+ 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

Benzodiazepine interactions with GABA receptors



Benzodiazepine interactions with GABA receptors



Neuroscience Letters 47(3): 201-206



Benzodiazepines (BZs) produce most, if not all, of their pharmacological actions by specifically enhancing the effects of endogenous and exogenous GABA that are mediated by GABAA receptors. This potentiation consists in an increase of the apparent affinity of GABA for increasing chloride conductance without increase in its efficacy and, on the single chloride channel level, seems to be the result of an increased probability of channel opening events. Recent studies indicate that the BZR is a site on the GABA receptor (GABA-R)-chloride channel complex, through which the gain of the signal transducer function of the latter is allosterically modulated. The unique feature of this drug receptor, which is located on a neurotransmitter receptor-gated ion channel, is its specific interaction with three classes of ligands. Agonists, competitive antagonists and inverse agonists at BZR, respectively increase, do not alter and reduce the gain of the GABA-R function. Compounds have been found that cover a whole spectrum of transition between the two extremes (partial agonists, partial inverse agonists) and for which interesting therapeutic applications can be foreseen.

Please choose payment method:






(PDF emailed within 0-6 h: $19.90)

Accession: 042375537

Download citation: RISBibTeXText

PMID: 6147796

DOI: 10.1016/0304-3940(84)90514-7


Related references

Radiohistochemical studies of benzodiazepine and GABA receptors and their interactions. Advances in Biochemical Psychopharmacology 26: 53-60, 1981

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, 1987

Interactions between phencyclidine and nmda receptors evidence for a gaba benzodiazepine like supramolecular complex. Pharmacology Biochemistry & Behavior 28(1): 135, 1987

In situ hybridization histochemistry a tool to study cells expressing gaba benzodiazepine receptors and cells affected by gaba benzodiazepine receptor ligands. Experientia 44(ABSTR): A17, 1988

Differential effects of kainic acid on benzodiazepine receptors, GABA receptors, and GABA-modulin in the cerebellar cortex. Advances in Biochemical Psychopharmacology 21: 265-270, 1980

GABA, GABA receptors and benzodiazepine receptors in the human spinal cord: an autoradiographic and immunohistochemical study at the light and electron microscopic levels. Neuroscience 39(2): 361-385, 1990

Acute swim stress increases benzodiazepine receptors, but not GABA-A or GABA-B receptors, in the rat cerebral cortex. Neurochemistry International. 23(4): 327-330, 1993

Chronic exposure of developing cortical neurons to GABA down-regulates GABA/benzodiazepine receptors and GABA-gated chloride currents. Brain Research 501(2): 332-338, 1989

Differences in the pharmacological profiles of benzodiazepine recognition site ligands reflect interactions with heterogeneous population of gaba a receptors. Society for Neuroscience Abstracts 15(1): 641, 1989

Chronic benzodiazepine agonist exposure and its consequences for gaba benzodiazepine interactions. Barnard, E A And E Costa (Ed ) Fidia Research Foundation Symposium Series, Vol 1 Allosteric Modulation Of Amino Acid Receptors: Therapeutic Implications; London, England, Uk, November 1987 Xviii+404p Raven Press: New York, New York, Usa Illus 91-108, 1989

Changes in GABA-benzodiazepine receptor complex and in peripheral benzodiazepine receptors in male mice after copulation. Pharmacology Biochemistry & Behavior. 51(2-3): 529-533, 1995

Multiple benzodiazepine receptor complexes: some benzodiazepine recognition sites are coupled to GABA receptors and ionophores. Advances in Biochemical Psychopharmacology 21: 285-293, 1980

The effect of chronic treatment with peripheral benzodiazepine receptor ligands on behavior and GABA-A/benzodiazepine receptors in rat. Naunyn-Schmiedeberg's Archives of Pharmacology 346(4): 432-436, 1992

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