5 OCT 2006
- Version of Record online: 5 OCT 2006
- Received April 15, 1982; accepted May 28, 1982
- Cl− channel;
- Soluble receptors
Abstract: Barbiturates enhance the binding of [3H]flunitrazepam to benzodiazepine receptors solubilized with the detergent 3-[(3-cholamidopropyl)-dimethylammonio]propanesulfonate (CHAPS) from bovine cortex. The enhancement by the barbiturates is seen as a decrease in the dissociation constant, Kd, for specific benzodiazepine binding, with no effect on the number of binding sites. The effect of the barbiturates is facilitated by chloride ions, is concentration-dependent, and has a specificity that correlates well with the anesthetic potency of barbiturates. [3H]Flunitrazepam binding activity is stable with storage at 4°C., but barbiturate enhancement of soluble benzodiazepine binding activity decayed rapidly (t1/2= 48 h). [3H]Muscimol binding (GABA receptor) activity was also enhanced by barbiturates. Agarose gel filtration column chromatography of the CHAPS-solubilized receptor proteins showed the same elution profile as receptors solubilized with sodium deoxycholate, and enhancement by barbiturates was observed for both the benzodiazepine and GABA binding activities.