+ Site Statistics
+ Search Articles
+ PDF Full Text Service
How our service works
Request PDF Full Text
+ Follow Us
Follow on Facebook
Follow on Twitter
Follow on LinkedIn
+ Subscribe to Site Feeds
Most Shared
PDF Full Text
+ Translate
+ Recently Requested

Functional coupling of gamma-aminobutyric acid (GABA)A and benzodiazepine type II receptors: analysis using purified GABA/benzodiazepine receptor complex from bovine cerebral cortex



Functional coupling of gamma-aminobutyric acid (GABA)A and benzodiazepine type II receptors: analysis using purified GABA/benzodiazepine receptor complex from bovine cerebral cortex



Neuropharmacology 26(12): 1745-1750



Possible functional coupling between gamma-aminobutyric acid (GABA) and benzodiazepine receptors was examined using a purified GABA/benzodiazepine receptor complex. The purified receptor complex was obtained by 1012-S-acetamide adipic hydrazide Sepharose 4B affinity column chromatography, following the solubilization of synaptic membrane from the bovine cerebral cortex with Nonidet P-40. The binding of [3H]GABA to the purified GABA receptor was displaced significantly by muscimol and bicuculline, GABAA receptor agonists and antagonists, respectively, but not by baclofen, a GABAB receptor agonist. On the other hand, the binding of [3H]flunitrazepam to the purified benzodiazepine receptor was found to be displaced by microM ranges of CL 218,872, which is known to be sensitive to the benzodiazepine type II receptor. Furthermore, it was found that the binding of [3H]muscimol to these purified GABAA receptors was enhanced by benzodiazepines, while the binding of [3H]flunitrazepam to these benzodiazepine type II receptors was increased by GABA receptor agonists. These enhancements by GABA agonists and benzodiazepine agonists were found to be blocked by bicuculline and a benzodiazepine receptor antagonist, Ro15-1788, respectively. These results strongly suggest that the purified receptor may consist of GABAA and benzodiazepine type II receptors and possess a functional coupling of these sites, as shown in cerebral synaptic membranes.

Please choose payment method:






(PDF emailed within 1 workday: $29.90)

Accession: 040180795

Download citation: RISBibTeXText

PMID: 2893987


Related references

Neurochemical studies on gamma aminobutyric acid receptor xv pharmacological properties of purified gamma aminobutyric acid a benzodiazepine receptor complex from bovine cerebral cortex and its co purification with sulfur 35 tert butylbicyclophosphorothionate binding site by benzodiazepine affinity column chromatography. Japanese Journal of Pharmacology 40(SUPPL): 134P, 1986

Purification of gamma aminobutyric acid benzodiazepine receptors from bovine cerebral cortex and formation of antibody against the purified receptor. Journal of Neurochemistry 44(SUPPL): S40, 1985

Reconstitution of the purified gamma-aminobutyric acid-benzodiazepine receptor complex from bovine cerebral cortex into phospholipid vesicles. Neuroscience Letters 61(1-2): 165-170, 1985

Interactions of gamma aminobutyric acid gaba beta carbolines and salsolinol at the central gaba benzodiazepine receptor complex. Japanese Journal of Pharmacology 43(SUPPL): 10P, 1987

A gamma-aminobutyric acid/benzodiazepine receptor complex of bovine cerebral cortex. Journal of Biological Chemistry 258(11): 6965-6971, 1983

Purification of gamma aminobutyric acid receptor benzodiazepine receptor and chloride channel from bovine cerebral cortex by benzodiazepine affinity gel column chromatography. Neurochemistry International 10(3): 253-264, 1987

Type I and type II gamma-aminobutyric acid/benzodiazepine receptors: purification and analysis of novel receptor complex from neonatal cortex. Journal of Neurochemistry 52(4): 1114-1122, 1989

Reconstitution of the purified -aminobutyric acid-benzodiazepine receptor complex from bovine cerebral cortex into phospholipid vesicles. Neuroscience Letters 61(1): 165-170, 1985

Purification of gamma-aminobutyric acid (GABA) and benzodiazepine receptors from rat brain using benzodiazepine-affinity column chromatography. Advances in Experimental Medicine and Biology 175: 221-233, 1984

(35)S]TBPS binding to purified benzodiazepine-GABA-ionophore receptor complex: the effect of GABA on the modulation exerted by benzodiazepine site ligands. Neurochemistry International 15(4): 377-379, 1989

Heterogeneity in the allosteric interaction between the gamma-aminobutyric acid (GABA) binding site and three different benzodiazepine binding sites of the GABAA/benzodiazepine receptor complex in the rat nervous system. Journal of Neurochemistry 58(2): 485-493, 1992

Relationships of structure to binding of gamma-aminobutyric acid (GABA) and related compounds with the GABA and benzodiazepine receptors. Research Communications in Chemical Pathology and Pharmacology 43(3): 355-368, 1984

Sulfur 35 labeled tbps binding to purified benzodiazepine gaba ionophore receptor complex the effect of gaba on the modulation exerted by benzodiazepine site ligands. Neurochemistry International 15(4): 377-380, 1989

Neurochemical studies on gamma aminobutyric acid gaba receptor xxii. functional coupling of cerebral gaba b receptor with adenylate cyclase system. Japanese Journal of Pharmacology 46(SUPPL): 203P, 1988

Chronic benzodiazepine antagonist treatment and its withdrawal upregulates components of GABA-benzodiazepine receptor ionophore complex in cerebral cortex of rat. Brain Research 519(1-2): 6-11, 1990