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Modulation of [3H]flunitrazepam binding to rat cerebellar benzodiazepine receptors by phosphatidylserine.
- Source :
-
European journal of pharmacology [Eur J Pharmacol] 1987 May 07; Vol. 137 (1), pp. 49-58. - Publication Year :
- 1987
-
Abstract
- The influence of phosphatidylserine on ligand binding to the benzodiazepine/GABA receptor complex was assessed in rat cerebellar synaptic membranes and in a detergent-solubilized membrane preparation. Intact synaptic membranes or membranes solubilized with the zwitterionic detergent CHAPS (3-[(3-cholamidopropyl)-dimethylammonio]propanesulfonate) were incubated with a range of concentrations of phosphatidylserine for 2 h at 4 degrees C, prior to use in radioligand binding assays. Phosphatidylserine, an endogenous membrane phospholipid, facilitated the site-specific binding of [3H]flunitrazepam to synaptic membranes and CHAPS-solubilized preparations. In addition, phosphatidylserine inhibited the facilitation of [3H]flunitrazepam binding induced by either cartazolate or gamma-aminobutyric acid (GABA). Although the maximum effect (38% facilitation of [3H]flunitrazepam binding; greater than 90% inhibition of the cartazolate action) was produced using 130 microM phosphatidylserine, a significant enhancement of [3H]flunitrazepam binding could be observed upon preincubation of synaptic membranes with concentrations of phosphatidylserine as low as 5 microM. These results suggest that endogenous phosphatidylserine may play a role in the regulation of benzodiazepine/GABA receptor function, possibly through modulation of the mechanisms which functionally link the various components of this complex receptor system.
- Subjects :
- Animals
Cholic Acids pharmacology
In Vitro Techniques
Pyrazoles pharmacology
Rats
Receptors, GABA-A isolation & purification
Solubility
Synaptic Membranes metabolism
Tritium
gamma-Aminobutyric Acid pharmacology
Cerebellum metabolism
Flunitrazepam metabolism
Phosphatidylserines pharmacology
Receptors, GABA-A metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 0014-2999
- Volume :
- 137
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- European journal of pharmacology
- Publication Type :
- Academic Journal
- Accession number :
- 3038577
- Full Text :
- https://doi.org/10.1016/0014-2999(87)90181-6