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241459 [2018/11/20 14:26] (current)
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 +====== Stimulation of benzodiazepine receptor binding by gamma-aminobutyric acid.======
 +
 +** Article date:** 1979/2/1
 +~~META:date created = 1979-02-01~~
 +
 +** PubMed ID: 241459 **
 +
 +** Journal name: Proceedings of the National Academy of Sciences of the United States of America (ISSN: 0027-8424) **
 +
 +** ABSTRACT **
 +
 +The effect of the neurotransmitter gamma-aminobutyric acid (GABA) on high-affinity binding of benzodiazepines to brain membranes has been investigated. GABA stimulated [3H]diazepam binding by more than 100% when extensively washed membranes from brain tissue were used. This GABA-stimulated benzodiazepine binding occurred in all brain regions examined. The stimulation was specific for GABA agonist. It was inhibited by the GABA receptor blocker bicuculline methiodide. A large number of compounds structurally closely related to GABA but without direct effect on the GABA receptor failed to enhance [3H]diazepam binding. The stimulation of benzodiazepine binding was caused by an increase in affinity; the number of binding sites remained unchanged. Half-maximal activation of [3H]diazepam binding occurred in the presence of 300 nM muscimol or 900 nM GABA. beta-Guanidinopropionic acid and imidazoleacetic acid were much weaker activators. It is suggested that the described stimulation of benzodiazepine high-affinity binding is mediated by a receptor for GABA. This site of GABA action exhibits different properties when compared to GABA receptors, as characterized by high-affinity binding of GABA agonists.
 +
 +===== ===== 
 +
 +Author List: Karobath M, Sperk G
 +
 +Publication Types: Journal Article
 +
 +Substances mentioned in the article: Receptors, Drug; Muscimol; gamma-Aminobutyric Acid; Diazepam; Bicuculline; ​
 +
 +Mesh terms: Animals; Bicuculline/​pharmacology;​ Brain/​metabolism;​ Cerebral Cortex/​metabolism;​ Diazepam/​metabolism;​ Kinetics; Membranes/​metabolism;​ Muscimol/​pharmacology;​ Rats; Receptors, Drug/drug effects; gamma-Aminobutyric Acid/​pharmacology; ​
 +
 +Citations: ​  - //​[[918669]]//​
 +  - //​[[25362]]//​
 +  - //​[[27722]]//​
 +  - //​[[207386]]//​
 +  - //​[[304755]]//​
 +  - //​[[563985]]//​
 +  - //​[[658148]]//​
 +  - //​[[639861]]//​
 +  - //​[[639854]]//​
 +  - //​[[876354]]//​
 +  - //​[[4405559]]//​
 +  - //​[[242199]]//​
 +  - //​[[241459]]//​
 +
 +{{tag> Bicuculline Diazepam Receptors,​_Drug gamma-Aminobutyric_Acid Muscimol }}
 +
 +{{keywords>​ Bicuculline,​ Diazepam, Receptors, Drug, gamma-Aminobutyric Acid, Muscimol}}
 +
  
241459.txt ยท Last modified: 2018/11/20 14:26 (external edit)